Ligand source activities (1 row/activity)





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CHEMBL427807 220164 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayActivity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm990590f
57397279 76774 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC(F)F)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939594 76774 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC(F)F)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
127032015 145416 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3561 116 51 45 -9.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775924 145416 0 None - 1 Mouse 9.4 pEC50 = 9.4 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3561 116 51 45 -9.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127032315 145206 0 None 1 2 Mouse 9.4 pEC50 = 9.4 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3774395 145206 0 None 1 2 Mouse 9.4 pEC50 = 9.4 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL4299295 220341 0 None 1 2 Mouse 9.4 pEC50 = 9.4 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
57390212 76782 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 5 0 5 4.5 CCC(CC)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939601 76782 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 5 0 5 4.5 CCC(CC)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
127030817 145285 0 None 1 2 Mouse 9.2 pEC50 = 9.2 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3824 122 55 49 -12.0 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774939 145285 0 None 1 2 Mouse 9.2 pEC50 = 9.2 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3824 122 55 49 -12.0 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
57395433 76763 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 387 6 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939583 76763 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 387 6 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
11153312 72280 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 383 6 1 6 5.5 CCC(CC)n1ccc2c(Nc3ccc(OC)cc3Cl)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830523 72280 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 383 6 1 6 5.5 CCC(CC)n1ccc2c(Nc3ccc(OC)cc3Cl)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
127033542 145400 0 None 1 2 Mouse 9.1 pEC50 = 9.1 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775796 145400 0 None 1 2 Mouse 9.1 pEC50 = 9.1 Functional
Antagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassayAntagonist activity at CRF-R1 in mouse AtT-20 cells assessed as inhibition of human CRF induced cAMP accumulation after 30 mins by radioimmunoassay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
25115057 76768 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 399 6 0 5 5.4 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939588 76768 0 None - 1 Human 9.0 pEC50 = 9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 399 6 0 5 5.4 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
57393713 76773 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939593 76773 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
57400682 76777 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 359 4 0 5 4.2 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939597 76777 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 359 4 0 5 4.2 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
145958142 168837 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRFR1 expressed in HEK293 cells assessed as inhibition of sauvagine-induced cAMP accumulation by measuring sauvagine EC50 at 1 uM after 30 mins (Rvb = 0.203 nM)Antagonist activity at human CRFR1 expressed in HEK293 cells assessed as inhibition of sauvagine-induced cAMP accumulation by measuring sauvagine EC50 at 1 uM after 30 mins (Rvb = 0.203 nM)
ChEMBL 383 6 1 6 4.8 CCCCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
CHEMBL4160471 168837 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Antagonist activity at human CRFR1 expressed in HEK293 cells assessed as inhibition of sauvagine-induced cAMP accumulation by measuring sauvagine EC50 at 1 uM after 30 mins (Rvb = 0.203 nM)Antagonist activity at human CRFR1 expressed in HEK293 cells assessed as inhibition of sauvagine-induced cAMP accumulation by measuring sauvagine EC50 at 1 uM after 30 mins (Rvb = 0.203 nM)
ChEMBL 383 6 1 6 4.8 CCCCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
57397276 76751 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 373 5 0 5 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939571 76751 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 373 5 0 5 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
57392001 76762 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 6 0 5 4.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939582 76762 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 6 0 5 4.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
57393711 76750 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 5 0 5 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939570 76750 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 5 0 5 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
24758072 76752 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 320 4 0 2 6.1 CCC(CC)c1cc(C)n2nc(-c3ccc(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939572 76752 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 320 4 0 2 6.1 CCC(CC)c1cc(C)n2nc(-c3ccc(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
24758076 76756 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 380 7 0 4 6.1 CCc1cc(OC)c(OC)cc1-c1nn2c(C)cc(C(CC)CC)c2cc1C 10.1016/j.bmc.2011.11.015
CHEMBL1939576 76756 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 380 7 0 4 6.1 CCc1cc(OC)c(OC)cc1-c1nn2c(C)cc(C(CC)CC)c2cc1C 10.1016/j.bmc.2011.11.015
56665181 71534 0 None - 1 Human 7.0 pEC50 = 7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 386 6 1 5 5.6 CCC(CC)Nc1c(C)c(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL1819085 71534 0 None - 1 Human 7.0 pEC50 = 7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 386 6 1 5 5.6 CCC(CC)Nc1c(C)c(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
24758075 76757 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 350 5 0 4 5.3 CCC(CC)c1cc(C)n2nc(-c3cnc(N(C)C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939577 76757 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 350 5 0 4 5.3 CCC(CC)c1cc(C)n2nc(-c3cnc(N(C)C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
10024020 209881 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Effective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell culturesEffective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell cultures
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63989 209881 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Effective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell culturesEffective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell cultures
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
56677028 72073 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 359 7 2 6 4.7 CCC(CC)Nc1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828886 72073 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 359 7 2 6 4.7 CCC(CC)Nc1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
44290322 107947 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Antagonist potency in hCRF1 stimulated adenylate cyclase assayAntagonist potency in hCRF1 stimulated adenylate cyclase assay
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm990590f
CHEMBL295563 107947 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Antagonist potency in hCRF1 stimulated adenylate cyclase assayAntagonist potency in hCRF1 stimulated adenylate cyclase assay
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm990590f
10178898 71515 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 396 6 1 6 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CSC2 10.1016/j.bmc.2011.07.055
CHEMBL1819065 71515 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 396 6 1 6 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CSC2 10.1016/j.bmc.2011.07.055
10024020 209881 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63989 209881 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
57400680 76771 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3cnc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939591 76771 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3cnc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
10177704 71510 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 378 6 1 5 5.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819060 71510 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 378 6 1 5 5.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
56680359 72085 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828897 72085 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
57400681 76775 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 4 0 5 3.8 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939595 76775 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 4 0 5 3.8 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
24758074 76755 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 350 4 0 4 5.6 CCC(CC)c1cc(C)n2nc(-c3cc4c(cc3C)OCO4)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939575 76755 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 350 4 0 4 5.6 CCC(CC)c1cc(C)n2nc(-c3cc4c(cc3C)OCO4)c(C)cc12 10.1016/j.bmc.2011.11.015
25114821 76772 0 None -1 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939592 76772 0 None -1 2 Rat 8.6 pEC50 = 8.6 Functional
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
10222795 71531 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 402 5 1 4 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(Cl)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819082 71531 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 402 5 1 4 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(Cl)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
56668632 71532 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 434 7 1 5 6.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819083 71532 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 434 7 1 5 6.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
56659877 72080 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 9 1 6 5.9 CCCN(CCC)c1c(C(C)C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828892 72080 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 9 1 6 5.9 CCCN(CCC)c1c(C(C)C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56683765 72279 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1nc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830522 72279 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1nc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56683688 72088 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 413 10 0 6 5.3 C=CCN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
CHEMBL1828900 72088 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 413 10 0 6 5.3 C=CCN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
25114821 76772 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939592 76772 0 None 1 2 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
24758071 76753 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 334 4 0 2 6.4 CCC(CC)c1cc(C)n2nc(-c3cc(C)c(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939573 76753 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 334 4 0 2 6.4 CCC(CC)c1cc(C)n2nc(-c3cc(C)c(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL429560 220319 0 None -2 2 Human 8.5 pEC50 = 8.5 Functional
Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayActivity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)CNC(=O)[C@@H](N)CCC(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(N)=O 10.1021/jm990590f
CHEMBL2372650 217058 0 None 3 2 Human 8.5 pEC50 = 8.5 Functional
Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayActivity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O 10.1021/jm990590f
57398970 76765 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 403 7 1 6 4.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939585 76765 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 403 7 1 6 4.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
57402456 76784 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 4 0 5 4.1 CCC(C)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939603 76784 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 4 0 5 4.1 CCC(C)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
11588927 72281 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 377 7 1 6 5.4 CCc1cc(OC)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
CHEMBL1830524 72281 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 377 7 1 6 5.4 CCc1cc(OC)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
57397278 76767 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 379 6 0 5 5.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939587 76767 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 379 6 0 5 5.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
56659949 72282 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 381 6 1 5 6.0 CCc1cc(Cl)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
CHEMBL1830525 72282 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 381 6 1 5 6.0 CCc1cc(Cl)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
56678852 71533 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 372 6 1 5 5.3 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL1819084 71533 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 372 6 1 5 5.3 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
56670271 72283 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 360 5 0 4 5.6 CCC(CC)n1ccc2c(Cc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830526 72283 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 360 5 0 4 5.6 CCC(CC)n1ccc2c(Cc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
57400683 76781 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 4 0 6 3.3 CCC(C)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939600 76781 0 None - 1 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 353 4 0 6 3.3 CCC(C)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
56659947 72272 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 374 7 1 7 4.2 CCC(CC)Nc1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830516 72272 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 374 7 1 7 4.2 CCC(CC)Nc1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL428505 220231 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
Effective concentration to stimulate the human corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayEffective concentration to stimulate the human corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(N)=O 10.1021/jm990590f
136042278 76761 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 359 5 1 4 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939581 76761 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 359 5 1 4 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
11383650 72076 0 None 14 2 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828889 72076 0 None 14 2 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56668633 71535 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
CHEMBL1819086 71535 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
11552261 72284 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 361 5 1 5 5.7 CCC(CC)n1ccc2c(Nc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830527 72284 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 361 5 1 5 5.7 CCC(CC)n1ccc2c(Nc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
57400679 76764 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 383 7 1 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939584 76764 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 383 7 1 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
54754517 72270 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 417 10 0 7 4.8 CCCN(CCC)c1cc(N(COC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830514 72270 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 417 10 0 7 4.8 CCCN(CCC)c1cc(N(COC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
57398972 76783 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 3 0 5 3.8 COc1cc(C)c(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(C)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939602 76783 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 3 0 5 3.8 COc1cc(C)c(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(C)c1 10.1016/j.bmc.2011.11.015
16126888 76749 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 336 5 0 3 5.8 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939569 76749 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 336 5 0 3 5.8 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
10376 9704 4 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
9801039 9704 4 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
CHEMBL1819077 9704 4 None 1 2 Human 7.4 pEC50 = 7.4 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
10376 9704 4 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
9801039 9704 4 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
CHEMBL1819077 9704 4 None -1 2 Rat 7.4 pEC50 = 7.4 Functional
Antagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at rat corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
56683763 72275 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
CHEMBL1830519 72275 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
10135150 71525 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)c(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819075 71525 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)c(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
57390211 76769 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 395 7 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939589 76769 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 395 7 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
57398971 76770 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 393 7 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939590 76770 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 393 7 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
57397277 76766 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 381 6 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939586 76766 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 381 6 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
57393714 76778 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 5 0 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939598 76778 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 367 5 0 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
11703582 72285 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 378 7 0 6 5.4 CCc1ccc(Oc2nc3ccnn3c3c2ccn3C(CC)CC)c(OC)c1 10.1016/j.bmc.2011.08.055
CHEMBL1830528 72285 0 None - 1 Human 8.3 pEC50 = 8.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 378 7 0 6 5.4 CCc1ccc(Oc2nc3ccnn3c3c2ccn3C(CC)CC)c(OC)c1 10.1016/j.bmc.2011.08.055
56673724 72075 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 373 8 1 6 4.8 CCCN(CCC)c1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828888 72075 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 373 8 1 6 4.8 CCCN(CCC)c1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
57393712 76759 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939579 76759 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
56670270 72271 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 374 7 2 7 4.4 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830515 72271 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 374 7 2 7 4.4 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL2373995 217161 0 None -4 2 Human 8.2 pEC50 = 8.2 Functional
Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayActivity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)N[C@@H](CC(=O)O)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)CC(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm990590f
24758073 76754 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 364 7 0 3 6.5 CCOc1ccc(-c2nn3c(C)cc(C(CC)CC)c3cc2C)c(CC)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939574 76754 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 364 7 0 3 6.5 CCOc1ccc(-c2nn3c(C)cc(C(CC)CC)c3cc2C)c(CC)c1 10.1016/j.bmc.2011.11.015
22177839 71511 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 380 6 1 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
CHEMBL1819061 71511 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 380 6 1 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
22177742 71536 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 5.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
CHEMBL1819087 71536 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 5.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
136042277 76760 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 5 1 4 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939580 76760 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 339 5 1 4 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
57402455 76776 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 345 3 0 5 3.8 COc1ccc(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(Cl)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939596 76776 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as CRF-stimulated cAMP accumulation by enzyme immunoassay
ChEMBL 345 3 0 5 3.8 COc1ccc(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(Cl)c1 10.1016/j.bmc.2011.11.015
54754515 72074 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 373 7 2 6 5.0 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828887 72074 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 373 7 2 6 5.0 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
9970050 71514 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 380 6 1 6 4.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
CHEMBL1819064 71514 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 380 6 1 6 4.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
56670201 72086 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 10 0 6 5.6 CCCN(CCC)c1cc(N(CCC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828898 72086 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 10 0 6 5.6 CCCN(CCC)c1cc(N(CCC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56663414 72278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
CHEMBL1830521 72278 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
56668634 71537 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)OCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819088 71537 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)OCC2 10.1016/j.bmc.2011.07.055
54754516 72078 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 1 6 5.3 CCCN(CCC)c1c(CC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828890 72078 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 401 9 1 6 5.3 CCCN(CCC)c1c(CC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
10111139 71526 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4c(C)cc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819076 71526 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4c(C)cc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
11383650 72076 0 None -14 2 Rat 7.1 pEC50 = 7.1 Functional
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828889 72076 0 None -14 2 Rat 7.1 pEC50 = 7.1 Functional
Antagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at rat CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56663337 72087 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 427 10 0 6 5.7 C=C(C)CN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
CHEMBL1828899 72087 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 427 10 0 6 5.7 C=C(C)CN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
56673725 72083 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 403 9 1 7 4.8 CCCN(CCC)c1c(OC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828895 72083 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 403 9 1 7 4.8 CCCN(CCC)c1c(OC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56683762 72274 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830518 72274 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
56659948 72273 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 1 7 4.5 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830517 72273 0 None - 1 Human 8.1 pEC50 = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 388 8 1 7 4.5 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1077301 215270 0 None -8 3 Human 8.0 pEC50 = 8.0 Functional
Activity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assayActivity of peptidic agonists on corticotropin releasing factor receptor using agonist-stimulated adenylate cyclase assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm990590f
22177924 71521 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819071 71521 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
56663335 72079 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 10 1 6 5.7 CCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
CHEMBL1828891 72079 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 415 10 1 6 5.7 CCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
56663336 72084 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828896 72084 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP accumulation after 15 mins by cAMP enzyme immunoassay
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
9865575 210176 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Effective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell culturesEffective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell cultures
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL65484 210176 1 None - 1 Human 6.0 pEC50 = 6.0 Functional
Effective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell culturesEffective dose against human Corticotropin releasing factor receptor 1 stimulated ACTH release from primary rat anterior pituitary cell cultures
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
9865575 210176 1 None - 1 Human 6.0 pEC50 = 6 Functional
Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL65484 210176 1 None - 1 Human 6.0 pEC50 = 6 Functional
Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1Effective dose against CRF stimulated cAMP production in CHO cells expressing human Corticotropin releasing factor receptor 1
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL2370939 216742 0 None 5 2 Human 9.6 pIC50 = 9.6 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]1CCC(=O)NNC(=O)C[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC1=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
10408534 82985 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058338 82985 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL1794009 215714 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@H](C)CC)[C@H](C)CC)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H](C)NC1=O 10.1021/jm0202122
9979210 83062 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 414 5 0 5 5.0 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(N(C)C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058596 83062 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 414 5 0 5 5.0 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(N(C)C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL439883 220628 0 None -1 5 Human 9.1 pIC50 = 9.1 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm0202122
44362115 7952 0 None 2 6 Human 9.0 pIC50 = 9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None None 10.1021/jm0202122
6967 7952 0 None 2 6 Human 9.0 pIC50 = 9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None None 10.1021/jm0202122
CHEMBL1201609 7952 0 None 2 6 Human 9.0 pIC50 = 9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None None 10.1021/jm0202122
CHEMBL440057 7952 0 None 2 6 Human 9.0 pIC50 = 9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None None 10.1021/jm0202122
44587375 200179 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 393 9 0 6 4.8 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL525716 200179 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 393 9 0 6 4.8 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
70688491 83064 0 None - 1 Rat 9.0 pIC50 = 9.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(Cl)cc3OC)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058598 83064 0 None - 1 Rat 9.0 pIC50 = 9.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(Cl)cc3OC)ccnc21 10.1016/j.bmcl.2012.06.034
44610627 146753 0 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production preincubated for 30 mins followed by CRF addition measured after 30 mins by HTRF assayAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production preincubated for 30 mins followed by CRF addition measured after 30 mins by HTRF assay
ChEMBL 519 9 2 8 5.5 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
CHEMBL3799870 146753 0 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production preincubated for 30 mins followed by CRF addition measured after 30 mins by HTRF assayAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production preincubated for 30 mins followed by CRF addition measured after 30 mins by HTRF assay
ChEMBL 519 9 2 8 5.5 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
70690504 82858 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 417 6 0 6 4.2 COCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057479 82858 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 417 6 0 6 4.2 COCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
70682137 83059 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 401 5 0 5 4.9 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058593 83059 0 None - 1 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 401 5 0 5 4.9 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
45483574 204813 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production after 30 mins by HTRF analysisAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production after 30 mins by HTRF analysis
ChEMBL 425 8 1 8 3.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL573978 204813 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production after 30 mins by HTRF analysisAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production after 30 mins by HTRF analysis
ChEMBL 425 8 1 8 3.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
44194976 202713 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production by HTRF methodAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production by HTRF method
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL559437 202713 0 None -7 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production by HTRF methodAntagonist activity at CRF1 receptor in human Y79 cells assessed as inhibition of CRF-stimulated cAMP production by HTRF method
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL2370938 216741 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
9884878 179804 18 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL45187 179804 18 None - 1 Human 8.0 pIC50 = 8 Functional
Antagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassayAntagonist activity at human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells assessed as inhibition of CRF-induced cAMP production after 15 mins by enzyme immunoassay
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL2369741 216444 0 None -2 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0202122
21984762 84317 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 409 8 0 4 5.9 CCc1nn2c(-c3ccc(OC)cc3Cl)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087550 84317 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 409 8 0 4 5.9 CCc1nn2c(-c3ccc(OC)cc3Cl)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
21984648 84319 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087552 84319 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
10378 10757 37 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
11596613 10757 37 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
CHEMBL1287935 10757 37 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
DB12512 10757 37 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
11509708 25764 3 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CC[C@@H](Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
CHEMBL1287905 25764 3 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CC[C@@H](Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
58317452 133264 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 424 5 2 2 6.1 CC(Nc1ccccc1)[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652065 133264 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 424 5 2 2 6.1 CC(Nc1ccccc1)[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
10044263 83066 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 363 5 0 5 4.4 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058600 83066 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 363 5 0 5 4.4 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
9820671 195597 0 None -6 2 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL506214 195597 0 None -6 2 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
58801661 84340 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 495 11 0 8 4.8 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087573 84340 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 495 11 0 8 4.8 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300259r
53357662 133310 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 447 4 1 3 5.8 Cc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1Cl nan
CHEMBL3652110 133310 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 447 4 1 3 5.8 Cc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1Cl nan
58317263 133306 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 435 4 1 3 5.7 O=C(N[C@H]1CC[C@H](Cn2ncc3ccccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652106 133306 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 435 4 1 3 5.7 O=C(N[C@H]1CC[C@H](Cn2ncc3ccccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58398961 143111 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 431 4 1 4 4.6 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3731086 143111 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 431 4 1 4 4.6 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3734018 143111 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 431 4 1 4 4.6 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)ccc3Cl)CC2)c2ccccc21 nan
58317281 133299 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 415 5 3 4 4.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2cc(C(F)(F)F)n[nH]2)CC1 nan
CHEMBL3652099 133299 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 415 5 3 4 4.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2cc(C(F)(F)F)n[nH]2)CC1 nan
CHEMBL2369693 216426 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](C)NC1=O 10.1021/jm0202122
53308745 142352 0 None 67 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 441 4 1 3 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C3(CC3)c3cc(F)ccc32)CC1 nan
CHEMBL3729075 142352 0 None 67 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 441 4 1 3 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C3(CC3)c3cc(F)ccc32)CC1 nan
44446725 175732 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2008.07.063
CHEMBL438888 175732 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2008.07.063
CHEMBL2370930 216738 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm0202122
60155991 84354 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 515 12 0 9 4.8 COCCN(CC1CCOCC1)c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
CHEMBL2087801 84354 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 515 12 0 9 4.8 COCCN(CC1CCOCC1)c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
59186840 133239 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 7 2 4 5.2 CN(C)Cc1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
CHEMBL3652040 133239 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 7 2 4 5.2 CN(C)Cc1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
53341220 142354 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 444 4 1 2 5.6 CC1(C)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3729078 142354 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 444 4 1 2 5.6 CC1(C)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)ccc3Cl)CC2)c2ccccc21 nan
10379 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH productionAntagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
9884366 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH productionAntagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
CHEMBL482950 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH productionAntagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
DB12572 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH productionAntagonist activity at CRF1 receptor in rat pituitary cells assessed as inhibition of CRF-mediated ACTH production
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
44621879 133269 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 443 5 2 3 5.6 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)ncc1F nan
CHEMBL3652070 133269 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 443 5 2 3 5.6 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)ncc1F nan
70694747 83068 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 377 5 0 5 4.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058602 83068 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 377 5 0 5 4.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
70686533 83393 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063381 83393 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
70686533 83393 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063381 83393 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmcl.2012.07.047
44814766 133260 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 342 5 2 2 4.7 O=C(N[C@H]1CC[C@H](CNc2ccccc2)CC1)c1cccc(Cl)c1 nan
CHEMBL3652061 133260 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 342 5 2 2 4.7 O=C(N[C@H]1CC[C@H](CNc2ccccc2)CC1)c1cccc(Cl)c1 nan
53341553 142798 0 None 331 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccc(Cl)cc32)CC1 nan
CHEMBL3731783 142798 0 None 331 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccc(Cl)cc32)CC1 nan
44341743 117360 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 418 8 0 4 5.6 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL325430 117360 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 418 8 0 4 5.6 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
44342075 174652 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 360 6 0 2 6.8 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL431076 174652 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 360 6 0 2 6.8 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL2370931 216739 0 None -2 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NC1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](CCC(N)=O)NC1=O 10.1021/jm0202122
60155887 84348 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 465 9 0 7 5.0 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(OC)nn12 10.1021/jm300259r
CHEMBL2087795 84348 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 465 9 0 7 5.0 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(OC)nn12 10.1021/jm300259r
58317445 131191 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 3 3 6.5 Cc1n[nH]c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1-c1ccccc1 nan
CHEMBL3639509 131191 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 3 3 6.5 Cc1n[nH]c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1-c1ccccc1 nan
58317390 133311 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 427 4 1 3 5.5 Cc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1C nan
CHEMBL3652111 133311 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 427 4 1 3 5.5 Cc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1C nan
59186797 133273 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 401 5 3 4 4.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2n[nH]c3c2CCCC3)CC1 nan
CHEMBL3652074 133273 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 401 5 3 4 4.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2n[nH]c3c2CCCC3)CC1 nan
58398959 142675 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 466 4 1 5 4.4 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ncccc21 nan
CHEMBL3731041 142675 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 466 4 1 5 4.4 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ncccc21 nan
53341428 142997 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 520 4 1 2 6.4 O=C(N[C@H]1CC[C@H](CN2C(=O)C(F)(F)c3ccc(Cl)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3732979 142997 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 520 4 1 2 6.4 O=C(N[C@H]1CC[C@H](CN2C(=O)C(F)(F)c3ccc(Cl)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
70696789 83056 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 425 6 0 5 5.9 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC(C)C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058590 83056 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 425 6 0 5 5.9 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC(C)C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
70686397 83069 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 378 5 0 6 4.1 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)nc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058603 83069 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 378 5 0 6 4.1 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(OC)nc3C)ccnc21 10.1016/j.bmcl.2012.06.034
59186799 133289 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 510 6 3 3 6.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]cc2-c2ccc(Cl)cc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652089 133289 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 510 6 3 3 6.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]cc2-c2ccc(Cl)cc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
44342014 16315 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 392 6 0 5 4.7 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112290 16315 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 392 6 0 5 4.7 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9909978 16810 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL115142 16810 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
21984613 84318 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087551 84318 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
10385822 82855 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)nccc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057476 82855 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)nccc21 10.1016/j.bmcl.2012.06.034
58317503 133302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 475 6 2 4 5.8 COc1ncc(Cl)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652102 133302 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 475 6 2 4 5.8 COc1ncc(Cl)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
53341600 142147 0 None 30 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 439 4 1 3 5.0 Cc1cccc2c1C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
CHEMBL3727810 142147 0 None 30 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 439 4 1 3 5.0 Cc1cccc2c1C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
53341554 142510 0 None 19 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 467 4 1 3 5.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(F)(F)c3ccc(Cl)cc32)CC1 nan
CHEMBL3730045 142510 0 None 19 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 467 4 1 3 5.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(F)(F)c3ccc(Cl)cc32)CC1 nan
67185290 133309 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 483 5 2 4 4.4 Cc1cc(N2CCNC2=O)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652109 133309 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 483 5 2 4 4.4 Cc1cc(N2CCNC2=O)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
53341474 142794 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 482 4 1 2 5.9 C[C@]1(F)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3731745 142794 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 482 4 1 2 5.9 C[C@]1(F)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
62705998 82852 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 406 6 0 7 3.6 CCC(COC)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057473 82852 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 406 6 0 7 3.6 CCC(COC)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
44341832 16190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL111665 16190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
9952997 177382 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of (Corticotropin-Releasing Factor Receptor) CRF-stimulated cAMP productionInhibition of (Corticotropin-Releasing Factor Receptor) CRF-stimulated cAMP production
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL445075 177382 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of (Corticotropin-Releasing Factor Receptor) CRF-stimulated cAMP productionInhibition of (Corticotropin-Releasing Factor Receptor) CRF-stimulated cAMP production
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44341832 16190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL111665 16190 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9908879 16852 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 398 6 0 2 7.1 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115389 16852 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 398 6 0 2 7.1 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
70696576 82358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2046526 82358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70696576 82358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046526 82358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
53341472 142169 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 508 5 1 3 6.0 COc1ccc2c(c1)C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3727976 142169 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 508 5 1 3 6.0 COc1ccc2c(c1)C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
60141295 82363 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 410 9 0 6 5.3 CCN(CC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046534 82363 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 410 9 0 6 5.3 CCN(CC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
58398963 142959 0 None 54 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3cccc(Cl)c32)CC1 nan
CHEMBL3732730 142959 0 None 54 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3cccc(Cl)c32)CC1 nan
59186812 133278 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 5 3 3 5.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3cccc(F)c23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652079 133278 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 5 3 3 5.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3cccc(F)c23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
9821586 174882 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL432800 174882 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
70684375 83388 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 424 9 0 6 4.8 COCCN(C)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063374 83388 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 424 9 0 6 4.8 COCCN(C)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
44816479 133259 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 470 7 2 3 5.8 CN(Cc1cc(-c2ccccc2)n[nH]1)C[C@H]1CC[C@H](NC(=O)c2cc(Cl)ccc2Cl)CC1 nan
CHEMBL3652060 133259 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 470 7 2 3 5.8 CN(Cc1cc(-c2ccccc2)n[nH]1)C[C@H]1CC[C@H](NC(=O)c2cc(Cl)ccc2Cl)CC1 nan
58398949 142097 0 None 109 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 479 5 1 4 5.5 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3727515 142097 0 None 109 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 479 5 1 4 5.5 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
53341019 143018 0 None 16 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 454 6 1 5 4.8 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(CC(C)C)c3ccccc32)CC1 nan
CHEMBL3733118 143018 0 None 16 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 454 6 1 5 4.8 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(CC(C)C)c3ccccc32)CC1 nan
44341739 120278 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 392 6 1 5 4.5 CCCN(CCO)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL332040 120278 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 392 6 1 5 4.5 CCCN(CCO)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL2368116 216366 0 None -43 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
60155989 84352 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 513 11 0 9 4.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4COCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087799 84352 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 513 11 0 9 4.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4COCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
145968888 171937 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4228089 171937 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
58317267 133313 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 414 4 1 4 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C(F)(F)F)cc2C)CC1 nan
CHEMBL3652113 133313 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 414 4 1 4 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C(F)(F)F)cc2C)CC1 nan
44587456 194827 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 344 7 0 5 4.7 CCC(CC)Oc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497652 194827 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 344 7 0 5 4.7 CCC(CC)Oc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
44816314 133236 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ncccc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652037 133236 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ncccc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
58317442 133285 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(Cl)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652085 133285 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(Cl)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
59186841 133240 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 508 6 3 3 6.5 C[C@@H]1C[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC[C@@H]1CNc1cc(-c2ccc(F)cc2)[nH]n1 nan
CHEMBL3652041 133240 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 508 6 3 3 6.5 C[C@@H]1C[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC[C@@H]1CNc1cc(-c2ccc(F)cc2)[nH]n1 nan
70696788 83054 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 411 6 0 5 5.5 CCOc1cc(Cl)c(-c2ccnc3c2nc(C)c(=O)n3C(CC)C2CC2)cc1C 10.1016/j.bmcl.2012.06.034
CHEMBL2058589 83054 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 411 6 0 5 5.5 CCOc1cc(Cl)c(-c2ccnc3c2nc(C)c(=O)n3C(CC)C2CC2)cc1C 10.1016/j.bmcl.2012.06.034
10069877 82857 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 405 6 0 6 4.2 CCC(COC)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057478 82857 0 None - 1 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 405 6 0 6 4.2 CCC(COC)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
60155709 84329 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(OC)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087562 84329 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(OC)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
10200135 84322 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 385 8 0 4 5.9 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3Cl)cccc12 10.1021/jm300259r
CHEMBL2087555 84322 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 385 8 0 4 5.9 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3Cl)cccc12 10.1021/jm300259r
127035055 142433 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 516 4 1 2 6.5 C[C@@]1(F)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2cc(Cl)ccc21 nan
CHEMBL3729578 142433 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 516 4 1 2 6.5 C[C@@]1(F)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2cc(Cl)ccc21 nan
53341116 142587 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 484 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3cc(Cl)ccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3730505 142587 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 484 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3cc(Cl)ccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
10454889 82981 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 421 4 0 4 5.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(C(F)(F)F)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058334 82981 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 421 4 0 4 5.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(C(F)(F)F)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
44129684 171809 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4226158 171809 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
44815438 133242 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 439 5 2 3 5.8 Cc1cc(C)nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
CHEMBL3652043 133242 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 439 5 2 3 5.8 Cc1cc(C)nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
71449705 88283 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(OC)c2nc(-c3c(Cl)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160157 88283 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(OC)c2nc(-c3c(Cl)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
58317483 133255 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 413 4 1 3 5.2 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3652056 133255 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 413 4 1 3 5.2 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
58317373 133283 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)ncc1Cl nan
CHEMBL3652083 133283 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)ncc1Cl nan
44816481 133263 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ccncc1NC[C@H]1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652064 133263 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ccncc1NC[C@H]1CC[C@@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
70690704 83389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063375 83389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
10255153 84334 8 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087549 84334 8 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087567 84334 8 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
70690704 83389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063375 83389 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
44816989 133268 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 3 5.3 O=C(N[C@H]1CC[C@H](CNc2ccc(F)cn2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652069 133268 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 3 5.3 O=C(N[C@H]1CC[C@H](CNc2ccc(F)cn2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58317471 133312 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 461 5 1 3 6.2 O=C(N[C@H]1CC[C@H](Cn2ccc(-c3ccccc3)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652112 133312 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 461 5 1 3 6.2 O=C(N[C@H]1CC[C@H](Cn2ccc(-c3ccccc3)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
70686532 83386 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 408 8 0 5 5.5 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063372 83386 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 408 8 0 5 5.5 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
62705994 83070 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 388 4 0 5 4.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058604 83070 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 388 4 0 5 4.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2369694 216427 0 None -4 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)NC(=O)[C@@H](C)NC(=O)[C@H](CC(C)C)NC1=O 10.1021/jm0202122
53341430 143010 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 426 4 1 4 4.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3cccnc32)CC1 nan
CHEMBL3733081 143010 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 426 4 1 4 4.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3cccnc32)CC1 nan
70690481 82680 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 429 6 1 4 6.6 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2049196 82680 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 429 6 1 4 6.6 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
71458702 88289 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 462 8 0 5 6.2 CCN(CC)c1ccc(C(F)(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160163 88289 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 462 8 0 5 6.2 CCN(CC)c1ccc(C(F)(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
44816824 133267 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 3 5.3 O=C(N[C@H]1CC[C@H](CNc2cncc(F)c2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652068 133267 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 3 5.3 O=C(N[C@H]1CC[C@H](CNc2cncc(F)c2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL526149 222454 10 None -8 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm9000242
53340970 143011 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 427 5 1 6 3.6 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c2ccncc21 nan
CHEMBL3733082 143011 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 427 5 1 6 3.6 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c2ccncc21 nan
53341118 142334 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 496 4 1 2 6.1 CC1(C)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccc(F)cc21 nan
CHEMBL3728921 142334 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 496 4 1 2 6.1 CC1(C)C(=O)N(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccc(F)cc21 nan
71455050 88287 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(Cl)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160161 88287 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(Cl)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
58317277 133271 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 439 6 2 3 5.7 CCc1cncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
CHEMBL3652072 133271 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 439 6 2 3 5.7 CCc1cncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
58317419 133284 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 2 4 5.6 Cn1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3652084 133284 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 2 4 5.6 Cn1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
58317366 133295 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 478 6 2 6 4.7 O=C(N[C@H]1CC[C@H](CNc2nnnn2-c2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652095 133295 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 478 6 2 6 4.7 O=C(N[C@H]1CC[C@H](CNc2nnnn2-c2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58317417 133308 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 414 4 1 4 4.6 Cc1nc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3652108 133308 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 414 4 1 4 4.6 Cc1nc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
70684210 82856 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 5 0 5 4.4 COc1ccc(-c2ccnc3c2nc(C)c(=O)n3C(C2CC2)C2CC2)c(C)c1 10.1016/j.bmcl.2012.06.034
CHEMBL2057477 82856 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 5 0 5 4.4 COc1ccc(-c2ccnc3c2nc(C)c(=O)n3C(C2CC2)C2CC2)c(C)c1 10.1016/j.bmcl.2012.06.034
44341723 174912 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 416 7 0 4 6.3 CCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL432976 174912 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 416 7 0 4 6.3 CCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
70686396 83065 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 413 6 0 6 4.8 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC)cc3OC)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058599 83065 0 None - 1 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 413 6 0 6 4.8 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC)cc3OC)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2370929 216737 0 None -6 2 Human 8.5 pIC50 = 8.5 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCNC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
10075105 84341 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 511 11 0 8 5.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087574 84341 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 511 11 0 8 5.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL1794007 215713 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](N)Cc1ccccc1)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@H](C)CC)[C@H](C)CC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm0202122
3663 106743 83 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationInhibition of recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 10.1021/np1000329
CHEMBL286494 106743 83 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationInhibition of recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 10.1021/np1000329
58317349 133237 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 412 5 2 5 4.9 Cc1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3Cl)CC2)sc1C nan
CHEMBL3652038 133237 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 412 5 2 5 4.9 Cc1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3Cl)CC2)sc1C nan
59186870 133270 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 454 5 3 3 5.4 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3c2CCCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652071 133270 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 454 5 3 3 5.4 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3c2CCCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
71458705 88296 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.5 CCc1cc2c(N(CC)CC)ccc(OC)c2nc1-c1c(OC)cc(COC)cc1OC 10.1016/j.bmc.2012.09.028
CHEMBL2160170 88296 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 438 10 0 6 5.5 CCc1cc2c(N(CC)CC)ccc(OC)c2nc1-c1c(OC)cc(COC)cc1OC 10.1016/j.bmc.2012.09.028
59186828 133282 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 480 6 3 4 5.6 COc1ccc2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2c1 nan
CHEMBL3652082 133282 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 480 6 3 4 5.6 COc1ccc2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2c1 nan
44815273 133262 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 494 6 3 3 6.3 O=C(N[C@H]1CC[C@@H](CNc2cc(-c3ccc(F)cc3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652063 133262 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 494 6 3 3 6.3 O=C(N[C@H]1CC[C@@H](CNc2cc(-c3ccc(F)cc3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
71458704 88292 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 410 9 0 6 4.9 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
CHEMBL2160167 88292 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 410 9 0 6 4.9 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
58317316 133307 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 435 4 1 3 5.7 O=C(N[C@H]1CC[C@H](Cn2cc3ccccc3n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652107 133307 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 435 4 1 3 5.7 O=C(N[C@H]1CC[C@H](Cn2cc3ccccc3n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58317324 133303 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 448 5 3 3 5.4 Cc1n[nH]c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1Cl nan
CHEMBL3652103 133303 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 448 5 3 3 5.4 Cc1n[nH]c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1Cl nan
70692691 82980 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 4 0 4 5.4 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(C)c(C)c3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058333 82980 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 4 0 4 5.4 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(C)c(C)c3C)ccnc21 10.1016/j.bmcl.2012.06.034
44815603 133246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 491 7 2 4 6.1 O=C(N[C@H]1CC[C@H](CNCc2cc(-c3ccccc3)on2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652047 133246 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 491 7 2 4 6.1 O=C(N[C@H]1CC[C@H](CNCc2cc(-c3ccccc3)on2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
53341473 142342 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 509 5 1 4 5.4 COc1cc2c(cn1)C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3729005 142342 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 509 5 1 4 5.4 COc1cc2c(cn1)C(C)(C)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
53357410 133316 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3652116 133316 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
9906984 82958 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 361 3 0 4 4.7 Cc1nc2c(-c3ccc(Cl)cc3Cl)ccnc2n(CC(C)C)c1=O 10.1016/j.bmcl.2012.06.034
CHEMBL2058066 82958 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 361 3 0 4 4.7 Cc1nc2c(-c3ccc(Cl)cc3Cl)ccnc2n(CC(C)C)c1=O 10.1016/j.bmcl.2012.06.034
42618197 191085 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL484158 191085 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
71458703 88290 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 419 8 0 6 5.1 CCN(CC)c1ccc(C#N)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160164 88290 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 419 8 0 6 5.1 CCN(CC)c1ccc(C#N)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
44815437 133241 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 431 5 2 4 5.5 Cc1cnc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)s1 nan
CHEMBL3652042 133241 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 431 5 2 4 5.5 Cc1cnc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)s1 nan
12086065 17607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 406 7 0 5 5.1 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL117209 17607 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 406 7 0 5 5.1 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9908466 121582 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL334039 121582 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
53341173 142085 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 465 4 1 4 5.0 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
CHEMBL3727446 142085 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 465 4 1 4 5.0 Cn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c2ccccc21 nan
62705997 82851 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 376 5 0 6 3.8 COc1ccc(-c2ncnc3c2nc(C)c(=O)n3C(C2CC2)C2CC2)c(C)c1 10.1016/j.bmcl.2012.06.034
CHEMBL2057472 82851 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 376 5 0 6 3.8 COc1ccc(-c2ncnc3c2nc(C)c(=O)n3C(C2CC2)C2CC2)c(C)c1 10.1016/j.bmcl.2012.06.034
59186851 133288 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 3 3 6.5 Cc1c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]c1-c1ccccc1 nan
CHEMBL3652088 133288 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 3 3 6.5 Cc1c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]c1-c1ccccc1 nan
59186801 133298 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 477 6 3 4 5.5 O=C(N[C@H]1CC[C@H](CNc2[nH]ncc2-c2cccnc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652098 133298 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 477 6 3 4 5.5 O=C(N[C@H]1CC[C@H](CNc2[nH]ncc2-c2cccnc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
70688432 82677 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 375 7 1 3 6.8 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049193 82677 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 375 7 1 3 6.8 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
70696935 83384 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 450 11 0 5 6.6 CCCN(CCC)c1ccc(CC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063370 83384 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 450 11 0 5 6.6 CCCN(CCC)c1ccc(CC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
53341596 142440 0 None 79 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 455 5 1 4 4.7 COc1ccc2c(c1)N(C[C@H]1CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC1)C(=O)C2(C)C nan
CHEMBL3729602 142440 0 None 79 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 455 5 1 4 4.7 COc1ccc2c(c1)N(C[C@H]1CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC1)C(=O)C2(C)C nan
42618195 191065 0 None 1 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL483993 191065 0 None 1 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
62705996 83072 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 434 6 0 6 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC(F)F)cc3C)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058606 83072 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 434 6 0 6 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC(F)F)cc3C)ncnc21 10.1016/j.bmcl.2012.06.034
44814573 133235 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cccnc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652036 133235 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cccnc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
58317295 133290 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 406 5 2 4 4.8 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)ncc1Cl nan
CHEMBL3652090 133290 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 406 5 2 4 4.8 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)ncc1Cl nan
44341814 117441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 422 8 0 6 4.4 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL325918 117441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 422 8 0 6 4.4 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
22052143 82959 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 3 0 4 5.3 Cc1nc2c(-c3ccc(Cl)cc3Cl)ccnc2n(C(C)C(C)C)c1=O 10.1016/j.bmcl.2012.06.034
CHEMBL2058067 82959 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 3 0 4 5.3 Cc1nc2c(-c3ccc(Cl)cc3Cl)ccnc2n(C(C)C(C)C)c1=O 10.1016/j.bmcl.2012.06.034
70682294 83392 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
CHEMBL2063380 83392 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
70682294 83392 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063380 83392 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmcl.2012.07.047
60155888 84349 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 481 9 0 7 5.7 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(SC)nn12 10.1021/jm300259r
CHEMBL2087796 84349 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 481 9 0 7 5.7 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(SC)nn12 10.1021/jm300259r
59186815 133244 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3652045 133244 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
3520 10041 54 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassayAntagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300864p
9821250 10041 54 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassayAntagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300864p
CHEMBL309138 10041 54 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassayAntagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300864p
9977800 82975 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058329 82975 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
10339953 82983 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 383 5 0 5 4.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058336 82983 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 383 5 0 5 4.8 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
22052073 82973 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 401 5 0 4 5.8 CCCC(C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058327 82973 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 401 5 0 4 5.8 CCCC(C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
57786006 171742 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 4 0 4 6.4 CCN(CC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4225254 171742 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 422 4 0 4 6.4 CCN(CC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
10362573 82984 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 383 5 0 5 4.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058337 82984 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 383 5 0 5 4.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
70694746 83057 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058591 83057 0 None - 1 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 397 5 0 5 5.1 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
70682138 83063 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 392 4 0 5 5.0 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C#N)c(C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058597 83063 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 392 4 0 5 5.0 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C#N)c(C)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
44194975 203089 16 None -4 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CRF1 receptor in human Y-79 cells assessed as inhibition of CRF-induced cAMP production after 30 mins by HTRF analysisAntagonist activity at CRF1 receptor in human Y-79 cells assessed as inhibition of CRF-induced cAMP production after 30 mins by HTRF analysis
ChEMBL 423 6 1 5 5.5 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL562219 203089 16 None -4 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at CRF1 receptor in human Y-79 cells assessed as inhibition of CRF-induced cAMP production after 30 mins by HTRF analysisAntagonist activity at CRF1 receptor in human Y-79 cells assessed as inhibition of CRF-induced cAMP production after 30 mins by HTRF analysis
ChEMBL 423 6 1 5 5.5 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
44816316 133258 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
CHEMBL3652059 133258 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1cncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
53340971 142124 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 427 4 1 6 3.4 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(C)c3nccc(C)c32)CC1 nan
CHEMBL3727694 142124 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 427 4 1 6 3.4 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(C)c3nccc(C)c32)CC1 nan
71456848 88285 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 394 7 0 5 5.4 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160159 88285 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 394 7 0 5 5.4 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
59186833 133305 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 6 3 3 5.4 CCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
CHEMBL3652105 133305 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 6 3 3 5.4 CCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
53340926 142553 0 None 19 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 463 4 1 3 5.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(F)c3ccc(Cl)cc32)CC1 nan
CHEMBL3730298 142553 0 None 19 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 463 4 1 3 5.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(F)c3ccc(Cl)cc32)CC1 nan
53341018 142722 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 426 5 1 5 4.2 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c2ccccc21 nan
CHEMBL3731280 142722 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 426 5 1 5 4.2 CCn1c(=O)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c2ccccc21 nan
11948286 163448 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4069551 163448 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
70684376 83394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063382 83394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
70684376 83394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063382 83394 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2370917 216731 0 None -34 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
70692846 83387 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 460 10 0 5 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
CHEMBL2063373 83387 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 460 10 0 5 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
70692631 82675 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.bmcl.2012.05.066
CHEMBL2049190 82675 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.bmcl.2012.05.066
53341117 142885 0 None 83 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 468 4 1 2 5.4 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3ccc(F)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3732322 142885 0 None 83 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 468 4 1 2 5.4 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3ccc(F)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
44815110 133256 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 440 6 3 3 5.4 O=C(N[C@H]1CC[C@H](CNc2cc(C3CC3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652057 133256 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 440 6 3 3 5.4 O=C(N[C@H]1CC[C@H](CNc2cc(C3CC3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
53341427 142122 0 None 79 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 425 4 1 3 4.7 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccccc32)CC1 nan
CHEMBL3727689 142122 0 None 79 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 425 4 1 3 4.7 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccccc32)CC1 nan
21984746 84323 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 365 8 0 4 5.5 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3C)cccc12 10.1021/jm300259r
CHEMBL2087556 84323 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 365 8 0 4 5.5 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3C)cccc12 10.1021/jm300259r
9952997 177382 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL445075 177382 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Compound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP productionCompound was tested to inhibit Corticotropin releasing factor receptor 1-stimulated c-AMP production
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
9909978 16810 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL115142 16810 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
70696779 82979 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 361 4 0 4 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(C)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058332 82979 0 None - 1 Rat 8.3 pIC50 = 8.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 361 4 0 4 5.1 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(C)c(C)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2370933 216740 0 None -9 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@](C)(CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)NC(CC(=O)O)C(=O)N[C@@](C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
53341556 142373 0 None 33 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 508 5 1 3 6.0 COc1cccc2c1N(C[C@H]1CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC1)C(=O)C2(C)C nan
CHEMBL3729197 142373 0 None 33 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 508 5 1 3 6.0 COc1cccc2c1N(C[C@H]1CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC1)C(=O)C2(C)C nan
58801647 84342 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 479 10 0 7 5.1 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087575 84342 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 479 10 0 7 5.1 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300259r
59186865 133252 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 410 5 2 2 5.8 O=C(N[C@H]1CC[C@H](CNc2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652053 133252 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 410 5 2 2 5.8 O=C(N[C@H]1CC[C@H](CNc2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
44815774 133257 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 428 5 2 2 5.9 O=C(N[C@H]1CC[C@H](CNc2cccc(F)c2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652058 133257 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 428 5 2 2 5.9 O=C(N[C@H]1CC[C@H](CNc2cccc(F)c2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
3520 10041 54 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptorInhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050384+
9821250 10041 54 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptorInhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050384+
CHEMBL309138 10041 54 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptorInhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050384+
59186804 133265 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 424 5 2 2 6.0 C[C@H]1CC(CNc2ccccc2)CCC1NC(=O)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652066 133265 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 424 5 2 2 6.0 C[C@H]1CC(CNc2ccccc2)CCC1NC(=O)c1cc(C(F)(F)F)ccc1Cl nan
44341636 16467 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 386 6 0 2 7.1 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL113097 16467 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of Corticotropin releasing factor receptor 1-stimulated cAMP productionInhibition of Corticotropin releasing factor receptor 1-stimulated cAMP production
ChEMBL 386 6 0 2 7.1 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
60155540 84347 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 490 10 0 8 4.7 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C#N)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087794 84347 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 490 10 0 8 4.7 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C#N)nn23)c(OC)c1 10.1021/jm300259r
70688490 83061 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 385 5 0 5 4.4 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3F)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058595 83061 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 385 5 0 5 4.4 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3F)ccnc21 10.1016/j.bmcl.2012.06.034
58317486 133294 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 475 6 2 4 5.8 COc1ccc(Cl)c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3652094 133294 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 475 6 2 4 5.8 COc1ccc(Cl)c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
59186805 133280 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 3 3 5.9 Cc1cccc2[nH]nc(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)c12 nan
CHEMBL3652080 133280 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 3 3 5.9 Cc1cccc2[nH]nc(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)c12 nan
59186875 133286 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 465 5 3 4 5.3 Cc1ccc2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2n1 nan
CHEMBL3652086 133286 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 465 5 3 4 5.3 Cc1ccc2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2n1 nan
58317325 133314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1Cl nan
CHEMBL3652114 133314 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1Cl nan
145969226 171776 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4225709 171776 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of human CRF-stimulated cAMP accumulation after 4 hrs by luciferase reporter gene assay
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
11740957 82854 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)nccc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057475 82854 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)nccc21 10.1016/j.bmcl.2012.06.034
70692630 82673 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049188 82673 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation preincubated for 30 mins measured after 30 mins by enzyme immunoassay
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
53341597 142074 0 None 37 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 492 4 1 2 6.3 Cc1cccc2c1N(C[C@H]1CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC1)C(=O)C2(C)C nan
CHEMBL3727391 142074 0 None 37 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 492 4 1 2 6.3 Cc1cccc2c1N(C[C@H]1CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC1)C(=O)C2(C)C nan
71453344 88294 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 444 9 0 6 5.6 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160169 88294 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 444 9 0 6 5.6 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
59186854 133291 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 524 6 3 3 7.1 Cc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1-c1ccc(Cl)cc1 nan
CHEMBL3652091 133291 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 524 6 3 3 7.1 Cc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1-c1ccc(Cl)cc1 nan
53358726 133266 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 374 4 1 4 4.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(C)c2C)CC1 nan
CHEMBL3652067 133266 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 374 4 1 4 4.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(C)c2C)CC1 nan
53341068 142901 0 None 77 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 457 4 1 3 5.2 Cc1cc2c(cc1C)C(C)(F)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
CHEMBL3732415 142901 0 None 77 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 457 4 1 3 5.2 Cc1cc2c(cc1C)C(C)(F)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
21984771 84320 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087553 84320 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
59186844 133293 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 476 6 3 3 6.2 O=C(N[C@H]1CC[C@H](CNc2n[nH]cc2-c2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652093 133293 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 476 6 3 3 6.2 O=C(N[C@H]1CC[C@H](CNc2n[nH]cc2-c2ccccc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58317306 133304 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 524 6 2 4 6.9 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n(-c2ccc(Cl)cc2)n1 nan
CHEMBL3652104 133304 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 524 6 2 4 6.9 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n(-c2ccc(Cl)cc2)n1 nan
53341068 142901 0 None 77 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 457 4 1 3 5.2 Cc1cc2c(cc1C)C(C)(F)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
CHEMBL3732415 142901 0 None 77 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 457 4 1 3 5.2 Cc1cc2c(cc1C)C(C)(F)C(=O)N2C[C@H]1CC[C@H](NC(=O)c2cc(Cl)cnc2C)CC1 nan
59186847 133247 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 445 5 2 4 5.8 Cc1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)sc1C nan
CHEMBL3652048 133247 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 445 5 2 4 5.8 Cc1nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)sc1C nan
44815273 133248 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 494 6 3 3 6.3 O=C(N[C@H]1CC[C@H](CNc2cc(-c3ccc(F)cc3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652049 133248 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 494 6 3 3 6.3 O=C(N[C@H]1CC[C@H](CNc2cc(-c3ccc(F)cc3)n[nH]2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
59186813 133249 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 7 3 3 5.4 CCCc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]1 nan
CHEMBL3652050 133249 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 7 3 3 5.4 CCCc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]1 nan
53341066 142379 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.0 Cc1ncc(C(F)(F)F)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccccc32)CC1 nan
CHEMBL3729224 142379 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 459 4 1 3 5.0 Cc1ncc(C(F)(F)F)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)C(C)(C)c3ccccc32)CC1 nan
53341558 142893 0 None 74 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 429 4 1 3 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)[C@@](C)(F)c3ccccc32)CC1 nan
CHEMBL3732369 142893 0 None 74 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 429 4 1 3 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CN2C(=O)[C@@](C)(F)c3ccccc32)CC1 nan
22052205 82960 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 4 0 4 5.4 CCCC(C)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058068 82960 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 375 4 0 4 5.4 CCCC(C)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
59186819 133272 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 390 5 2 4 4.3 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)ncc1F nan
CHEMBL3652073 133272 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 390 5 2 4 4.3 Cc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)ncc1F nan
59186796 133281 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 484 5 3 3 6.3 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ccc(Cl)cc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652081 133281 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 484 5 3 3 6.3 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ccc(Cl)cc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
71451515 88284 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 405 7 0 6 5.0 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C#N)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160158 88284 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 405 7 0 6 5.0 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C#N)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
22052069 82974 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 377 4 0 5 4.3 COCC(C)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058328 82974 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 377 4 0 5 4.3 COCC(C)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
59186871 133245 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 444 5 2 2 6.4 O=C(N[C@H]1CC[C@H](CNc2ccccc2Cl)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652046 133245 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 444 5 2 2 6.4 O=C(N[C@H]1CC[C@H](CNc2ccccc2Cl)CC1)c1cc(C(F)(F)F)ccc1Cl nan
44815276 133250 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 6 3 3 5.6 CC(C)c1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]1 nan
CHEMBL3652051 133250 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 442 6 3 3 5.6 CC(C)c1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n[nH]1 nan
67238091 133238 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 455 6 3 4 4.9 O=C(O)c1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
CHEMBL3652039 133238 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 455 6 3 4 4.9 O=C(O)c1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
53341425 142730 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 484 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3ccc(Cl)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3731360 142730 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 484 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3ccc(Cl)cc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
71455053 88299 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 482 12 0 7 5.5 COCCN(CC(C)C)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160173 88299 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 482 12 0 7 5.5 COCCN(CC(C)C)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
9908904 187266 4 None -5 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL474287 187266 4 None -5 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475306 187266 4 None -5 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP productionAntagonist activity at CRF1 receptor in rat brain homogenates assessed as inhibition of CRF-stimulted cAMP production
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
44815440 133243 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
CHEMBL3652044 133243 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 425 5 2 3 5.5 Cc1ccc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1 nan
58317463 133253 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 392 5 2 5 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2nc(C)c(C)s2)CC1 nan
CHEMBL3652054 133253 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 392 5 2 5 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2nc(C)c(C)s2)CC1 nan
71453343 88286 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160160 88286 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
59186843 133292 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 451 5 3 4 5.0 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3cccnc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652092 133292 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 451 5 3 4 5.0 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3cccnc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58317395 133296 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 2 4 6.2 Cn1cc(-c2ccccc2)c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3652096 133296 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 490 6 2 4 6.2 Cn1cc(-c2ccccc2)c(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
24971237 194828 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497653 194828 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
57912459 89392 5 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassayAntagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179195 89392 5 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassayAntagonist activity at CRF1 receptor in human IMR32 cells assessed as inhibition of CRF-induced intracellular cAMP accumulation after 30 mins by immunoassay
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
69658040 82982 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 419 6 0 5 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC(F)F)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058335 82982 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 419 6 0 5 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC(F)F)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
10249650 82972 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058326 82972 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
62706160 82853 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 418 6 0 7 3.6 COCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2057474 82853 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 418 6 0 7 3.6 COCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2370916 216730 0 None -13 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagineInhibition of recombinant corticotropin releasing factor receptor 1 assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H](N)CCC(=O)O)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N(C)[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)O)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(N)=O)NC1=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm0202122
70682293 83383 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063369 83383 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
70682293 83383 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063369 83383 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
58317340 133261 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 427 5 2 3 5.7 O=C(N[C@H]1CC[C@H](CNc2cccc3ncccc23)CC1)c1cccc(C(F)(F)F)c1 nan
CHEMBL3652062 133261 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 427 5 2 3 5.7 O=C(N[C@H]1CC[C@H](CNc2cccc3ncccc23)CC1)c1cccc(C(F)(F)F)c1 nan
58317279 133315 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 394 4 1 4 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(Cl)c2C)CC1 nan
CHEMBL3652115 133315 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 394 4 1 4 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(Cl)c2C)CC1 nan
9843598 74550 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptorInhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190845 74550 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptorInhibition of CRF stimulated cAMP production in CHO cells expressing CRF1 receptor
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
58317422 133300 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 376 5 2 4 4.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2ccc(F)cn2)CC1 nan
CHEMBL3652100 133300 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 376 5 2 4 4.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](CNc2ccc(F)cn2)CC1 nan
9908904 187266 4 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
Agonist activity at CRF1 receptor in rat pituitary cellsAgonist activity at CRF1 receptor in rat pituitary cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474287 187266 4 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
Agonist activity at CRF1 receptor in rat pituitary cellsAgonist activity at CRF1 receptor in rat pituitary cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL475306 187266 4 None -5 2 Rat 7.1 pIC50 = 7.1 Functional
Agonist activity at CRF1 receptor in rat pituitary cellsAgonist activity at CRF1 receptor in rat pituitary cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm900025h
10363079 82977 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058330 82977 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 391 5 0 5 4.7 CC[C@@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
71455052 88293 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 9 0 6 5.1 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160168 88293 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 428 9 0 6 5.1 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
9865624 22316 12 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmc.2022.116614
CHEMBL121896 22316 12 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmc.2022.116614
11774042 210131 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmc.2022.116614
CHEMBL65078 210131 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmc.2022.116614
10338811 83067 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 364 5 0 6 3.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)nc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058601 83067 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 364 5 0 6 3.8 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(OC)nc3C)ccnc21 10.1016/j.bmcl.2012.06.034
44815112 133251 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 411 5 2 3 5.2 O=C(N[C@H]1CC[C@H](CNc2cccnc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652052 133251 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 411 5 2 3 5.2 O=C(N[C@H]1CC[C@H](CNc2cccnc2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
59186853 133297 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 4 5.4 Cc1noc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
CHEMBL3652097 133297 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 429 5 2 4 5.4 Cc1noc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
59186802 133287 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 520 7 3 3 6.2 CCCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1Br nan
CHEMBL3652087 133287 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 520 7 3 3 6.2 CCCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1Br nan
11025 9517 7 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptorIn vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptor
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
11713007 9517 7 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptorIn vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptor
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
CHEMBL380800 9517 7 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptorIn vitro inhibition of CRF-stimulated cAMP production in cell membranes expressing human CRF1 receptor
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
10407938 82961 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058069 82961 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 387 4 0 4 5.4 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ccnc21 10.1016/j.bmcl.2012.06.034
70692690 82978 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 347 4 0 4 4.7 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3ccc(C)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058331 82978 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 347 4 0 4 4.7 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3ccc(C)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
58317325 133314 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1Cl nan
CHEMBL3652114 133314 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 459 5 2 3 6.1 Cc1ncc(NC[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1Cl nan
58317360 133274 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 455 6 2 4 5.5 COc1ncc(C)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3652075 133274 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 455 6 2 4 5.5 COc1ncc(C)cc1NC[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
53341022 142957 0 None 41 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 412 4 1 5 3.7 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(C)c3ccccc32)CC1 nan
CHEMBL3732721 142957 0 None 41 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 412 4 1 5 3.7 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2c(=O)n(C)c3ccccc32)CC1 nan
59186825 133276 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 3 3 5.9 Cc1ccc2[nH]nc(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)c2c1 nan
CHEMBL3652077 133276 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 464 5 3 3 5.9 Cc1ccc2[nH]nc(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)c2c1 nan
70909805 146092 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated cAMP accumulation after 4 hrs by steady-glo luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated cAMP accumulation after 4 hrs by steady-glo luciferase reporter gene assay
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3792517 146092 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated cAMP accumulation after 4 hrs by steady-glo luciferase reporter gene assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated cAMP accumulation after 4 hrs by steady-glo luciferase reporter gene assay
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
59186817 133275 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 451 5 3 4 5.0 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ncccc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652076 133275 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 451 5 3 4 5.0 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ncccc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
53341471 142363 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 494 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)C3(CC3)c3cc(F)ccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3729128 142363 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 494 4 1 2 5.9 O=C(N[C@H]1CC[C@H](CN2C(=O)C3(CC3)c3cc(F)ccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
10429933 83060 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 381 5 0 5 4.6 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058594 83060 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 381 5 0 5 4.6 CC[C@H](C1CC1)n1c(=O)c(C)nc2c(-c3cc(F)c(OC)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
70692700 83058 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 433 6 0 5 5.7 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC(F)F)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058592 83058 0 None - 1 Rat 8.0 pIC50 = 8.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 433 6 0 5 5.7 CCC(C1CC1)n1c(=O)c(C)nc2c(-c3cc(Cl)c(OC(F)F)cc3C)ccnc21 10.1016/j.bmcl.2012.06.034
21984718 84321 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087554 84321 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysisAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated cAMP accumulation after 30 mins by fluorescence analysis
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
44816141 133254 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 469 5 2 4 4.1 O=C(N[C@H]1CC[C@H](Cn2ccc(N3CCNC3=O)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652055 133254 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 469 5 2 4 4.1 O=C(N[C@H]1CC[C@H](Cn2ccc(N3CCNC3=O)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
59186860 133277 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 5 3 3 5.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ccc(F)cc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3652078 133277 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 468 5 3 3 5.8 O=C(N[C@H]1CC[C@H](CNc2n[nH]c3ccc(F)cc23)CC1)c1cc(C(F)(F)F)ccc1Cl nan
53341470 142165 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 451 4 1 3 4.6 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3cccnc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3727930 142165 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 451 4 1 3 4.6 O=C(N[C@H]1CC[C@H](CN2C(=O)Cc3cccnc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
53341172 142962 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 451 4 2 3 5.0 O=C(N[C@H]1CC[C@H](Cn2c(=O)[nH]c3ccccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3732765 142962 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assayAntagonist activity against rat/human CRFR1 expressed in CHO cells assessed as inhibition of rat/human CRF-induced cAMP accumulation pre-incubated for 15 mins before CRF stimulation for 30 mins by FRET based HTRF assay
ChEMBL 451 4 2 3 5.0 O=C(N[C@H]1CC[C@H](Cn2c(=O)[nH]c3ccccc32)CC1)c1cc(C(F)(F)F)ccc1Cl nan
71456850 88291 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 424 9 0 6 5.2 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160166 88291 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 424 9 0 6 5.2 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
9822241 70783 8 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human CRF-1 receptor expressed in human IMR-32 cells assessed as effect on cAMP production by ELISA in presence of 3 nM CRFInhibition of human CRF-1 receptor expressed in human IMR-32 cells assessed as effect on cAMP production by ELISA in presence of 3 nM CRF
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
CHEMBL1807053 70783 8 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human CRF-1 receptor expressed in human IMR-32 cells assessed as effect on cAMP production by ELISA in presence of 3 nM CRFInhibition of human CRF-1 receptor expressed in human IMR-32 cells assessed as effect on cAMP production by ELISA in presence of 3 nM CRF
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
70692845 83382 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 422 10 0 5 6.0 CCCN(CCC)c1cccc2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063368 83382 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-stimulated intracellular cAMP accumulation after 30 mins by enzyme immunoassay
ChEMBL 422 10 0 5 6.0 CCCN(CCC)c1cccc2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70692701 83071 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 392 5 0 6 4.1 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
CHEMBL2058605 83071 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Antagonist activity at rat CFR1RAntagonist activity at rat CFR1R
ChEMBL 392 5 0 6 4.1 CC[C@H](COC)n1c(=O)c(C)nc2c(-c3ccc(Cl)cc3Cl)ncnc21 10.1016/j.bmcl.2012.06.034
59186874 133301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 389 7 3 4 4.1 CCCc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n[nH]1 nan
CHEMBL3652101 133301 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.In Vitro Inhibition Assay: Chinese hamster ovary (CHO) cells expressing either the human recombinant CRF-1 or CRF-2a receptors (Chen et al., Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al., Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin (G418). For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) cAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions. CHO cells, previously cryopreserved, were thawed, centrifuged for 7 mins at 1200 rpm and resuspended in serum free media, then pipetted out onto clear bottomed black tissue culture treated 384-well microtitre plates (Corning Inc, US) at 2,000 cells per well. Compounds of the invention, prepared in DMSO, and subsequently diluted 50 fold in assay buffer (1x Hanks balanced salt solution, 0.2% (w/v) bovine serum albumin.
ChEMBL 389 7 3 4 4.1 CCCc1cc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n[nH]1 nan
71462234 88297 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 452 11 0 6 6.0 CCCN(CCC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160171 88297 0 None - 1 Human 7.0 pIC50 = 7 Functional
Antagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassayAntagonist activity at human CRF1 receptor expressed in HEK293 cells assessed as inhibition of CRF-induced intracellular cAMP production preincubated for 30 mins before CRF addition measured after 30 mins by enzyme immunoassay
ChEMBL 452 11 0 6 6.0 CCCN(CCC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
11223423 196321 30 None - 1 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as effect on sauvagine-induced cAMP productionAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as effect on sauvagine-induced cAMP production
ChEMBL 404 4 1 6 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL514270 196321 30 None - 1 Human 7.1 pKd = 7.1 Functional
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as effect on sauvagine-induced cAMP productionAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as effect on sauvagine-induced cAMP production
ChEMBL 404 4 1 6 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
11546255 194896 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1021/jm200365y
CHEMBL498311 194896 0 None - 0 Human 9.7 pKi = 9.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1021/jm200365y
54591779 72804 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 429 8 1 7 4.6 COc1cc(OC(F)F)ccc1-n1c(C)nc2c(NC(C3CC3)C3CC3)nc(C)nc21 10.1016/j.bmcl.2011.08.040
CHEMBL1836947 72804 0 None - 0 Human 9.5 pKi = 9.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 429 8 1 7 4.6 COc1cc(OC(F)F)ccc1-n1c(C)nc2c(NC(C3CC3)C3CC3)nc(C)nc21 10.1016/j.bmcl.2011.08.040
44545165 72802 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 433 7 1 6 5.3 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3Cl)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836945 72802 0 None - 0 Human 9.4 pKi = 9.4 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 433 7 1 6 5.3 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3Cl)c2n1 10.1016/j.bmcl.2011.08.040
9821586 174882 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1021/jm200365y
CHEMBL432800 174882 0 None - 1 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1021/jm200365y
9884878 179804 18 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2011.08.040
CHEMBL45187 179804 18 None - 1 Human 8.8 pKi = 8.8 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2011.08.040
11509708 25764 3 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CC[C@@H](Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
CHEMBL1287905 25764 3 None - 1 Human 8.0 pKi = 8 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CC[C@@H](Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
11509709 25774 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nnc(C)o1 10.1016/j.bmcl.2010.10.095
CHEMBL1287996 25774 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nnc(C)o1 10.1016/j.bmcl.2010.10.095
45485065 203809 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 378 7 0 7 3.5 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C#N)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL567164 203809 0 None - 0 Human 7.0 pKi = 7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 378 7 0 7 3.5 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C#N)cc1C 10.1016/j.bmcl.2009.09.016
56663539 70713 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1c(C)ncc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1021/jm200365y
CHEMBL1806727 70713 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1c(C)ncc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1021/jm200365y
9980466 160907 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 436 9 1 6 5.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1021/jm200365y
CHEMBL398531 160907 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 436 9 1 6 5.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1021/jm200365y
10255153 84334 8 None - 1 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087549 84334 8 None - 1 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087567 84334 8 None - 1 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
56835113 76392 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 408 8 0 5 5.7 CCCCN(CC)c1nc(C)nc2c1c(C)c(COC)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
CHEMBL1934751 76392 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 408 8 0 5 5.7 CCCCN(CC)c1nc(C)nc2c1c(C)c(COC)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
56672697 72797 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 367 5 1 5 4.7 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(Cl)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836940 72797 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 367 5 1 5 4.7 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(Cl)cc3)c2n1 10.1016/j.bmcl.2011.08.040
45485057 203787 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 355 6 2 7 2.9 CC[C@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566939 203787 0 None - 0 Human 6.0 pKi = 6.0 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 355 6 2 7 2.9 CC[C@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485022 203844 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 0 7 3.2 CCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL567383 203844 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 0 7 3.2 CCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
44446725 175732 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL438888 175732 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
3496 7963 42 None - 1 Rat 7.9 pKi = 7.9 Functional
Antagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillationAntagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9862166 7963 42 None - 1 Rat 7.9 pKi = 7.9 Functional
Antagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillationAntagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270948 7963 42 None - 1 Rat 7.9 pKi = 7.9 Functional
Antagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillationAntagonist activity at CRF1 receptor in rat cortical membrane assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
3496 7963 42 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation countingAntagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9862166 7963 42 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation countingAntagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270948 7963 42 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation countingAntagonist activity at human CRF1 receptor assessed as oCRF-stimulated adenylate cyclase activity after 15 mins by liquid scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
3520 10041 54 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
9821250 10041 54 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
CHEMBL309138 10041 54 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
44545284 72803 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 397 6 1 6 4.7 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(Cl)c1 10.1016/j.bmcl.2011.08.040
CHEMBL1836946 72803 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 397 6 1 6 4.7 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(Cl)c1 10.1016/j.bmcl.2011.08.040
45485056 203786 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1nc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)no1 10.1016/j.bmcl.2009.09.016
CHEMBL566938 203786 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1nc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)no1 10.1016/j.bmcl.2009.09.016
45485032 203781 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.0 CCCN(CCO)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566910 203781 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.0 CCCN(CCO)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485040 204063 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL568606 204063 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485040 204063 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2011.08.040
CHEMBL568606 204063 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2011.08.040
45484977 204069 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 383 9 1 7 4.1 CCCC(CCOC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL568656 204069 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 383 9 1 7 4.1 CCCC(CCOC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485009 205215 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.6 CC[C@@H](COC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL577239 205215 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.6 CC[C@@H](COC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
44543774 72790 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 377 6 1 6 4.4 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
CHEMBL1836933 72790 0 None - 0 Human 7.9 pKi = 7.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 377 6 1 6 4.4 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
56658150 72391 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 411 6 1 7 3.4 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(S(C)(=O)=O)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1834003 72391 0 None - 0 Human 6.9 pKi = 6.9 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 411 6 1 7 3.4 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(S(C)(=O)=O)cc3)c2n1 10.1016/j.bmcl.2011.08.040
45485033 203782 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 410 7 0 7 3.1 CCCN(CC(=O)N(C)C)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566911 203782 0 None - 0 Human 5.9 pKi = 5.9 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 410 7 0 7 3.1 CCCN(CC(=O)N(C)C)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
56682683 72791 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 393 8 1 7 3.9 COCc1nc2c(NC(C3CC3)C3CC3)nc(C)nc2n1-c1ccc(OC)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836934 72791 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 393 8 1 7 3.9 COCc1nc2c(NC(C3CC3)C3CC3)nc(C)nc2n1-c1ccc(OC)cc1 10.1016/j.bmcl.2011.08.040
18691322 11433 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 397 2 0 5 5.1 Cc1cc(C)c(-n2nnc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(C)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10315 11433 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 397 2 0 5 5.1 Cc1cc(C)c(-n2nnc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(C)c1 10.1016/s0960-894x(99)00133-x
45484988 204080 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 400 9 0 9 2.7 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)nc1OC 10.1016/j.bmcl.2009.09.016
CHEMBL568685 204080 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 400 9 0 9 2.7 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)nc1OC 10.1016/j.bmcl.2009.09.016
45484992 205681 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 397 8 0 8 3.1 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1cnc(N(C)C)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL584472 205681 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 397 8 0 8 3.1 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1cnc(N(C)C)cc1C 10.1016/j.bmcl.2009.09.016
54591854 72789 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836932 72789 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
45485023 205531 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL583005 205531 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
3533 7989 24 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1021/jm200365y
5282340 7989 24 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1021/jm200365y
CHEMBL291657 7989 24 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1021/jm200365y
3499 8230 28 None -25 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm200365y
9909468 8230 28 None -25 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm200365y
CHEMBL44698 8230 28 None -25 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm200365y
176157 9515 28 None - 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm200365y
3512 9515 28 None - 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm200365y
CHEMBL45281 9515 28 None - 2 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm200365y
44266581 11199 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 398 6 1 4 6.0 CCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1016/s0960-894x(99)00133-x
CHEMBL10154 11199 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 398 6 1 4 6.0 CCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1016/s0960-894x(99)00133-x
3495 7958 28 None -14 2 Human 8.6 pKi = 8.6 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00133-x
5311055 7958 28 None -14 2 Human 8.6 pKi = 8.6 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00133-x
CHEMBL9946 7958 28 None -14 2 Human 8.6 pKi = 8.6 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00133-x
56662343 72799 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 377 7 1 6 4.4 CCOc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836942 72799 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 377 7 1 6 4.4 CCOc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
18691310 11379 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 508 4 1 7 5.3 COc1cc(Br)c(-n2c(O)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10279 11379 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 508 4 1 7 5.3 COc1cc(Br)c(-n2c(O)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
44266488 105300 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 493 4 0 7 5.0 COc1cc(Br)c(-n2nnc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL276263 105300 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 493 4 0 7 5.0 COc1cc(Br)c(-n2nnc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
45485034 203783 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.6 CC[C@H](COC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566912 203783 0 None - 0 Human 6.7 pKi = 6.7 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 1 7 3.6 CC[C@H](COC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
44446726 101609 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 476 11 0 3 7.5 CCCN(CCC)c1c(C)nc(-c2c(CC(F)F)cc(CC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253699 101609 0 None - 0 Human 7.7 pKi = 7.7 Functional
Antagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulationAntagonist activity at CRF1 receptor expressed in mouse AtT20 cells assessed as inhibition of sauvagine-stimulated cAMP accumulation
ChEMBL 476 11 0 3 7.5 CCCN(CCC)c1c(C)nc(-c2c(CC(F)F)cc(CC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
18691303 11073 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 512 6 1 7 5.9 COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2[N+](=O)[O-])c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10080 11073 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 512 6 1 7 5.9 COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2[N+](=O)[O-])c(OC)c1 10.1016/s0960-894x(99)00133-x
52947302 25760 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 392 5 1 8 4.2 COc1ccc(-c2c(C)nn3c(NC(C)c4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287878 25760 0 None - 0 Human 7.6 pKi = 7.6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 392 5 1 8 4.2 COc1ccc(-c2c(C)nn3c(NC(C)c4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
45484976 203843 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 420 8 2 9 3.3 CCCNCc1cncn1Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL567382 203843 0 None - 0 Human 5.6 pKi = 5.6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 420 8 2 9 3.3 CCCNCc1cncn1Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
11697131 25775 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4nnc(C)o4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287997 25775 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4nnc(C)o4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
56682684 72795 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 439 7 1 6 5.2 COc1ccc(-n2c(C3CC(F)(F)C3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836938 72795 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 439 7 1 6 5.2 COc1ccc(-n2c(C3CC(F)(F)C3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
45485079 203870 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 396 8 1 7 2.7 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C(N)=O)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL567538 203870 0 None - 0 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 396 8 1 7 2.7 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C(N)=O)cc1C 10.1016/j.bmcl.2009.09.016
3495 7958 28 None -14 2 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm200365y
5311055 7958 28 None -14 2 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm200365y
CHEMBL9946 7958 28 None -14 2 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm200365y
3520 10041 54 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
9821250 10041 54 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
CHEMBL309138 10041 54 None - 1 Human 8.5 pKi = 8.5 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
9955329 214609 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 448 8 0 8 3.9 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00133-x
CHEMBL9633 214609 0 None - 0 Human 8.5 pKi = 8.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 448 8 0 8 3.9 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00133-x
9934089 11779 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00133-x
CHEMBL10504 11779 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00133-x
3520 10041 54 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2010.10.095
9821250 10041 54 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2010.10.095
CHEMBL309138 10041 54 None - 1 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2010.10.095
56658860 72792 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 403 8 1 6 4.7 COc1ccc(-n2c(CC3CC3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836935 72792 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 403 8 1 6 4.7 COc1ccc(-n2c(CC3CC3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
11509641 25765 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 404 5 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC4(c5nc(C)no5)CC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287936 25765 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 404 5 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC4(c5nc(C)no5)CC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
11531570 25771 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287966 25771 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
45485105 204207 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 367 8 1 6 4.8 CCCC(CCC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL569666 204207 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 367 8 1 6 4.8 CCCC(CCC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
177990 7214 23 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.bmcl.2011.10.066
3489 7214 23 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.bmcl.2011.10.066
CHEMBL296641 7214 23 None - 1 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.bmcl.2011.10.066
46175148 72806 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2ncc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
CHEMBL1836950 72806 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2ncc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
18691329 11175 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 506 4 0 6 5.9 COc1cc(Br)c(-n2c(C)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10142 11175 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 506 4 0 6 5.9 COc1cc(Br)c(-n2c(C)nc3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
44266555 11232 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 502 3 0 5 7.5 CSc1nn(-c2c(Cl)cc(Cl)cc2Cl)c2nc(C)nc(-c3ccccc3C(F)(F)F)c12 10.1016/s0960-894x(99)00133-x
CHEMBL10174 11232 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 502 3 0 5 7.5 CSc1nn(-c2c(Cl)cc(Cl)cc2Cl)c2nc(C)nc(-c3ccccc3C(F)(F)F)c12 10.1016/s0960-894x(99)00133-x
45485086 203703 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 381 8 1 6 5.1 CCCC(CCC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566279 203703 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 381 8 1 6 5.1 CCCC(CCC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
10375 9516 18 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm200365y
9888194 9516 18 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm200365y
CHEMBL188907 9516 18 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm200365y
45485080 203903 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 420 8 2 9 3.3 CCCNCc1nccn1Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL567741 203903 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 420 8 2 9 3.3 CCCNCc1nccn1Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485073 203556 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 353 6 1 6 4.4 CCC(CC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL565442 203556 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 353 6 1 6 4.4 CCC(CC)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45484980 204072 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 384 8 0 8 3.0 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)nc1C 10.1016/j.bmcl.2009.09.016
CHEMBL568665 204072 0 None - 0 Human 7.4 pKi = 7.4 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 384 8 0 8 3.0 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)nc1C 10.1016/j.bmcl.2009.09.016
56676057 72788 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2cnc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
CHEMBL1836931 72788 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2cnc3c(NC(C4CC4)C4CC4)nc(C)nc32)c(C)c1 10.1016/j.bmcl.2011.08.040
44545161 72801 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 399 7 1 6 4.6 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836944 72801 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 399 7 1 6 4.6 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
11589539 25759 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 0 8 4.0 CCN(Cc1nc(C)no1)c1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2010.10.095
CHEMBL1287877 25759 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 0 8 4.0 CCN(Cc1nc(C)no1)c1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2010.10.095
10367821 11077 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 478 5 0 4 6.9 CCN(c1nc(C)nc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00133-x
CHEMBL10082 11077 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 478 5 0 4 6.9 CCN(c1nc(C)nc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00133-x
52944875 25770 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 418 5 1 8 4.5 COc1ccc(-c2c(C)nn3c(NC4(c5nc(C)no5)CCC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287965 25770 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 418 5 1 8 4.5 COc1ccc(-c2c(C)nn3c(NC4(c5nc(C)no5)CCC4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
52947334 25779 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 420 6 1 9 4.0 CCC(Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
CHEMBL1288027 25779 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 420 6 1 9 4.0 CCC(Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
11531898 25784 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 422 7 1 9 4.3 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
CHEMBL1288058 25784 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 422 7 1 9 4.3 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
57390674 76391 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 392 7 0 5 5.4 CCCCN(CC)c1nc(C)nc2c1c(C)c(C=O)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
CHEMBL1934750 76391 0 None - 0 Human 7.3 pKi = 7.3 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 392 7 0 5 5.4 CCCCN(CC)c1nc(C)nc2c1c(C)c(C=O)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
45485042 204146 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 2 7 3.3 CCC[C@@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL569202 204146 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 2 7 3.3 CCC[C@@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
45485008 205149 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 397 8 1 8 2.1 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C(N)=O)nc1C 10.1016/j.bmcl.2009.09.016
CHEMBL576639 205149 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 397 8 1 8 2.1 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C(N)=O)nc1C 10.1016/j.bmcl.2009.09.016
56835112 76390 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 394 7 1 5 5.1 CCCCN(CC)c1nc(C)nc2c1c(C)c(CO)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
CHEMBL1934749 76390 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assayAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells by cAMP assay
ChEMBL 394 7 1 5 5.1 CCCCN(CC)c1nc(C)nc2c1c(C)c(CO)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2011.10.066
10378 10757 37 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
11596613 10757 37 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
CHEMBL1287935 10757 37 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
DB12512 10757 37 None - 1 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 10.1016/j.bmcl.2010.10.095
18691308 11098 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 482 5 2 6 5.6 COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2N)c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10091 11098 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 482 5 2 6 5.6 COc1cc(Br)c(Nc2nc(C)nc(-c3ccccc3C(F)(F)F)c2N)c(OC)c1 10.1016/s0960-894x(99)00133-x
56672696 72793 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 405 8 1 6 4.9 COc1ccc(-n2c(CC(C)C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836936 72793 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 405 8 1 6 4.9 COc1ccc(-n2c(CC(C)C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
56682685 72796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 358 5 1 6 3.9 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(C#N)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836939 72796 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 358 5 1 6 3.9 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(C#N)cc3)c2n1 10.1016/j.bmcl.2011.08.040
45485045 204028 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 355 6 2 7 2.9 CC[C@@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL568397 204028 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 355 6 2 7 2.9 CC[C@@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
11538121 25756 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 378 5 1 8 3.6 COc1ccc(-c2c(C)nn3c(NCc4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1287848 25756 0 None - 0 Human 7.2 pKi = 7.2 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 378 5 1 8 3.6 COc1ccc(-c2c(C)nn3c(NCc4nc(C)no4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
45485078 205561 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 389 7 0 8 3.0 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C#N)cc1C#N 10.1016/j.bmcl.2009.09.016
CHEMBL583223 205561 0 None - 0 Human 6.2 pKi = 6.2 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 389 7 0 8 3.0 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(C#N)cc1C#N 10.1016/j.bmcl.2009.09.016
44545396 72805 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 417 7 1 6 4.8 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3F)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836948 72805 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 417 7 1 6 4.8 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3F)c2n1 10.1016/j.bmcl.2011.08.040
10377 7962 27 None 3 2 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activityAntagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activity
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
9818802 7962 27 None 3 2 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activityAntagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activity
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
CHEMBL270738 7962 27 None 3 2 Rat 8.1 pKi = 8.1 Functional
Antagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activityAntagonist activity at rat cortex CRF1 receptor assessed as inhibition of CRF-stimulated adenylate cyclase activity
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
11545949 25763 10 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
CHEMBL1287904 25763 10 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.6 CCC(Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12)c1nc(C)no1 10.1016/j.bmcl.2010.10.095
45485064 205564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 399 9 0 8 3.3 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1OC 10.1016/j.bmcl.2009.09.016
CHEMBL583237 205564 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 399 9 0 8 3.3 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1OC 10.1016/j.bmcl.2009.09.016
45485035 203665 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 2 7 3.3 CCC[C@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL566073 203665 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 369 7 2 7 3.3 CCC[C@H](CO)Nc1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
52947738 25778 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4noc(C)n4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
CHEMBL1288026 25778 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptorAntagonist activity at human recombinant CRF1 receptor
ChEMBL 406 6 1 8 4.1 COc1ccc(-c2c(C)nn3c(NC(C)Cc4noc(C)n4)cc(C)nc23)c(C)c1 10.1016/j.bmcl.2010.10.095
3520 10041 54 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300259r
9821250 10041 54 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300259r
CHEMBL309138 10041 54 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulationAntagonist activity at human CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF-stimulated cAMP accumulation
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm300259r
10377 7962 27 None -3 2 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cellsAntagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
9818802 7962 27 None -3 2 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cellsAntagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
CHEMBL270738 7962 27 None -3 2 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cellsAntagonist activity at human CRF1 receptor endogenously expressed in human IMR32 cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
45485050 203985 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1noc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)n1 10.1016/j.bmcl.2009.09.016
CHEMBL568188 203985 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1noc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)n1 10.1016/j.bmcl.2009.09.016
45484981 205152 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 339 6 1 6 4.0 CCC(CC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL576664 205152 0 None - 0 Human 7.1 pKi = 7.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 339 6 1 6 4.0 CCC(CC)Nc1nc(C)nc2c1cnn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2009.09.016
56662342 72794 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 419 7 1 7 4.6 COc1ccc(-n2c(C3CCCO3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836937 72794 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 419 7 1 7 4.6 COc1ccc(-n2c(C3CCCO3)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
24971237 194828 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1021/jm200365y
CHEMBL497653 194828 0 None - 1 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human CRF-1 receptorAntagonist activity at human CRF-1 receptor
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1021/jm200365y
22004628 205085 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 365 6 0 5 5.0 CCCCN(CC)c1nc(C)nc2c1c(C)nn2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2009.09.016
CHEMBL576049 205085 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 365 6 0 5 5.0 CCCCN(CC)c1nc(C)nc2c1c(C)nn2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2009.09.016
56672698 72800 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 417 6 1 6 4.9 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836943 72800 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 417 6 1 6 4.9 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
18691298 104935 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 423 2 0 3 7.0 Cc1cc(C)c(-n2c(C)c(C)c3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(C)c1 10.1016/s0960-894x(99)00133-x
CHEMBL273839 104935 0 None - 0 Human 8.0 pKi = 8.0 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 423 2 0 3 7.0 Cc1cc(C)c(-n2c(C)c(C)c3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(C)c1 10.1016/s0960-894x(99)00133-x
44545281 72798 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 351 5 1 5 4.2 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836941 72798 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formationAntagonist activity at recombinant human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP formation
ChEMBL 351 5 1 5 4.2 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
18691301 11096 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 522 4 0 7 4.9 COc1cc(Br)c(-n2c(=O)n(C)c3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
CHEMBL10090 11096 0 None - 0 Human 7.0 pKi = 7.0 Functional
Antagonistic activity for Corticotropin releasing factor receptor 1Antagonistic activity for Corticotropin releasing factor receptor 1
ChEMBL 522 4 0 7 4.9 COc1cc(Br)c(-n2c(=O)n(C)c3c(-c4ccccc4C(F)(F)F)nc(C)nc32)c(OC)c1 10.1016/s0960-894x(99)00133-x
45485041 204064 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1nnc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)o1 10.1016/j.bmcl.2009.09.016
CHEMBL568607 204064 0 None - 0 Human 6.0 pKi = 6 Functional
Antagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP productionAntagonist activity at human recombinant CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-induced cAMP production
ChEMBL 422 8 2 10 3.4 CCCNCc1nnc(Nc2nc(C)nc3c2c(C)nn3-c2ccc(OC)cc2C)o1 10.1016/j.bmcl.2009.09.016
10379 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonism of CRF-mediated ACTH production in rat pituitary cells.Antagonism of CRF-mediated ACTH production in rat pituitary cells.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
9884366 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonism of CRF-mediated ACTH production in rat pituitary cells.Antagonism of CRF-mediated ACTH production in rat pituitary cells.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
CHEMBL482950 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonism of CRF-mediated ACTH production in rat pituitary cells.Antagonism of CRF-mediated ACTH production in rat pituitary cells.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
DB12572 9833 39 None -1 3 Rat 6.9 pIC50 = 6.9 Functional
Antagonism of CRF-mediated ACTH production in rat pituitary cells.Antagonism of CRF-mediated ACTH production in rat pituitary cells.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
3498 7987 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 7 0 5 7.2 CCN(c1ccc(cc1SC)C(C)C)c1nc(cc(n1)C)N1CCC(=CC1)c1cccc(c1)F 10357258
9849313 7987 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 7 0 5 7.2 CCN(c1ccc(cc1SC)C(C)C)c1nc(cc(n1)C)N1CCC(=CC1)c1cccc(c1)F 10357258
CHEMBL297986 7987 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 7 0 5 7.2 CCN(c1ccc(cc1SC)C(C)C)c1nc(cc(n1)C)N1CCC(=CC1)c1cccc(c1)F 10357258
3496 7963 42 None - 1 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18288792
9862166 7963 42 None - 1 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18288792
CHEMBL270948 7963 42 None - 1 Rat 8.3 pIC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18288792
10376 9704 4 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 21865047
9801039 9704 4 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 21865047
CHEMBL1819077 9704 4 None 1 2 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 21865047
16133798 7294 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12361401
925 7294 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12361401
3495 7958 28 None 14 2 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 8874139
5311055 7958 28 None 14 2 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 8874139
CHEMBL9946 7958 28 None 14 2 Rat 9.9 pIC50 = 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 8874139
10335 7295 0 None -389 2 Human 6.3 pIC50 > 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12361401
90488758 7295 0 None -389 2 Human 6.3 pIC50 > 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12361401




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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DOI

CHEMBL264275 217390 0 None - 0 Mouse 7.0 pEC50 = 7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL442112 220685 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL263862 217375 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL427923 220173 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL427811 220165 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL437089 220483 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438391 220547 0 None - 0 Mouse 6.9 pEC50 = 6.9 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL414130 219891 0 None - 0 Mouse 6.8 pEC50 = 6.8 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL439883 220628 0 None - 1 Mouse 7.8 pEC50 = 7.8 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438220 220535 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL410568 219605 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
44362115 7952 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None None 10.1021/jm049490m
6967 7952 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None None 10.1021/jm049490m
CHEMBL1201609 7952 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None None 10.1021/jm049490m
CHEMBL440057 7952 0 None - 0 Mouse 7.7 pEC50 = 7.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None None 10.1021/jm049490m
CHEMBL428127 220196 0 None - 0 Mouse 6.7 pEC50 = 6.7 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL415130 219949 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438601 220561 0 None - 0 Mouse 6.6 pEC50 = 6.6 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL412296 219761 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL429403 220307 0 None - 0 Mouse 6.5 pEC50 = 6.5 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL427611 220134 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL428809 220253 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL268549 217537 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL428296 220214 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL409748 219560 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL427792 220162 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438760 220573 0 None - 0 Mouse 6.4 pEC50 = 6.4 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL413414 219843 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL267635 217505 0 None - 0 Mouse 7.3 pEC50 = 7.3 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL429547 220318 0 None - 0 Mouse 6.3 pEC50 = 6.3 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL410814 219623 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL429719 220322 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438210 220533 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL411590 219729 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438948 220595 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438928 220591 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL412026 219750 0 None - 0 Mouse 7.2 pEC50 = 7.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL437289 220494 0 None - 0 Mouse 6.2 pEC50 = 6.2 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL439102 220601 0 None - 0 Mouse 6.1 pEC50 = 6.1 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL438939 220594 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL428824 220256 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL436912 220475 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL436914 220476 0 None - 0 Mouse 7.1 pEC50 = 7.1 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL430078 220387 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL441929 220681 0 None - 0 Mouse 6.0 pEC50 = 6.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL414711 219927 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
CHEMBL410347 219592 0 None - 0 Mouse 7.0 pEC50 = 7.0 Binding
In vitro effective concentration for mouse corticotropin releasing factor 1 receptorIn vitro effective concentration for mouse corticotropin releasing factor 1 receptor
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1021/jm049490m
44596586 205555 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 398 7 1 6 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL583153 205555 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 398 7 1 6 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
44596589 204943 3 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL574852 204943 3 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
44596589 204943 3 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL574852 204943 3 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
44194976 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL559437 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
44194976 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL559437 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
44194976 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900302q
CHEMBL559437 202713 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 377 7 1 6 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900302q
44190059 202028 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL551033 202028 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
44596809 205670 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 362 6 1 6 4.0 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL584343 205670 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 362 6 1 6 4.0 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
44596589 204943 3 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
CHEMBL574852 204943 3 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
44190148 202785 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 7 1 6 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL560036 202785 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 7 1 6 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
44596812 205583 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 384 6 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1OC(F)F 10.1021/jm900716v
CHEMBL583387 205583 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 384 6 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1OC(F)F 10.1021/jm900716v
44596812 205583 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 384 6 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2010.01.129
CHEMBL583387 205583 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 384 6 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2010.01.129
11420978 18536 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 402 7 1 5 4.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1Cl 10.1021/jm049737f
CHEMBL1181645 18536 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 402 7 1 5 4.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1Cl 10.1021/jm049737f
CHEMBL187073 18536 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 402 7 1 5 4.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1Cl 10.1021/jm049737f
44190143 201620 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 5 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900301y
CHEMBL539670 201620 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 5 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900301y
44190143 201620 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 347 5 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
CHEMBL539670 201620 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 347 5 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
44190915 202783 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 401 6 1 5 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL560033 202783 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 401 6 1 5 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1021/jm900302q
71580213 95207 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 409 9 1 6 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
CHEMBL2349558 95207 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 409 9 1 6 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
71580215 95209 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 493 9 1 6 5.0 COc1cc(Cl)c(Nc2nc(Br)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
CHEMBL2349560 95209 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 493 9 1 6 5.0 COc1cc(Cl)c(Nc2nc(Br)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
44190828 203088 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 423 6 1 5 5.5 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL562218 203088 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 423 6 1 5 5.5 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
11384238 73624 0 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 406 6 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1021/jm049737f
CHEMBL186203 73624 0 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 406 6 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1021/jm049737f
44596588 204643 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 414 8 1 7 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL572589 204643 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 414 8 1 7 3.9 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
9931946 18542 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 420 7 1 5 4.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1cc(F)c(OC)cc1Cl 10.1021/jm049737f
CHEMBL1181679 18542 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 420 7 1 5 4.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1cc(F)c(OC)cc1Cl 10.1021/jm049737f
CHEMBL188464 18542 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 420 7 1 5 4.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1cc(F)c(OC)cc1Cl 10.1021/jm049737f
45266992 202855 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL560634 202855 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1021/jm900301y
44190242 201988 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 385 5 1 4 5.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(Cl)cc2Cl)c1=O 10.1021/jm900301y
CHEMBL550686 201988 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 385 5 1 4 5.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(Cl)cc2Cl)c1=O 10.1021/jm900301y
44190242 201988 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 385 5 1 4 5.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(Cl)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL550686 201988 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 385 5 1 4 5.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(Cl)cc2Cl)c1=O 10.1021/jm900302q
44190144 202244 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 7 1 6 3.9 CC[C@H](COC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL552504 202244 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 7 1 6 3.9 CC[C@H](COC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
71580214 95208 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 449 9 1 6 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
CHEMBL2349559 95208 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 449 9 1 6 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
71580426 95218 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 345 6 1 5 3.8 COc1cc(C)c(Nc2nc(C)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
CHEMBL2349570 95218 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 345 6 1 5 3.8 COc1cc(C)c(Nc2nc(C)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
44190058 202823 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 8 1 5 5.4 CCCC(CCC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL560350 202823 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 377 8 1 5 5.4 CCCC(CCC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
44190446 203457 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 379 4 0 5 4.2 COc1cc(Cl)c2c(c1)CCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
CHEMBL564588 203457 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 379 4 0 5 4.2 COc1cc(Cl)c2c(c1)CCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
44189950 203288 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL563489 203288 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
44189950 203288 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900302q
CHEMBL563489 203288 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900302q
56961965 88772 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 425 8 1 7 3.2 COCC(COC)n1cc(Br)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165202 88772 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 425 8 1 7 3.2 COCC(COC)n1cc(Br)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
46881748 13697 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 5 1 6 3.7 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1N(C)C 10.1016/j.bmcl.2010.01.129
CHEMBL1084423 13697 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 5 1 6 3.7 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1N(C)C 10.1016/j.bmcl.2010.01.129
10027220 73639 0 None - 1 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 458 7 1 4 6.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
CHEMBL186252 73639 0 None - 1 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 458 7 1 4 6.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
44610627 146753 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 519 9 2 8 5.5 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
CHEMBL3799870 146753 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 519 9 2 8 5.5 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
46881834 14514 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 400 8 1 7 3.5 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2ccc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1089036 14514 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 400 8 1 7 3.5 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2ccc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
44190057 202327 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 349 6 1 5 4.6 CCC(CC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL554517 202327 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 349 6 1 5 4.6 CCC(CC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
45483573 204944 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 395 6 1 7 3.8 Cc1nc(OC(F)F)c(C#N)cc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900716v
CHEMBL574853 204944 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 395 6 1 7 3.8 Cc1nc(OC(F)F)c(C#N)cc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900716v
10363553 73600 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 399 8 1 7 3.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm0611410
CHEMBL186097 73600 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 399 8 1 7 3.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm0611410
10363553 73600 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 399 8 1 7 3.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm049737f
CHEMBL186097 73600 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 399 8 1 7 3.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm049737f
45483574 204813 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 425 8 1 8 3.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL573978 204813 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 425 8 1 8 3.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
44190145 201987 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 351 6 1 6 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL550685 201987 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 351 6 1 6 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
46891155 14008 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 342 6 1 6 3.7 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1085753 14008 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 342 6 1 6 3.7 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
44191013 203027 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 391 4 1 4 5.6 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561758 203027 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 391 4 1 4 5.6 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1=O 10.1021/jm900302q
11752878 19035 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 414 7 1 4 5.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL1184703 19035 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 414 7 1 4 5.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL364883 19035 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 414 7 1 4 5.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
11417694 74227 0 None - 1 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm0611410
CHEMBL189089 74227 0 None - 1 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm0611410
11417694 74227 0 None - 1 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm049737f
CHEMBL189089 74227 0 None - 1 Rat 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm049737f
44190447 203083 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 423 4 0 5 4.3 COc1cc(Br)c2c(c1)CCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
CHEMBL562161 203083 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 423 4 0 5 4.3 COc1cc(Br)c2c(c1)CCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
44191012 203015 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 351 4 1 4 4.9 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900302q
CHEMBL561698 203015 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 351 4 1 4 4.9 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900302q
42618183 186592 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 393 8 0 7 3.9 C=CCN(CC=C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL474498 186592 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 393 8 0 7 3.9 C=CCN(CC=C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
42618197 191085 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL484158 191085 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
44194975 203089 16 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 423 6 1 5 5.5 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL562219 203089 16 None - 0 Rat 9.0 pIC50 = 9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 423 6 1 5 5.5 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
71580425 95217 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 365 6 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
CHEMBL2349569 95217 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 365 6 1 5 4.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
44596808 205019 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 378 7 1 7 3.3 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL575491 205019 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 378 7 1 7 3.3 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
46891337 13182 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082349 13182 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
46891439 13839 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COC[C@@H](C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1084987 13839 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COC[C@@H](C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
44190826 201599 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 387 5 1 5 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900301y
CHEMBL539184 201599 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 387 5 1 5 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900301y
44190826 201599 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 387 5 1 5 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900302q
CHEMBL539184 201599 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 387 5 1 5 4.9 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1021/jm900302q
42618199 190943 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 437 9 0 8 3.3 COCCN(CCOC)c1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL482982 190943 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 437 9 0 8 3.3 COCCN(CCOC)c1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
42618197 191085 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL484158 191085 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 391 6 1 6 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
3499 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2016.03.067
9909468 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2016.03.067
CHEMBL44698 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2016.03.067
127047546 146436 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 441 8 1 8 4.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3797830 146436 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 441 8 1 8 4.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
46881792 14106 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 402 5 1 6 4.3 COc1nc(C(F)(F)F)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
CHEMBL1086179 14106 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 402 5 1 6 4.3 COc1nc(C(F)(F)F)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
46881793 14108 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 370 6 1 6 3.9 Cc1nc(OC(F)F)ccc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1086180 14108 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 370 6 1 6 3.9 Cc1nc(OC(F)F)ccc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
46881835 14515 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 400 8 1 7 3.5 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1089037 14515 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 400 8 1 7 3.5 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
44190149 201839 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
CHEMBL549538 201839 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
44190450 202437 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 432 5 1 6 4.1 COc1ccc(Nc2nc(Br)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL556462 202437 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 432 5 1 6 4.1 COc1ccc(Nc2nc(Br)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL1077301 215270 0 None - 2 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1016/j.bmcl.2010.01.129
42618181 191137 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 0 7 3.6 CCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL484420 191137 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 0 7 3.6 CCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
3499 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm900302q
9909468 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm900302q
CHEMBL44698 8230 28 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm900302q
44190149 201839 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL549538 201839 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
44190829 202080 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 371 4 1 4 5.2 Cc1cc(Cl)cc(Cl)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
CHEMBL551433 202080 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 371 4 1 4 5.2 Cc1cc(Cl)cc(Cl)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
44190913 202724 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 361 6 1 5 4.6 CCOc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
CHEMBL559507 202724 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 361 6 1 5 4.6 CCOc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
11246513 73634 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCN(CCC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL186241 73634 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCN(CCC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL526149 222454 10 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm9000242
44629380 146664 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 508 8 2 9 4.7 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccc(C#N)c3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799337 146664 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 508 8 2 9 4.7 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccc(C#N)c3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44189947 201879 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL549875 201879 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 6 1 5 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
44191008 203036 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 439 5 1 4 6.3 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561819 203036 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 439 5 1 4 6.3 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
45483576 205144 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 425 8 1 8 3.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL576589 205144 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 425 8 1 8 3.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C#N)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
44189951 201806 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 349 6 1 5 4.2 CC[C@H](COC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL549329 201806 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 349 6 1 5 4.2 CC[C@H](COC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
44591500 196511 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCN(c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12)C1CC1 10.1021/jm9000242
CHEMBL515740 196511 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCN(c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12)C1CC1 10.1021/jm9000242
44596810 204781 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 348 5 1 6 3.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900716v
CHEMBL573748 204781 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 348 5 1 6 3.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900716v
44596807 204876 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 378 7 1 7 3.3 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL574436 204876 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 378 7 1 7 3.3 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
44629379 146463 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 517 8 2 8 5.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3Cl)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3797992 146463 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 517 8 2 8 5.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3Cl)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44629309 146597 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 483 8 2 8 4.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3798885 146597 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 483 8 2 8 4.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccccc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
127047519 146686 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 468 8 1 8 4.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccccc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799452 146686 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 468 8 1 8 4.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccccc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
127047547 146855 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 519 8 1 8 4.8 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cc(Br)ccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3800497 146855 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 519 8 1 8 4.8 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cc(Br)ccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44596807 204876 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 378 7 1 7 3.3 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
CHEMBL574436 204876 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 378 7 1 7 3.3 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
44190340 202249 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 373 6 0 4 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(N(CC)c2cc(C)c(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL552559 202249 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 373 6 0 4 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(N(CC)c2cc(C)c(C)cc2C)c1=O 10.1021/jm900301y
44190337 202912 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 391 8 1 6 4.3 CCOc1cc(C)c(Nc2nc(Cl)cn([C@@H](COC)C3CC3)c2=O)cc1C 10.1021/jm900301y
CHEMBL561097 202912 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 391 8 1 6 4.3 CCOc1cc(C)c(Nc2nc(Cl)cn([C@@H](COC)C3CC3)c2=O)cc1C 10.1021/jm900301y
44596810 204781 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 348 5 1 6 3.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
CHEMBL573748 204781 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 348 5 1 6 3.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
11211931 131121 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 406 5 1 5 4.5 CCN(c1cc(C)nc2c1NC(=O)CN2c1cc(F)c(OC)cc1Cl)C(C)C 10.1021/jm049737f
CHEMBL363654 131121 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 406 5 1 5 4.5 CCN(c1cc(C)nc2c1NC(=O)CN2c1cc(F)c(OC)cc1Cl)C(C)C 10.1021/jm049737f
54582097 67813 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 372 7 0 7 3.3 CCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762820 67813 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 372 7 0 7 3.3 CCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
44596587 204642 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 388 7 1 7 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
CHEMBL572588 204642 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 388 7 1 7 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1021/jm900716v
127047548 146464 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 509 8 1 8 5.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccc(C(F)(F)F)cn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3798004 146464 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 509 8 1 8 5.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccc(C(F)(F)F)cn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44629378 146612 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 517 8 2 8 5.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccc(Cl)cc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799036 146612 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 517 8 2 8 5.5 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccc(Cl)cc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44190449 202756 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 388 5 1 6 4.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.01.129
CHEMBL559764 202756 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 388 5 1 6 4.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.01.129
42618230 198117 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 380 7 0 7 3.7 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL519159 198117 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 380 7 0 7 3.7 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
44191010 201926 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 6 1 5 5.6 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL550216 201926 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 6 1 5 5.6 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
42618198 190942 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 377 5 0 6 4.1 CCN(CC)c1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL482981 190942 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 377 5 0 6 4.1 CCN(CC)c1nc(C)nc2c(-c3cc(F)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
44596701 204812 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 353 6 1 7 3.2 CC[C@H](C1CC1)n1cc(C#N)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL573976 204812 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 353 6 1 7 3.2 CC[C@H](C1CC1)n1cc(C#N)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
44629377 146743 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 551 8 2 8 6.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cc(Cl)cc(Cl)c3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799825 146743 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 551 8 2 8 6.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cc(Cl)cc(Cl)c3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44629312 146839 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 551 8 2 8 6.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccc(Cl)cc3Cl)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3800413 146839 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 551 8 2 8 6.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3ccc(Cl)cc3Cl)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44190145 201987 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 6 1 6 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL550685 201987 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 6 1 6 3.5 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
44189946 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.01.129
44189946 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1021/jm900301y
CHEMBL558280 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.01.129
CHEMBL558280 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1021/jm900301y
44189946 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1021/jm900302q
CHEMBL558280 202607 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)c1 10.1021/jm900302q
44190918 202784 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 400 6 1 6 4.4 CC[C@H](COC)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL560034 202784 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 400 6 1 6 4.4 CC[C@H](COC)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
42618187 186943 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 397 8 0 7 4.4 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL474901 186943 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 397 8 0 7 4.4 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
42618188 186057 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 399 8 0 8 3.2 CCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL473075 186057 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 399 8 0 8 3.2 CCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
44190449 202756 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 388 5 1 6 4.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL559764 202756 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 388 5 1 6 4.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
42618189 196469 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 425 9 0 8 3.6 COCCN(CC1CC1)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL515396 196469 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 425 9 0 8 3.6 COCCN(CC1CC1)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
44190823 202976 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 6 1 5 6.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561416 202976 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 6 1 5 6.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
11154464 74244 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 423 6 1 5 5.0 CCCN(CC1CCC1)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL189196 74244 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 423 6 1 5 5.0 CCCN(CC1CCC1)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
42618172 186777 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 376 6 0 7 3.6 COc1ccc(-c2c(C)nn3c(N(CCC#N)C4CC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
CHEMBL474701 186777 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 376 6 0 7 3.6 COc1ccc(-c2c(C)nn3c(N(CCC#N)C4CC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
52918270 67814 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 402 9 0 8 2.9 COCCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762821 67814 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 402 9 0 8 2.9 COCCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
44629381 146738 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 520 9 2 9 4.8 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccnc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
CHEMBL3799784 146738 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 520 9 2 9 4.8 Cc1cc(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccnc3)C3CC3)c2=O)c(C)nc1OC(F)F 10.1016/j.bmcl.2016.03.067
42618196 198252 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 371 6 1 6 4.5 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL519340 198252 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 371 6 1 6 4.5 CCC(CC)Nc1nc(C)nc2c(-c3cc(F)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
42618170 187618 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 379 7 0 6 4.4 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475706 187618 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 379 7 0 6 4.4 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
42618195 191065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL483993 191065 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
21984762 84317 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 409 8 0 4 5.9 CCc1nn2c(-c3ccc(OC)cc3Cl)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087550 84317 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 409 8 0 4 5.9 CCc1nn2c(-c3ccc(OC)cc3Cl)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
44596702 204726 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 339 5 1 7 2.9 COc1nc(C)c(Nc2nc(C#N)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900716v
CHEMBL573284 204726 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 339 5 1 7 2.9 COc1nc(C)c(Nc2nc(C#N)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900716v
46891188 13416 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 4 1 6 4.5 Cc1nc(Nc2c(Cl)cc(C#N)c(Cl)c2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083343 13416 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 4 1 6 4.5 Cc1nc(Nc2c(Cl)cc(C#N)c(Cl)c2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
44629310 146676 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 484 8 2 9 4.3 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799417 146676 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 484 8 2 9 4.3 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)Nc3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
58280026 146860 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 449 9 2 8 3.7 CCCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
CHEMBL3800523 146860 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 449 9 2 8 3.7 CCCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
44190147 203523 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 6 2 6 3.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](CO)C3CC3)c2=O)cc1C 10.1021/jm900301y
CHEMBL565169 203523 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 6 2 6 3.2 COc1cc(C)c(Nc2nc(Cl)cn([C@@H](CO)C3CC3)c2=O)cc1C 10.1021/jm900301y
24768326 104552 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 0 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)nc2C)c1C 10.1021/jm070578k
CHEMBL271762 104552 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 0 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)nc2C)c1C 10.1021/jm070578k
10295702 129678 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 420 6 0 4 5.7 CCCC(C1CC1)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL360589 129678 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 420 6 0 4 5.7 CCCC(C1CC1)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
11306819 19180 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1C#N 10.1021/jm049737f
CHEMBL1185802 19180 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1C#N 10.1021/jm049737f
CHEMBL433592 19180 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1C#N 10.1021/jm049737f
24768326 104552 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 0 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)nc2C)c1C 10.1021/jm070578k
CHEMBL271762 104552 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 0 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)nc2C)c1C 10.1021/jm070578k
9927970 104512 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL271558 104512 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
9819482 164326 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.2 CCC(COC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL408028 164326 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.2 CCC(COC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
70692631 82675 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.ejmech.2021.114085
CHEMBL2049190 82675 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.ejmech.2021.114085
70692631 82675 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.bmcl.2012.05.066
CHEMBL2049190 82675 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.bmcl.2012.05.066
17961227 101182 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 483 6 0 3 8.2 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL250982 101182 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 483 6 0 3 8.2 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
44589204 196280 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 384 3 0 7 4.3 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL513967 196280 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 384 3 0 7 4.3 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
21912321 104555 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 4 0 4 4.6 Cc1cc(C)c(Oc2nc(C)cc(OC3CCOC3)c2C)c(C)c1 10.1021/jm070578k
CHEMBL271770 104555 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 4 0 4 4.6 Cc1cc(C)c(Oc2nc(C)cc(OC3CCOC3)c2C)c(C)c1 10.1021/jm070578k
57785838 171884 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 503 6 0 6 6.3 CCc1nc(C)nc(CC)c1N1CCCn2c1nc1c(Cl)ccc(C(OC(F)F)C(F)(F)F)c12 10.1016/j.bmc.2018.01.020
CHEMBL4227282 171884 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 503 6 0 6 6.3 CCc1nc(C)nc(CC)c1N1CCCn2c1nc1c(Cl)ccc(C(OC(F)F)C(F)(F)F)c12 10.1016/j.bmc.2018.01.020
11122528 72002 0 None - 1 Human 6.0 pIC50 = 6 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 413 10 0 7 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182643 72002 0 None - 1 Human 6.0 pIC50 = 6 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 413 10 0 7 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
58223462 135588 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 10 0 9 4.7 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(C=O)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3669429 135588 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 10 0 9 4.7 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(C=O)cc3OC)csc12)C1CCOCC1 nan
57912458 89381 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 10 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179184 89381 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 10 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
71458703 88290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 419 8 0 6 5.1 CCN(CC)c1ccc(C#N)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160164 88290 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 419 8 0 6 5.1 CCN(CC)c1ccc(C#N)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
24768342 92353 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 364 6 1 6 4.2 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(C#N)cc1C 10.1021/jm0611410
CHEMBL228130 92353 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 364 6 1 6 4.2 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(C#N)cc1C 10.1021/jm0611410
21912321 104555 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 4 0 4 4.6 Cc1cc(C)c(Oc2nc(C)cc(OC3CCOC3)c2C)c(C)c1 10.1021/jm070578k
CHEMBL271770 104555 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 4 0 4 4.6 Cc1cc(C)c(Oc2nc(C)cc(OC3CCOC3)c2C)c(C)c1 10.1021/jm070578k
71462234 88297 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 11 0 6 6.0 CCCN(CCC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160171 88297 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 452 11 0 6 6.0 CCCN(CCC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
60155794 84337 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 449 9 0 6 5.2 CCc1nn2c(-c3c(OC)cccc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087570 84337 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 449 9 0 6 5.2 CCc1nn2c(-c3c(OC)cccc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
71458705 88296 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 438 10 0 6 5.5 CCc1cc2c(N(CC)CC)ccc(OC)c2nc1-c1c(OC)cc(COC)cc1OC 10.1016/j.bmc.2012.09.028
CHEMBL2160170 88296 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 438 10 0 6 5.5 CCc1cc2c(N(CC)CC)ccc(OC)c2nc1-c1c(OC)cc(COC)cc1OC 10.1016/j.bmc.2012.09.028
44392550 71342 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 489 9 0 8 5.0 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1cc(-c2cccnc2)c(OC)cc1C 10.1021/jm049787k
CHEMBL181546 71342 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 489 9 0 8 5.0 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1cc(-c2cccnc2)c(OC)cc1C 10.1021/jm049787k
70690704 83389 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063375 83389 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70690704 83389 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063375 83389 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 438 10 0 6 5.2 CCN(CCOC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
21912293 104591 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cccc2C)c1C 10.1021/jm070578k
CHEMBL271974 104591 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cccc2C)c1C 10.1021/jm070578k
21912397 104812 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 8 0 4 6.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC(C)C)cc2C)c1C 10.1021/jm070578k
CHEMBL273033 104812 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 8 0 4 6.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC(C)C)cc2C)c1C 10.1021/jm070578k
58896510 146286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 430 6 1 5 5.6 CCN(c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12)C(C)C 10.1021/acs.jmedchem.5b01715
CHEMBL3793568 146286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 430 6 1 5 5.6 CCN(c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12)C(C)C 10.1021/acs.jmedchem.5b01715
CHEMBL3794598 146286 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 430 6 1 5 5.6 CCN(c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12)C(C)C 10.1021/acs.jmedchem.5b01715
46891088 13842 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 452 7 1 7 4.5 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1084997 13842 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 452 7 1 7 4.5 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46891035 14175 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 436 6 1 6 4.6 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1086510 14175 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 436 6 1 6 4.6 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46845695 13694 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 334 5 1 6 3.3 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
CHEMBL1084413 13694 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 334 5 1 6 3.3 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
44190917 203004 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 429 5 1 5 5.2 COC[C@@H](C)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561615 203004 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 429 5 1 5 5.2 COC[C@@H](C)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
9927970 104512 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL271558 104512 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
9819482 164326 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.2 CCC(COC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL408028 164326 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.2 CCC(COC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
57785862 171720 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 388 4 0 4 5.7 CCN(CC)c1cccc2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4224887 171720 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 388 4 0 4 5.7 CCN(CC)c1cccc2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
3495 7958 28 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
5311055 7958 28 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
CHEMBL9946 7958 28 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
42618206 186950 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 1 6 4.6 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)c(C)c3C)c(C)nn12 10.1021/jm9000242
CHEMBL474907 186950 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 1 6 4.6 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)c(C)c3C)c(C)nn12 10.1021/jm9000242
42618165 181314 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 385 9 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1021/jm9000242
CHEMBL455588 181314 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 385 9 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1021/jm9000242
24758072 76752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 320 4 0 2 6.1 CCC(CC)c1cc(C)n2nc(-c3ccc(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939572 76752 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 320 4 0 2 6.1 CCC(CC)c1cc(C)n2nc(-c3ccc(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
24768331 92249 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 369 7 1 6 4.3 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(OC)cc1C 10.1021/jm0611410
CHEMBL226761 92249 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 369 7 1 6 4.3 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(OC)cc1C 10.1021/jm0611410
44362115 7952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellumCompound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellum
ChEMBL None None None None 10.1021/jm0202122
6967 7952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellumCompound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellum
ChEMBL None None None None 10.1021/jm0202122
CHEMBL1201609 7952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellumCompound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellum
ChEMBL None None None None 10.1021/jm0202122
CHEMBL440057 7952 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Compound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellumCompound was evaluated for affinity towards Corticotropin releasing factor receptor 1 expressing tissues such as Cortex, cerebellum
ChEMBL None None None None 10.1021/jm0202122
71456850 88291 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 424 9 0 6 5.2 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160166 88291 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 424 9 0 6 5.2 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
21912293 104591 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cccc2C)c1C 10.1021/jm070578k
CHEMBL271974 104591 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cccc2C)c1C 10.1021/jm070578k
21912397 104812 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 8 0 4 6.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC(C)C)cc2C)c1C 10.1021/jm070578k
CHEMBL273033 104812 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 8 0 4 6.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC(C)C)cc2C)c1C 10.1021/jm070578k
70909662 163007 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 448 6 1 5 6.1 CCC(=O)N(c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12)C(C)C 10.1016/j.bmc.2016.11.011
CHEMBL4064670 163007 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 448 6 1 5 6.1 CCC(=O)N(c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12)C(C)C 10.1016/j.bmc.2016.11.011
137654892 165404 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 420 7 2 5 6.5 CCC(CC)Nc1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4092351 165404 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 420 7 2 5 6.5 CCC(CC)Nc1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
44129684 171809 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4226158 171809 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
9951076 74185 2 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
CHEMBL188844 74185 2 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
CHEMBL2165204 74185 2 None - 1 Human 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
10616876 108135 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 336 5 1 4 5.2 CCCCNc1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
CHEMBL296977 108135 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 336 5 1 4 5.2 CCCCNc1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
46891338 14151 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 346 6 1 9 1.8 COc1nc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1086374 14151 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 346 6 1 9 1.8 COc1nc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.04.121
70888282 181916 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 556 7 1 7 6.3 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3ccc(S(C)(=O)=O)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4569860 181916 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 556 7 1 7 6.3 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3ccc(S(C)(=O)=O)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
54585865 67427 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 394 6 0 5 4.8 CCCN(CCC)c1nc2c(c(-c3c(C)cc(C)cc3C)c(C)n2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760257 67427 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 394 6 0 5 4.8 CCCN(CCC)c1nc2c(c(-c3c(C)cc(C)cc3C)c(C)n2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
57390211 76769 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 395 7 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939589 76769 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 395 7 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
9800812 130414 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 5 0 4 5.3 CCc1nc2c(n1C(CC)CC)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL361912 130414 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 5 0 4 5.3 CCc1nc2c(n1C(CC)CC)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
56659877 72080 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 9 1 6 5.9 CCCN(CCC)c1c(C(C)C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828892 72080 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 9 1 6 5.9 CCCN(CCC)c1c(C(C)C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
60155990 84353 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 513 11 0 9 4.9 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4OCCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087800 84353 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 513 11 0 9 4.9 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4OCCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
10111759 71130 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 402 6 0 5 4.7 CCc1nc2c(n1C(CC)C1CC1)C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
CHEMBL181259 71130 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 402 6 0 5 4.7 CCc1nc2c(n1C(CC)C1CC1)C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
44589350 196381 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 387 3 0 7 3.7 N#Cc1ccc(N2CCc3c(-n4ccc(-n5cccn5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
CHEMBL514761 196381 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 387 3 0 7 3.7 N#Cc1ccc(N2CCc3c(-n4ccc(-n5cccn5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
70696935 83384 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 450 11 0 5 6.6 CCCN(CCC)c1ccc(CC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063370 83384 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 450 11 0 5 6.6 CCCN(CCC)c1ccc(CC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
58223504 134612 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 9 5.2 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)c(CC)sc12)C1CCOCC1 nan
CHEMBL3664547 134612 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 9 5.2 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)c(CC)sc12)C1CCOCC1 nan
71455052 88293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 9 0 6 5.1 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160168 88293 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 9 0 6 5.1 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
58896594 146282 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 444 8 1 5 6.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793367 146282 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 444 8 1 5 6.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794594 146282 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 444 8 1 5 6.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
56683763 72275 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
CHEMBL1830519 72275 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
21984648 84319 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087552 84319 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
44596700 205398 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 369 7 1 8 2.5 COC[C@H](C1CC1)n1cc(C#N)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL578838 205398 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 369 7 1 8 2.5 COC[C@H](C1CC1)n1cc(C#N)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
46891490 13240 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082625 13240 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
46891233 13470 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083592 13470 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
46845696 13161 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 348 5 1 6 3.6 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
CHEMBL1082241 13161 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 348 5 1 6 3.6 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
44190054 202792 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 335 5 1 5 3.8 COC[C@@H](C)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL560098 202792 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 335 5 1 5 3.8 COC[C@@H](C)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
42618225 186082 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL473276 186082 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
21912223 104361 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 1 4 5.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N 10.1021/jm070578k
CHEMBL270780 104361 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 1 4 5.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N 10.1021/jm070578k
21912419 104790 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 439 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(I)cc2C)c1C 10.1021/jm070578k
CHEMBL272912 104790 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 439 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(I)cc2C)c1C 10.1021/jm070578k
21912223 104361 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 1 4 5.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N 10.1021/jm070578k
CHEMBL270780 104361 1 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 328 6 1 4 5.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N 10.1021/jm070578k
21912419 104790 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 439 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(I)cc2C)c1C 10.1021/jm070578k
CHEMBL272912 104790 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 439 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(I)cc2C)c1C 10.1021/jm070578k
44444317 100836 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 363 5 0 4 5.7 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL248962 100836 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 363 5 0 4 5.7 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
44444316 168453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 358 4 0 4 5.6 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL413134 168453 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 358 4 0 4 5.6 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
42618213 190872 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 8 0 7 4.5 CCCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL482543 190872 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 8 0 7 4.5 CCCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
58801644 84335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(COC)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087568 84335 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(COC)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
58801647 84342 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.1 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087575 84342 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.1 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300259r
45268739 202734 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 365 4 1 5 4.3 C[C@H](C1CC1)n1cc(Cl)nc(Nc2cc3c(cc2Cl)COC3)c1=O 10.1021/jm900302q
CHEMBL559566 202734 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 365 4 1 5 4.3 C[C@H](C1CC1)n1cc(Cl)nc(Nc2cc3c(cc2Cl)COC3)c1=O 10.1021/jm900302q
155543377 180082 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 563 8 2 6 6.7 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(C)(C)C(N)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4526083 180082 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 563 8 2 6 6.7 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(C)(C)C(N)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
155568703 182892 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 521 7 2 6 6.0 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(N)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4591720 182892 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 521 7 2 6 6.0 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(N)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
11639510 67423 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 380 6 0 5 4.5 CCCN(CCC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760253 67423 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 380 6 0 5 4.5 CCCN(CCC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL5280146 200832 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibition of human recombinant CRF1 in HEK cell line incubated for 2 hrs by MicroBeta scintillation counter methodInhibition of human recombinant CRF1 in HEK cell line incubated for 2 hrs by MicroBeta scintillation counter method
ChEMBL 382 4 0 5 5.5 CCN(CC)c1cc(C)nn2c(-c3sc4ccc(F)cc4c3C)c(C)nc12 10.1016/j.ejmech.2021.113867
11282792 196274 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 469 4 1 7 3.6 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1OC(F)(F)F)CC2 10.1021/jm800744m
CHEMBL513937 196274 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 469 4 1 7 3.6 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1OC(F)(F)F)CC2 10.1021/jm800744m
11338604 196466 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 402 4 1 7 3.1 COc1ccc(N2CCc3c(-n4ccc(-n5cc[nH]c5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL515363 196466 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 402 4 1 7 3.1 COc1ccc(N2CCc3c(-n4ccc(-n5cc[nH]c5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
45272175 201869 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 380 6 1 6 4.0 C=Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
CHEMBL549747 201869 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 380 6 1 6 4.0 C=Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
10474043 71351 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 365 7 0 4 4.9 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL181593 71351 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 365 7 0 4 4.9 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
57393712 76759 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939579 76759 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
9865886 182645 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 403 4 0 6 3.7 COc1ccc(N2CCc3c(-n4ccc(N5CCCC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL458599 182645 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 403 4 0 6 3.7 COc1ccc(N2CCc3c(-n4ccc(N5CCCC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
11189676 182368 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 432 5 1 6 3.9 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(OC(C)C)cc1C)CC2 10.1021/jm800744m
CHEMBL457975 182368 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 432 5 1 6 3.9 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(OC(C)C)cc1C)CC2 10.1021/jm800744m
44444331 101149 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 455 4 0 3 7.4 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL250803 101149 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 455 4 0 3 7.4 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
44444312 174554 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 391 7 0 4 6.5 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL430396 174554 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 391 7 0 4 6.5 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
44589224 182806 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 398 4 0 7 4.5 CCc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL459007 182806 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 398 4 0 7 4.5 CCc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
71459110 89389 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 456 8 0 9 4.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179192 89389 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 456 8 0 9 4.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
53357535 137385 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 429 5 1 4 4.9 COc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3681390 137385 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 429 5 1 4 4.9 COc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
11166718 74039 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 444 3 1 5 4.2 Cc1cc(N2CCOCC2)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2 10.1021/jm049737f
CHEMBL188112 74039 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 444 3 1 5 4.2 Cc1cc(N2CCOCC2)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2 10.1021/jm049737f
44589205 182737 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 425 4 0 8 4.6 Cc1cc(-n2cccn2)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL458826 182737 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 425 4 0 8 4.6 Cc1cc(-n2cccn2)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
127030924 146146 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 397 6 1 6 5.0 CCN(CC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793070 146146 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 397 6 1 6 5.0 CCN(CC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
127030927 146272 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 402 7 1 6 5.1 CCN(CC)c1ccc(OC)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794479 146272 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 402 7 1 6 5.1 CCN(CC)c1ccc(OC)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
58896493 146284 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 416 6 1 5 5.2 CCN(CC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793322 146284 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 416 6 1 5 5.2 CCN(CC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794596 146284 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 416 6 1 5 5.2 CCN(CC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
56673725 72083 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 403 9 1 7 4.8 CCCN(CCC)c1c(OC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828895 72083 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 403 9 1 7 4.8 CCCN(CCC)c1c(OC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
21984718 84321 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087554 84321 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
46891386 13183 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n([C@H](C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082355 13183 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n([C@H](C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
46891191 13199 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 353 6 1 7 3.2 CCC(C1CC1)n1nc(C)nc(Nc2cc(OC)c(C#N)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082402 13199 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 353 6 1 7 3.2 CCC(C1CC1)n1nc(C)nc(Nc2cc(OC)c(C#N)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
155561680 182468 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 434 6 1 5 6.8 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccccc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4581950 182468 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 434 6 1 5 6.8 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccccc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
53357921 137390 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 427 5 1 3 5.4 CCc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3681395 137390 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 427 5 1 3 5.4 CCc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
57398972 76783 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 3 0 5 3.8 COc1cc(C)c(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(C)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939602 76783 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 3 0 5 3.8 COc1cc(C)c(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(C)c1 10.1016/j.bmc.2011.11.015
24758073 76754 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 364 7 0 3 6.5 CCOc1ccc(-c2nn3c(C)cc(C(CC)CC)c3cc2C)c(CC)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939574 76754 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 364 7 0 3 6.5 CCOc1ccc(-c2nn3c(C)cc(C(CC)CC)c3cc2C)c(CC)c1 10.1016/j.bmc.2011.11.015
42618204 186059 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 429 10 0 9 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL473077 186059 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 429 10 0 9 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
42618214 199307 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 353 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL520955 199307 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 353 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
58223500 134629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 10 0 9 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCOCC1 nan
CHEMBL3664564 134629 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 10 0 9 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCOCC1 nan
60155793 84332 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.2 CCc1nn2c(-c3cc(OC)c(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087565 84332 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.2 CCc1nn2c(-c3cc(OC)c(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
57785779 171710 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 459 4 0 5 6.7 CCC(c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl)n1ccnc1 10.1016/j.bmc.2018.01.020
CHEMBL4224722 171710 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 459 4 0 5 6.7 CCC(c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl)n1ccnc1 10.1016/j.bmc.2018.01.020
57393715 76779 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 3 0 6 2.9 Cc1nc(N(C)C)ccc1-c1nn2c(C)cc(C(C)C)c2c(=O)n1C 10.1016/j.bmc.2011.11.015
CHEMBL1939599 76779 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 3 0 6 2.9 Cc1nc(N(C)C)ccc1-c1nn2c(C)cc(C(C)C)c2c(=O)n1C 10.1016/j.bmc.2011.11.015
53358605 137372 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 422 5 1 4 5.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@@H](Cn2nc(-c3ccccc3)cc2C)CC1 nan
CHEMBL3681377 137372 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 422 5 1 4 5.2 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@@H](Cn2nc(-c3ccccc3)cc2C)CC1 nan
58223436 134617 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 9 0 9 3.8 CCCN(CC1CCOC1)c1c(OC)nn2c(-c3cnc(N(C)C)cc3OC)csc12 nan
CHEMBL3664552 134617 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 9 0 9 3.8 CCCN(CC1CCOC1)c1c(OC)nn2c(-c3cnc(N(C)C)cc3OC)csc12 nan
71451515 88284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 405 7 0 6 5.0 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C#N)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160158 88284 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 405 7 0 6 5.0 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C#N)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
53357793 137387 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 399 4 1 3 4.9 Cc1cnn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
CHEMBL3681392 137387 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 399 4 1 3 4.9 Cc1cnn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1 nan
42618209 186588 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 427 9 0 9 2.6 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474492 186588 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 427 9 0 9 2.6 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
53358858 137367 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 389 6 3 4 4.0 CCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c1C nan
CHEMBL3681372 137367 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 389 6 3 4 4.0 CCc1[nH]nc(NC[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)c1C nan
21912226 104511 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 329 6 1 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(O)cc2C)c1C 10.1021/jm070578k
CHEMBL271557 104511 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 329 6 1 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(O)cc2C)c1C 10.1021/jm070578k
71453735 89386 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 475 9 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(C(C)C)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179189 89386 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 475 9 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(C(C)C)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
70696576 82358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2046526 82358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70696576 82358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046526 82358 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 438 11 0 6 6.1 CCCN(CCC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
58896474 146222 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 400 8 1 5 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793985 146222 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 400 8 1 5 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
127031514 146230 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 425 8 1 6 5.8 CCCN(CCC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794030 146230 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 425 8 1 6 5.8 CCCN(CCC)c1ccc(C#N)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
58896536 146285 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 472 10 1 5 6.8 CCCCN(CCCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3792935 146285 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 472 10 1 5 6.8 CCCCN(CCCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794597 146285 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 472 10 1 5 6.8 CCCCN(CCCC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
56677028 72073 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 359 7 2 6 4.7 CCC(CC)Nc1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828886 72073 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 359 7 2 6 4.7 CCC(CC)Nc1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
71580312 95212 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 475 9 1 8 3.4 COc1nc(Cl)nc(C)c1Nc1nc(Br)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
CHEMBL2349563 95212 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 475 9 1 8 3.4 COc1nc(Cl)nc(C)c1Nc1nc(Br)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
44596811 205022 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 352 6 1 7 2.9 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
CHEMBL575510 205022 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assayDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenate by binding titration assay
ChEMBL 352 6 1 7 2.9 COC[C@@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1021/jm900716v
46891033 14173 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 406 4 1 5 5.0 Cc1nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1086508 14173 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 406 4 1 5 5.0 Cc1nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
58280027 146782 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 435 8 2 8 3.4 CCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
CHEMBL3800035 146782 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 435 8 2 8 3.4 CCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
10179550 71653 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 406 5 0 4 5.3 CCc1nc2c(n1C(CC)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL182169 71653 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 406 5 0 4 5.3 CCc1nc2c(n1C(CC)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
136042278 76761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 359 5 1 4 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939581 76761 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 359 5 1 4 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
42618218 190912 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL482751 190912 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCN(CC)c1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
42618211 186081 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL473275 186081 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
58896427 146281 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cccc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793329 146281 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cccc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794593 146281 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cccc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
46881864 14782 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 360 5 1 8 2.6 COc1nc(C)nc(C#N)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1090738 14782 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 360 5 1 8 2.6 COc1nc(C)nc(C#N)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
137646761 164619 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 479 7 2 6 4.4 CCN(CC(N)=O)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4083664 164619 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 479 7 2 6 4.4 CCN(CC(N)=O)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
54586828 67425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 404 6 0 5 4.5 Cc1cc(C)c(-c2cn(C)c3nc(N(CC4CC4)CC4CC4)n(C)c(=O)c23)c(C)c1 10.1016/j.bmcl.2011.02.086
CHEMBL1760255 67425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 404 6 0 5 4.5 Cc1cc(C)c(-c2cn(C)c3nc(N(CC4CC4)CC4CC4)n(C)c(=O)c23)c(C)c1 10.1016/j.bmcl.2011.02.086
21912226 104511 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 329 6 1 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(O)cc2C)c1C 10.1021/jm070578k
CHEMBL271557 104511 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 329 6 1 4 5.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(O)cc2C)c1C 10.1021/jm070578k
53357269 137378 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 423 5 1 5 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(-c3cccnc3)cc2C)CC1 nan
CHEMBL3681383 137378 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 423 5 1 5 4.6 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(-c3cccnc3)cc2C)CC1 nan
70686533 83393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063381 83393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmcl.2012.07.047
70686533 83393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063381 83393 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(F)cc12 10.1016/j.bmc.2012.09.028
71453344 88294 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 444 9 0 6 5.6 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160169 88294 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 444 9 0 6 5.6 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
11983528 181684 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 4 1 6 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL456448 181684 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 4 1 6 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
44589351 184607 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 421 3 0 7 4.0 N#Cc1ccc(N2CCc3c(-n4ccc(-n5cccn5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
CHEMBL464390 184607 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 421 3 0 7 4.0 N#Cc1ccc(N2CCc3c(-n4ccc(-n5cccn5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
71451920 89382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 461 9 0 9 4.2 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179185 89382 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 461 9 0 9 4.2 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
67380345 137376 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 425 4 1 3 5.0 O=C(N[C@H]1CC[C@H](Cn2cc3c(n2)CCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3681381 137376 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 425 4 1 3 5.0 O=C(N[C@H]1CC[C@H](Cn2cc3c(n2)CCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
21912127 104435 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1 10.1021/jm070578k
CHEMBL271117 104435 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1 10.1021/jm070578k
136042277 76760 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 5 1 4 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939580 76760 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 5 1 4 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)[nH]c(=O)c12 10.1016/j.bmc.2011.11.015
11210737 146232 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 364 7 1 4 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794051 146232 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 364 7 1 4 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
54754517 72270 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 417 10 0 7 4.8 CCCN(CCC)c1cc(N(COC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830514 72270 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 417 10 0 7 4.8 CCCN(CCC)c1cc(N(COC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
10200135 84322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 385 8 0 4 5.9 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3Cl)cccc12 10.1021/jm300259r
CHEMBL2087555 84322 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 385 8 0 4 5.9 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3Cl)cccc12 10.1021/jm300259r
22177744 71530 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 452 6 1 5 6.3 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819081 71530 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 452 6 1 5 6.3 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
46890982 13296 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
CHEMBL1082792 13296 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
46891494 13411 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COC[C@H](C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083325 13411 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COC[C@H](C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
44191109 202308 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 363 6 1 6 3.9 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1OC 10.1021/jm900302q
CHEMBL554086 202308 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 363 6 1 6 3.9 COc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1OC 10.1021/jm900302q
21912175 162498 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 358 7 0 5 5.6 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1[N+](=O)[O-] 10.1021/jm070578k
CHEMBL405347 162498 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 358 7 0 5 5.6 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1[N+](=O)[O-] 10.1021/jm070578k
58012333 166260 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 405 6 1 4 6.8 CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4101653 166260 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 405 6 1 4 6.8 CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
21912175 162498 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 358 7 0 5 5.6 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1[N+](=O)[O-] 10.1021/jm070578k
CHEMBL405347 162498 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 358 7 0 5 5.6 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1[N+](=O)[O-] 10.1021/jm070578k
42618195 191065 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL483993 191065 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3cc(C)c(OC)cc3C)c(C)nn12 10.1021/jm9000242
3495 7958 28 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.06.077
5311055 7958 28 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.06.077
CHEMBL9946 7958 28 None - 1 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.06.077
10277733 69916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 484 6 0 4 7.6 CCCC(CCC)n1cc2c3c(nc(C)nc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL178949 69916 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 484 6 0 4 7.6 CCCC(CCC)n1cc2c3c(nc(C)nc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
45268771 203412 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 354 5 1 6 3.4 COc1ccc(Nc2nccn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL564291 203412 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 354 5 1 6 3.4 COc1ccc(Nc2nccn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
21912127 104435 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1 10.1021/jm070578k
CHEMBL271117 104435 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 6 0 3 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1 10.1021/jm070578k
137642541 165075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 493 7 2 6 4.6 CCN(CC(=O)NC)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4089028 165075 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 493 7 2 6 4.6 CCN(CC(=O)NC)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
11164902 73076 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL184850 73076 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
70692630 82673 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.ejmech.2021.114085
CHEMBL2049188 82673 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.ejmech.2021.114085
70692630 82673 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049188 82673 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
71455053 88299 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 12 0 7 5.5 COCCN(CC(C)C)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160173 88299 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 482 12 0 7 5.5 COCCN(CC(C)C)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
70681900 82361 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 492 10 0 7 5.9 COCc1cc(OC)c(Oc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2046529 82361 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 492 10 0 7 5.9 COCc1cc(OC)c(Oc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.05.066
44444337 100908 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 379 6 0 5 5.0 CCC(COC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL249333 100908 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 379 6 0 5 5.0 CCC(COC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1C)CC2 10.1016/j.bmcl.2007.06.077
44589317 184462 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 426 3 1 6 4.1 Cc1cc(-n2ccc(-n3cc[nH]c3=O)n2)c2c(n1)N(c1ccc(Cl)cc1Cl)CC2 10.1021/jm800744m
CHEMBL464184 184462 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 426 3 1 6 4.1 Cc1cc(-n2ccc(-n3cc[nH]c3=O)n2)c2c(n1)N(c1ccc(Cl)cc1Cl)CC2 10.1021/jm800744m
44589237 183790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 454 4 0 8 4.9 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC(F)(F)F)c1 10.1021/jm800743q
CHEMBL462788 183790 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 454 4 0 8 4.9 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC(F)(F)F)c1 10.1021/jm800743q
56670270 72271 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 374 7 2 7 4.4 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830515 72271 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 374 7 2 7 4.4 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
21984613 84318 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087551 84318 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 389 8 0 4 5.5 CCc1nn2c(-c3ccc(OC)cc3C)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
15485774 203154 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 7 1 6 3.4 COCC(COC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL562619 203154 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 7 1 6 3.4 COCC(COC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
18392782 104744 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 325 5 0 3 6.1 C/C=C(\CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL272674 104744 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 325 5 0 3 6.1 C/C=C(\CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
44347046 121323 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.056
CHEMBL333713 121323 0 None - 1 Human 7.8 pIC50 = 7.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.056
18392782 104744 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 325 5 0 3 6.1 C/C=C(\CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL272674 104744 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 325 5 0 3 6.1 C/C=C(\CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL5269179 200373 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of human recombinant CRF1 in HEK cell line incubated for 2 hrs by MicroBeta scintillation counter methodInhibition of human recombinant CRF1 in HEK cell line incubated for 2 hrs by MicroBeta scintillation counter method
ChEMBL 381 4 0 4 6.6 CCC(CC)c1cc(C)nn2c(-c3sc4ccc(F)cc4c3C)c(C)nc12 10.1016/j.ejmech.2021.113867
16126888 76749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 336 5 0 3 5.8 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939569 76749 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 336 5 0 3 5.8 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
24758071 76753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 334 4 0 2 6.4 CCC(CC)c1cc(C)n2nc(-c3cc(C)c(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939573 76753 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 334 4 0 2 6.4 CCC(CC)c1cc(C)n2nc(-c3cc(C)c(C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
58896526 183407 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 468 5 1 5 6.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(C(C)=O)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4592625 183407 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 468 5 1 5 6.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(C(C)=O)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4597886 183407 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 468 5 1 5 6.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(C(C)=O)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
53358603 137370 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 388 6 1 4 4.4 CCc1cc(CC)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3681375 137370 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 388 6 1 4 4.4 CCc1cc(CC)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
11164902 73076 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL184850 73076 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
54580962 67429 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 366 6 0 5 4.2 CCCN(CCC)c1nc2c(c(-c3ccc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760259 67429 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 366 6 0 5 4.2 CCCN(CCC)c1nc2c(c(-c3ccc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
44392573 71064 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 475 10 0 6 5.8 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(OC)cc1Cc1cccnc1 10.1021/jm049787k
CHEMBL181007 71064 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 475 10 0 6 5.8 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(OC)cc1Cc1cccnc1 10.1021/jm049787k
44589206 182894 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 377 3 0 6 4.5 Cc1cc(F)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL459174 182894 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 377 3 0 6 4.5 Cc1cc(F)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
53358855 137373 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 413 4 1 3 5.2 Cc1cn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1C nan
CHEMBL3681378 137373 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 413 4 1 3 5.2 Cc1cn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)nc1C nan
145958142 168837 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 383 6 1 6 4.8 CCCCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
CHEMBL4160471 168837 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 383 6 1 6 4.8 CCCCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
46881695 13695 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 350 6 1 7 3.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.01.129
CHEMBL1084414 13695 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 350 6 1 7 3.0 COc1ccc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.01.129
3520 10041 54 None 1 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
9821250 10041 54 None 1 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
CHEMBL309138 10041 54 None 1 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
42618180 191136 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 5 1 7 3.7 COc1cc(C)c(-c2c(C)nn3c(NC4CCC4)nc(C)nc23)c(OC)c1 10.1021/jm9000242
CHEMBL484419 191136 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 5 1 7 3.7 COc1cc(C)c(-c2c(C)nn3c(NC4CCC4)nc(C)nc23)c(OC)c1 10.1021/jm9000242
42618232 190993 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL483349 190993 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 0 7 3.0 CCCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
70909803 146231 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 468 8 1 5 7.2 CCCN(CCC)c1c(Cl)cc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794050 146231 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 468 8 1 5 7.2 CCCN(CCC)c1c(Cl)cc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
10110271 71513 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 379 6 2 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCN2 10.1016/j.bmc.2011.07.055
CHEMBL1819063 71513 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 379 6 2 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCN2 10.1016/j.bmc.2011.07.055
53358857 137375 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 425 4 1 3 5.0 O=C(N[C@H]1CC[C@H](Cn2ncc3c2CCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3681380 137375 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 425 4 1 3 5.0 O=C(N[C@H]1CC[C@H](Cn2ncc3c2CCC3)CC1)c1cc(C(F)(F)F)ccc1Cl nan
24768346 92327 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 381 7 1 6 4.5 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
CHEMBL227834 92327 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 381 7 1 6 4.5 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
11188421 70663 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 388 7 0 4 5.4 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1 10.1021/jm049787k
CHEMBL180449 70663 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 388 7 0 4 5.4 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1 10.1021/jm049787k
44589236 185136 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 405 5 0 8 4.1 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC)c1 10.1021/jm800743q
CHEMBL465216 185136 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 405 5 0 8 4.1 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC)c1 10.1021/jm800743q
58223375 134645 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 11 0 9 4.6 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664580 134645 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 11 0 9 4.6 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
44190912 203148 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(Cl)cc2C#N)c1=O 10.1021/jm900302q
CHEMBL562550 203148 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(Cl)cc2C#N)c1=O 10.1021/jm900302q
44190824 203338 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 386 5 1 6 4.0 COC[C@@H](C)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL563819 203338 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 386 5 1 6 4.0 COC[C@@H](C)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
10108936 104789 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 1 4 4.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(N)=O)cc2C)c1C 10.1021/jm070578k
CHEMBL272910 104789 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 1 4 4.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(N)=O)cc2C)c1C 10.1021/jm070578k
137640280 163520 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 518 7 1 5 6.8 CCN(CCC(F)(F)F)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4070523 163520 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 518 7 1 5 6.8 CCN(CCC(F)(F)F)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
145968300 171760 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 376 5 1 4 5.8 CCN(CC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2018.01.020
CHEMBL4225516 171760 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 376 5 1 4 5.8 CCN(CC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2018.01.020
10224109 130811 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 422 7 0 4 6.1 CCCCC(CC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL363023 130811 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 422 7 0 4 6.1 CCCCC(CC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
11489867 19164 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 446 9 1 6 4.4 COCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL1185656 19164 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 446 9 1 6 4.4 COCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL425542 19164 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 446 9 1 6 4.4 COCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
10108936 104789 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 1 4 4.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(N)=O)cc2C)c1C 10.1021/jm070578k
CHEMBL272910 104789 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 1 4 4.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(N)=O)cc2C)c1C 10.1021/jm070578k
24758074 76755 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 350 4 0 4 5.6 CCC(CC)c1cc(C)n2nc(-c3cc4c(cc3C)OCO4)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939575 76755 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 350 4 0 4 5.6 CCC(CC)c1cc(C)n2nc(-c3cc4c(cc3C)OCO4)c(C)cc12 10.1016/j.bmc.2011.11.015
177990 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2017.07.016
3489 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2017.07.016
CHEMBL296641 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2017.07.016
177990 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2014.03.040
3489 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2014.03.040
CHEMBL296641 7214 23 None -1 2 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/j.ejmech.2014.03.040
44190560 202934 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 6 1 6 3.9 CCc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
CHEMBL561226 202934 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 6 1 6 3.9 CCc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
44190244 203499 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 337 5 1 4 4.7 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(Cl)cc2)c1=O 10.1021/jm900301y
CHEMBL564968 203499 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 337 5 1 4 4.7 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(Cl)cc2)c1=O 10.1021/jm900301y
21912198 104476 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 6 0 3 6.3 CCC(CC)Oc1c(C)c(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL271332 104476 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 6 0 3 6.3 CCC(CC)Oc1c(C)c(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
53357142 137377 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 440 5 1 4 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@@H](Cn2nc(-c3ccc(F)cc3)cc2C)CC1 nan
CHEMBL3681382 137377 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 440 5 1 4 5.3 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@@H](Cn2nc(-c3ccc(F)cc3)cc2C)CC1 nan
11773483 72347 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL183148 72347 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
11773483 72347 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL183148 72347 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1021/jm040058e
155567202 182744 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 492 8 1 6 7.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(OC(C)C)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4588387 182744 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 492 8 1 6 7.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(OC(C)C)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
21912198 104476 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 6 0 3 6.3 CCC(CC)Oc1c(C)c(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL271332 104476 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 6 0 3 6.3 CCC(CC)Oc1c(C)c(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
70682294 83392 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063380 83392 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmcl.2012.07.047
70682294 83392 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
CHEMBL2063380 83392 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 394 8 0 5 5.2 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
58223471 134647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 12 0 9 4.3 COCCN(CC(C)C)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664582 134647 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 12 0 9 4.3 COCCN(CC(C)C)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
71580311 95211 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 431 9 1 8 3.3 COc1nc(Cl)nc(C)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
CHEMBL2349562 95211 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 431 9 1 8 3.3 COc1nc(Cl)nc(C)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
46890978 13505 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 312 4 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.04.121
CHEMBL1083724 13505 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 312 4 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.04.121
44190448 201912 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 439 4 0 6 4.2 COc1cc(Br)c2c(c1)OCCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
CHEMBL550140 201912 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 439 4 0 6 4.2 COc1cc(Br)c2c(c1)OCCN2c1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
44191111 203258 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 362 4 1 5 4.4 Cc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C#N 10.1021/jm900302q
CHEMBL563313 203258 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 362 4 1 5 4.4 Cc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C#N 10.1021/jm900302q
57397277 76766 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 381 6 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939586 76766 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 381 6 0 5 5.3 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C(C)C)c(=O)c12 10.1016/j.bmc.2011.11.015
42618175 191563 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 10 1 8 3.6 CCOCC(COCC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL485140 191563 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 10 1 8 3.6 CCOCC(COCC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
9885105 104775 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 6.1 CCOc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL272826 104775 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 6.1 CCOc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
11291949 134287 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
CHEMBL366155 134287 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
10216313 71129 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 410 7 0 6 4.5 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1021/jm049787k
CHEMBL181258 71129 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 410 7 0 6 4.5 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1021/jm049787k
60156090 84351 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 536 11 0 9 5.4 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4(C#N)CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087798 84351 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 536 11 0 9 5.4 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4(C#N)CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
11441103 182647 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 405 4 0 7 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCOC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL458600 182647 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 405 4 0 7 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCOC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
70682070 82674 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 390 8 2 4 7.0 CCCC(CCC)Nc1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049189 82674 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 390 8 2 4 7.0 CCCC(CCC)Nc1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.bmcl.2012.05.066
11260682 18527 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 392 5 2 4 5.4 CCC(CC)Nc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1021/jm049737f
CHEMBL1181621 18527 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 392 5 2 4 5.4 CCC(CC)Nc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1021/jm049737f
CHEMBL185736 18527 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 392 5 2 4 5.4 CCC(CC)Nc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1021/jm049737f
CHEMBL526149 222454 10 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm9000242
57390212 76782 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 5 0 5 4.5 CCC(CC)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939601 76782 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 5 0 5 4.5 CCC(CC)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL526149 222454 10 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cellsDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
ChEMBL None None None CSCC[C@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CC(=O)O)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm900025h
9949999 104359 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC)cc2C)c1C 10.1021/jm070578k
CHEMBL270764 104359 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC)cc2C)c1C 10.1021/jm070578k
9949999 104359 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC)cc2C)c1C 10.1021/jm070578k
CHEMBL270764 104359 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(OC)cc2C)c1C 10.1021/jm070578k
46891090 13593 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 418 7 1 6 5.0 CCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083947 13593 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 418 7 1 6 5.0 CCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46881794 14109 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 384 6 1 6 4.2 Cc1cc(OC(F)F)nc(C)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1086181 14109 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 384 6 1 6 4.2 Cc1cc(OC(F)F)nc(C)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
44190146 204614 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 381 8 1 7 3.1 COCC(COC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL572347 204614 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 381 8 1 7 3.1 COCC(COC)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
42618179 191313 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 383 7 1 7 4.3 CCCC(C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL484781 191313 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 383 7 1 7 4.3 CCCC(C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
42618171 186776 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 378 7 0 7 3.9 CCCN(CCC#N)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL474700 186776 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 378 7 0 7 3.9 CCCN(CCC#N)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
24768332 92358 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 385 8 1 7 4.0 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(OC)nc1OC 10.1021/jm0611410
CHEMBL228168 92358 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 385 8 1 7 4.0 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(OC)nc1OC 10.1021/jm0611410
11176967 74016 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL187987 74016 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 397 6 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1Cl 10.1021/jm049737f
46891437 13184 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COC[C@@H](C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082358 13184 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COC[C@@H](C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
42618169 187616 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 7 0 6 4.4 CCCCN(CC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475705 187616 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 7 0 6 4.4 CCCCN(CC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
44190916 203525 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 443 6 1 5 5.6 CC[C@H](COC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL565182 203525 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 443 6 1 5 5.6 CC[C@H](COC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
11588927 72281 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 377 7 1 6 5.4 CCc1cc(OC)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
CHEMBL1830524 72281 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 377 7 1 6 5.4 CCc1cc(OC)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
71456930 88765 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 409 9 1 6 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165196 88765 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 409 9 1 6 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
46891438 13185 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn([C@@H](COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082359 13185 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn([C@@H](COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
44190336 201710 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL541756 201710 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 345 5 1 4 4.9 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(C)cc2C)c1=O 10.1021/jm900301y
44189949 202740 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 7 1 4 5.7 CCCC(CCC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL559633 202740 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 361 7 1 4 5.7 CCCC(CCC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
44190239 203416 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
CHEMBL564303 203416 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
42618235 190971 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 382 8 0 7 4.1 CCCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL483162 190971 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 382 8 0 7 4.1 CCCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
44190239 203416 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL564303 203416 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 382 4 1 5 4.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900302q
42618191 191138 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 394 7 0 8 3.5 CCN(CCC#N)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL484421 191138 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 394 7 0 8 3.5 CCN(CCC#N)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
42618168 187435 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475506 187435 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
57393711 76750 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 5 0 5 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939570 76750 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 5 0 5 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
9952426 104479 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070578k
CHEMBL271344 104479 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070578k
11249766 18531 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 430 8 1 5 5.1 CCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL1181636 18531 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 430 8 1 5 5.1 CCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
CHEMBL186517 18531 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 430 8 1 5 5.1 CCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049737f
9952426 104479 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070578k
CHEMBL271344 104479 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070578k
46891287 13653 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 6 1 7 3.8 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1084203 13653 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 6 1 7 3.8 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
46881747 12368 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 362 6 1 6 4.0 CCOc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
CHEMBL1077249 12368 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 362 6 1 6 4.0 CCOc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.01.129
42618193 190937 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL482976 190937 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3C)c(C)nn12 10.1021/jm9000242
44190149 201839 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
CHEMBL549538 201839 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 396 5 1 5 5.2 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
136164073 14928 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 411 7 2 7 3.5 COCC(COC)NC1NC(C)=Nc2c(-c3ccc(Cl)cc3Cl)c(C)nn21 10.1016/j.bmcl.2010.01.129
CHEMBL1091818 14928 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 411 7 2 7 3.5 COCC(COC)NC1NC(C)=Nc2c(-c3ccc(Cl)cc3Cl)c(C)nn21 10.1016/j.bmcl.2010.01.129
15485770 204373 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 333 5 1 4 4.9 CCC(CC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL570546 204373 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 333 5 1 4 4.9 CCC(CC)n1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
42618178 198468 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 1 7 3.9 CC[C@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL519677 198468 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 1 7 3.9 CC[C@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
44190827 202936 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 362 4 1 5 4.4 Cc1cc(C#N)cc(Cl)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
CHEMBL561230 202936 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 362 4 1 5 4.4 Cc1cc(C#N)cc(Cl)c1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
58223380 134646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 11 0 9 5.0 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCCC1 nan
CHEMBL3664581 134646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 11 0 9 5.0 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCCC1 nan
56663336 72084 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828896 72084 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56683765 72279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1nc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830522 72279 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1nc(N(C)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
21984697 84325 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 409 9 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CCCF)CC1CC1 10.1021/jm300259r
CHEMBL2087558 84325 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 409 9 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CCCF)CC1CC1 10.1021/jm300259r
46891336 13179 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 359 7 1 8 2.3 COCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082340 13179 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 359 7 1 8 2.3 COCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
46891092 14004 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 416 5 1 7 3.4 Cc1nc(Nc2c(Cl)cc(S(C)(=O)=O)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1085734 14004 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 416 5 1 7 3.4 Cc1nc(Nc2c(Cl)cc(S(C)(=O)=O)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
9885105 104775 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 6.1 CCOc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL272826 104775 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 6.1 CCOc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
57786312 171745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 423 4 0 4 6.6 CCC(OC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4225316 171745 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 423 4 0 4 6.6 CCC(OC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
21084107 84333 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 1 7 4.7 CCc1nn2c(-c3c(OC)cc(CO)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087566 84333 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 1 7 4.7 CCc1nn2c(-c3c(OC)cc(CO)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
11177197 174420 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 404 7 1 4 6.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2018.01.020
CHEMBL4226111 174420 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 404 7 1 4 6.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2018.01.020
CHEMBL4301639 174420 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 404 7 1 4 6.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2018.01.020
71458704 88292 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 410 9 0 6 4.9 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
CHEMBL2160167 88292 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 410 9 0 6 4.9 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)ccc12 10.1016/j.bmc.2012.09.028
44589304 182799 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 388 3 0 7 4.1 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(F)c1 10.1021/jm800743q
CHEMBL458981 182799 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 388 3 0 7 4.1 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(F)c1 10.1021/jm800743q
53328045 137384 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 441 6 1 3 5.7 CCc1cc(CC)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
CHEMBL3681389 137384 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 441 6 1 3 5.7 CCc1cc(CC)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)n1 nan
71449777 88768 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 453 10 1 7 4.1 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OCCF)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165199 88768 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 453 10 1 7 4.1 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OCCF)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
24768338 92315 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 415 9 1 8 3.5 CCCN(CCOC)c1nc(C)nc2c1NCCN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
CHEMBL227724 92315 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 415 9 1 8 3.5 CCCN(CCOC)c1nc(C)nc2c1NCCN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
57786300 171727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 407 3 0 4 6.1 CCC(=O)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4224989 171727 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 407 3 0 4 6.1 CCC(=O)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
57785808 171728 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 489 5 0 6 6.0 CCc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4225039 171728 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 489 5 0 6 6.0 CCc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
70690703 83385 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 380 6 0 5 4.7 COCc1cc(OC)c(-c2nc3c(C)ccc(N(C)C)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
CHEMBL2063371 83385 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 380 6 0 5 4.7 COCc1cc(OC)c(-c2nc3c(C)ccc(N(C)C)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
56683689 72089 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 427 10 0 6 5.6 CCCN(CCC)c1cc(N(CC2CC2)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828901 72089 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 427 10 0 6 5.6 CCCN(CCC)c1cc(N(CC2CC2)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
44589306 181767 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 406 5 0 9 3.5 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC)n1 10.1021/jm800743q
CHEMBL456651 181767 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 406 5 0 9 3.5 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(OC)n1 10.1021/jm800743q
53358856 137374 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 413 4 1 3 5.2 Cc1cnn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
CHEMBL3681379 137374 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 413 4 1 3 5.2 Cc1cnn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c1C nan
58896446 146283 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 412 8 1 4 7.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3C(C)C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3792636 146283 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 412 8 1 4 7.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3C(C)C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794595 146283 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 412 8 1 4 7.0 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(Cl)cc3C(C)C)n(C)c12 10.1021/acs.jmedchem.5b01715
60155708 84328 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 447 8 0 5 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087561 84328 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 447 8 0 5 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
60155709 84329 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(OC)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087562 84329 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(OC)cc(C)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
10135150 71525 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)c(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819075 71525 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)c(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
22177742 71536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 5.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
CHEMBL1819087 71536 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 5.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
24964084 163323 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 419 6 1 4 6.0 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(C(N)=O)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4068170 163323 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 419 6 1 4 6.0 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(C(N)=O)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
11948286 163448 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4069551 163448 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
53357920 137389 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 427 5 1 3 5.4 CCc1cc(C)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3681394 137389 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 427 5 1 3 5.4 CCc1cc(C)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
10294192 71980 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 396 7 0 4 5.7 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1c(C)cc(C)cc1C 10.1021/jm049787k
CHEMBL182550 71980 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 396 7 0 4 5.7 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1c(C)cc(C)cc1C 10.1021/jm049787k
58896429 180104 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 510 7 1 6 7.1 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(CC3CCOC3)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4526475 180104 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 510 7 1 6 7.1 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(CC3CCOC3)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
58896417 146279 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 426 8 1 4 7.3 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(-c3ccccc3)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793751 146279 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 426 8 1 4 7.3 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(-c3ccccc3)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794591 146279 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 426 8 1 4 7.3 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(-c3ccccc3)c12 10.1021/acs.jmedchem.5b01715
58223481 89374 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 517 11 1 10 4.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(O)CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179177 89374 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 517 11 1 10 4.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(O)CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
44589331 182259 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 378 3 0 6 4.2 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4ccccn4)n3)ccnc21 10.1021/jm800743q
CHEMBL457741 182259 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 378 3 0 6 4.2 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-c4ccccn4)n3)ccnc21 10.1021/jm800743q
71453343 88286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160160 88286 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 412 8 0 5 5.4 CCN(CC)c1ccc(F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
44589239 197269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 404 3 0 7 4.6 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
CHEMBL517910 197269 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 404 3 0 7 4.6 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
46891491 13718 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1084500 13718 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
46891390 13894 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COC[C@@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1085244 13894 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COC[C@@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
42618217 191402 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 400 9 0 9 2.2 COCCN(CCOC)c1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL484930 191402 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 400 9 0 9 2.2 COCCN(CCOC)c1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
44589256 196421 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 457 4 0 8 4.1 CS(=O)(=O)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
CHEMBL515070 196421 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 457 4 0 8 4.1 CS(=O)(=O)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
58223424 134649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 431 9 0 8 4.6 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
CHEMBL3664584 134649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 431 9 0 8 4.6 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
127030314 146167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793277 146167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
21984771 84320 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
CHEMBL2087553 84320 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 403 8 0 4 5.8 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CC1 10.1021/jm300259r
127030314 146167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL3793277 146167 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
42618176 191133 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 337 4 1 6 3.7 COc1ccc(-c2c(C)nn3c(NC4CCC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
CHEMBL484407 191133 1 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 337 4 1 6 3.7 COc1ccc(-c2c(C)nn3c(NC4CCC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
42618216 198898 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 1 7 3.8 CCC(CC)Nc1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL520344 198898 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 1 7 3.8 CCC(CC)Nc1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
22177988 71516 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 364 6 1 5 4.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)cnn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819066 71516 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 364 6 1 5 4.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)cnn13)CCC2 10.1016/j.bmc.2011.07.055
46881863 12374 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 6 1 8 2.7 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.01.129
CHEMBL1077299 12374 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 365 6 1 8 2.7 COc1nc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2010.01.129
90654669 116851 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 398 9 1 5 6.2 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SCC 10.1016/j.ejmech.2014.03.040
CHEMBL3235706 116851 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 398 9 1 5 6.2 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SCC 10.1016/j.ejmech.2014.03.040
70688637 83391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 490 9 0 6 6.1 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
CHEMBL2063377 83391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 490 9 0 6 6.1 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
58223432 134634 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 477 14 0 9 4.9 CCCCN(CCOC)c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12 nan
CHEMBL3664569 134634 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 477 14 0 9 4.9 CCCCN(CCOC)c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12 nan
58223378 134641 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.5 COCCN(CC1CCC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664576 134641 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.5 COCCN(CC1CCC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
60155887 84348 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 465 9 0 7 5.0 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(OC)nn12 10.1021/jm300259r
CHEMBL2087795 84348 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 465 9 0 7 5.0 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(OC)nn12 10.1021/jm300259r
21912058 104475 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N(C)C 10.1021/jm070578k
CHEMBL271329 104475 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N(C)C 10.1021/jm070578k
155552287 180851 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 465 7 1 7 6.2 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cn1 10.1016/j.bmc.2016.08.005
CHEMBL4544244 180851 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 465 7 1 7 6.2 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cn1 10.1016/j.bmc.2016.08.005
58896465 182875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 468 6 1 5 7.5 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(Cl)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4591335 182875 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 468 6 1 5 7.5 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(Cl)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
10204603 70119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 456 4 0 4 6.8 CCC(CC)n1cc2c3c(nc(C)nc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL179435 70119 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 456 4 0 4 6.8 CCC(CC)n1cc2c3c(nc(C)nc31)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1016/j.bmcl.2007.06.077
21912058 104475 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N(C)C 10.1021/jm070578k
CHEMBL271329 104475 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 356 7 0 4 5.7 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1N(C)C 10.1021/jm070578k
42618207 186585 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 381 6 1 7 4.1 CCC(CC)Nc1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474491 186585 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 381 6 1 7 4.1 CCC(CC)Nc1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
58896492 146278 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 2 3 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)[nH]c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793362 146278 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 2 3 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)[nH]c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794590 146278 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 2 3 5.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)[nH]c12 10.1021/acs.jmedchem.5b01715
71457263 89391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 445 9 0 8 4.6 CCCN(c1c(OC)nn2c(-c3ccc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179194 89391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 445 9 0 8 4.6 CCCN(c1c(OC)nn2c(-c3ccc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
58317279 133315 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 394 4 1 4 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(Cl)c2C)CC1 nan
CHEMBL3652115 133315 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 394 4 1 4 4.5 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(C)c(Cl)c2C)CC1 nan
44589329 182421 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 403 4 0 8 3.9 Cc1nc(N(C)C)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL458101 182421 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 403 4 0 8 3.9 Cc1nc(N(C)C)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
44589223 196304 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 443 4 0 7 5.3 Cc1cc(OC(F)(F)F)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL514126 196304 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 443 4 0 7 5.3 Cc1cc(OC(F)(F)F)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
58223390 134622 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 433 11 0 8 4.9 CCCN(CCC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664557 134622 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 433 11 0 8 4.9 CCCN(CCC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223381 134639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 11 0 9 4.6 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOC1 nan
CHEMBL3664574 134639 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 11 0 9 4.6 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOC1 nan
58223490 134656 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 9 0 8 5.0 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664590 134656 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 9 0 8 5.0 CCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
46891288 13654 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 329 5 1 7 2.7 COc1nc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
CHEMBL1084204 13654 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 329 5 1 7 2.7 COc1nc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
11304337 71621 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 406 4 0 4 5.3 CCc1nc2c(n1C(C)C1CCC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL182068 71621 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 406 4 0 4 5.3 CCc1nc2c(n1C(C)C1CCC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
46891229 13320 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 407 4 1 6 4.4 Cc1nc(Nc2c(Cl)cc(C(F)(F)F)nc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082956 13320 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 407 4 1 6 4.4 Cc1nc(Nc2c(Cl)cc(C(F)(F)F)nc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
53357410 133316 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3652116 133316 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
60155989 84352 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 513 11 0 9 4.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4COCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087799 84352 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 513 11 0 9 4.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CC4)CC4COCCO4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
46891552 14114 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn([C@H](COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1086239 14114 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn([C@H](COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
58896411 182984 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 464 7 1 6 6.8 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cc1 10.1016/j.bmc.2016.08.005
CHEMBL4593848 182984 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 464 7 1 6 6.8 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cc1 10.1016/j.bmc.2016.08.005
10136833 129121 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 418 8 0 5 5.4 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
CHEMBL359923 129121 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 418 8 0 5 5.4 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
44589092 182794 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 481 3 0 6 6.1 FC(F)(F)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
CHEMBL458968 182794 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 481 3 0 6 6.1 FC(F)(F)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
46891187 13415 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 363 4 1 6 3.8 Cc1nc(Nc2cc(Cl)c(C#N)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083342 13415 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 363 4 1 6 3.8 Cc1nc(Nc2cc(Cl)c(C#N)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
137635894 162690 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 507 7 1 6 5.0 CCN(CC(=O)N(C)C)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4060825 162690 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 507 7 1 6 5.0 CCN(CC(=O)N(C)C)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
57786068 171826 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 389 4 0 4 5.3 CCN(CC)c1cccc2nc3n(c12)CCOC3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4226353 171826 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 389 4 0 4 5.3 CCN(CC)c1cccc2nc3n(c12)CCOC3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
90654666 116848 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 404 10 1 7 4.3 COCCN(CCOC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SC 10.1016/j.ejmech.2014.03.040
CHEMBL3235700 116848 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 404 10 1 7 4.3 COCCN(CCOC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SC 10.1016/j.ejmech.2014.03.040
25149257 196322 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 397 3 0 8 4.2 Cc1cc(-n2ccc(-c3nccs3)n2)c2cnn(-c3ccc(C#N)cc3C)c2n1 10.1021/jm800743q
CHEMBL514272 196322 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 397 3 0 8 4.2 Cc1cc(-n2ccc(-c3nccs3)n2)c2cnn(-c3ccc(C#N)cc3C)c2n1 10.1021/jm800743q
70692845 83382 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 422 10 0 5 6.0 CCCN(CCC)c1cccc2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063368 83382 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 422 10 0 5 6.0 CCCN(CCC)c1cccc2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
46891156 14009 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 342 6 1 6 3.7 CCOc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
CHEMBL1085754 14009 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 342 6 1 6 3.7 CCOc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
21912152 102737 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 5 0 3 5.6 CCC(C)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL259467 102737 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 5 0 3 5.6 CCC(C)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
3520 10041 54 None 1 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm800744m
9821250 10041 54 None 1 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm800744m
CHEMBL309138 10041 54 None 1 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm800744m
21912152 102737 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 5 0 3 5.6 CCC(C)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL259467 102737 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 313 5 0 3 5.6 CCC(C)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
44190339 202899 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 6 2 6 3.6 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(O)cc2C)c1=O 10.1021/jm900301y
CHEMBL561024 202899 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 6 2 6 3.6 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(O)cc2C)c1=O 10.1021/jm900301y
70692847 83390 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 504 10 0 6 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
CHEMBL2063376 83390 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 504 10 0 6 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
71458702 88289 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 462 8 0 5 6.2 CCN(CC)c1ccc(C(F)(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160163 88289 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 462 8 0 5 6.2 CCN(CC)c1ccc(C(F)(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
11774042 210131 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm040058e
CHEMBL65078 210131 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm040058e
58223393 134610 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 465 10 1 8 4.6 CCCN(CCC)c1c(C)nn2c(-c3c(O)cc(COC)cc3OC)c([S+](C)[O-])sc12 nan
CHEMBL3664545 134610 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 465 10 1 8 4.6 CCCN(CCC)c1c(C)nn2c(-c3c(O)cc(COC)cc3OC)c([S+](C)[O-])sc12 nan
10309819 71990 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 408 5 0 6 4.1 CCc1nc2c(c(=O)n(C)c(=O)n2-c2ccc(Cl)cc2Cl)n1C(CC)CC 10.1021/jm049787k
CHEMBL182591 71990 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 408 5 0 6 4.1 CCc1nc2c(c(=O)n(C)c(=O)n2-c2ccc(Cl)cc2Cl)n1C(CC)CC 10.1021/jm049787k
56668632 71532 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 434 7 1 5 6.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819083 71532 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 434 7 1 5 6.0 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC(F)F)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
46891286 13395 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn(C(COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083293 13395 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 413 8 1 8 3.1 CCOc1ccc(Nc2nc(C)nn(C(COC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
42618219 190913 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC(CC)Nc1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL482752 190913 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC(CC)Nc1nc(C)nc2c(-c3cnc(OC)cc3C)c(C)nn12 10.1021/jm900025h
42618229 196576 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 396 8 0 8 3.0 COCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL516242 196576 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 396 8 0 8 3.0 COCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
42618220 198663 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL519967 198663 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
44190730 202752 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2c(C)cc(Cl)cc2C)n1 10.1021/jm900302q
CHEMBL559701 202752 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2c(C)cc(Cl)cc2C)n1 10.1021/jm900302q
21912269 175689 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(COC)cc2C)c1C 10.1021/jm070578k
CHEMBL438553 175689 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(COC)cc2C)c1C 10.1021/jm070578k
11153312 72280 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 383 6 1 6 5.5 CCC(CC)n1ccc2c(Nc3ccc(OC)cc3Cl)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830523 72280 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 383 6 1 6 5.5 CCC(CC)n1ccc2c(Nc3ccc(OC)cc3Cl)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
71580316 95216 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 441 8 0 6 4.2 COc1cc(Cl)c2c(c1)CCN2c1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
CHEMBL2349567 95216 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 441 8 0 6 4.2 COc1cc(Cl)c2c(c1)CCN2c1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
21912269 175689 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(COC)cc2C)c1C 10.1021/jm070578k
CHEMBL438553 175689 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 357 8 0 4 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(COC)cc2C)c1C 10.1021/jm070578k
42618192 199372 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 5 0 7 4.5 CCC1CCCCN1c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL521457 199372 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 5 0 7 4.5 CCC1CCCCN1c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
57398971 76770 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 393 7 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939590 76770 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 393 7 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
24768339 92341 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 377 6 1 5 4.3 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1C 10.1021/jm0611410
CHEMBL227946 92341 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 377 6 1 5 4.3 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1C 10.1021/jm0611410
11421422 18537 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 431 6 1 5 5.3 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1c(Cl)cc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL1181649 18537 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 431 6 1 5 5.3 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1c(Cl)cc(C#N)cc1Cl 10.1021/jm049737f
CHEMBL187410 18537 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 431 6 1 5 5.3 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1c(Cl)cc(C#N)cc1Cl 10.1021/jm049737f
9820671 195597 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL506214 195597 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
24768340 149703 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 363 6 1 5 4.8 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(C#N)cc1C 10.1021/jm0611410
CHEMBL389387 149703 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 363 6 1 5 4.8 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(C#N)cc1C 10.1021/jm0611410
46891387 13256 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082669 13256 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
42618223 186054 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCCC(C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL473069 186054 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCCC(C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
46891285 13394 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 7 1 7 3.9 CCOc1ccc(Nc2nc(C)nn(C(CC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083292 13394 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 7 1 7 3.9 CCOc1ccc(Nc2nc(C)nn(C(CC)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
46891231 13468 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCC(C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083590 13468 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCC(C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
46891232 13469 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COCC(C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083591 13469 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 399 7 1 8 2.7 COCC(C1CC1)n1nc(C)nc(Nc2ccc(OC)nc2C(F)(F)F)c1=O 10.1016/j.bmcl.2010.04.121
9858549 104446 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 5.9 CCC(CC)Oc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
CHEMBL271197 104446 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 5.9 CCC(CC)Oc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
44191009 202997 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 7 1 4 7.1 CCCC(CCC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561553 202997 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 455 7 1 4 7.1 CCCC(CCC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
9858549 104446 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 5.9 CCC(CC)Oc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
CHEMBL271197 104446 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 5.9 CCC(CC)Oc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
42618182 198680 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 397 8 0 7 4.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL519999 198680 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 397 8 0 7 4.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
57397276 76751 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 373 5 0 5 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939571 76751 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 373 5 0 5 4.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
57393713 76773 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939593 76773 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
44190556 202757 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 368 5 1 6 3.7 COc1ccc(Nc2nc(C)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL559765 202757 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 368 5 1 6 3.7 COc1ccc(Nc2nc(C)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
42618166 179721 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 339 6 1 6 4.0 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1021/jm9000242
CHEMBL451693 179721 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 339 6 1 6 4.0 CCC(CC)Nc1nc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1021/jm9000242
24180501 101252 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 386 6 0 4 6.4 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL251386 101252 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 386 6 0 4 6.4 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
24768328 104482 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 391 7 3 5 4.0 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)NC 10.1021/jm070579c
CHEMBL271370 104482 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 391 7 3 5 4.0 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)NC 10.1021/jm070579c
3663 106743 83 None - 28 Human 6.5 pIC50 = 6.5 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 10.1021/np1000329
CHEMBL286494 106743 83 None - 28 Human 6.5 pIC50 = 6.5 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 504 0 6 8 5.1 Cc1cc(O)c2c(=O)c3c(O)cc(O)c4c5c(O)cc(O)c6c(=O)c7c(O)cc(C)c8c1c2c(c34)c(c78)c65 10.1021/np1000329
54585866 67431 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 398 8 0 7 3.6 CCCN(CCC)c1nc2c(c(-c3ccc(OC)cc3OC)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760261 67431 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 398 8 0 7 3.6 CCCN(CCC)c1nc2c(c(-c3ccc(OC)cc3OC)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
54579975 67432 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 474 6 0 5 5.6 CCCN(CCC)c1nc2c(c(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760262 67432 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 474 6 0 5 5.6 CCCN(CCC)c1nc2c(c(-c3ccc(C(F)(F)F)cc3C(F)(F)F)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
11250707 19039 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 522 8 1 6 4.6 CCN(CCCS(C)(=O)=O)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
CHEMBL1184720 19039 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 522 8 1 6 4.6 CCN(CCCS(C)(=O)=O)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
CHEMBL365488 19039 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 522 8 1 6 4.6 CCN(CCCS(C)(=O)=O)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
56666769 72082 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 441 9 1 6 6.4 CCCN(CCC)c1c(C2CCCC2)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828894 72082 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 441 9 1 6 6.4 CCCN(CCC)c1c(C2CCCC2)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
11247672 181685 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 4 1 7 2.2 COc1ccc(N2CCc3c(-n4ccc(N5CCNS5(=O)=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL456449 181685 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 4 1 7 2.2 COc1ccc(N2CCc3c(-n4ccc(N5CCNS5(=O)=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
58223435 134648 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 11 0 9 4.2 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
CHEMBL3664583 134648 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 11 0 9 4.2 COCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
22177839 71511 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 380 6 1 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
CHEMBL1819061 71511 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 380 6 1 6 4.6 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
46881865 14783 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 395 8 1 9 2.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(C)nc(OC)nc2OC)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1090739 14783 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 395 8 1 9 2.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(C)nc(OC)nc2OC)c1=O 10.1016/j.bmcl.2010.01.129
24768328 104482 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 391 7 3 5 4.0 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)NC 10.1021/jm070579c
CHEMBL271370 104482 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 391 7 3 5 4.0 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)NC 10.1021/jm070579c
56680359 72085 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828897 72085 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
10180350 70181 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 418 6 0 4 6.5 CCCC(CCC)N1CCC2CN(c3ccc(Cl)cc3Cl)c3nc(C)nc1c32 10.1016/j.bmcl.2007.06.077
CHEMBL179608 70181 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 418 6 0 4 6.5 CCCC(CCC)N1CCC2CN(c3ccc(Cl)cc3Cl)c3nc(C)nc1c32 10.1016/j.bmcl.2007.06.077
21912361 104815 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 331 6 0 3 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(F)cc2C)c1C 10.1021/jm070578k
CHEMBL273068 104815 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 331 6 0 3 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(F)cc2C)c1C 10.1021/jm070578k
54580963 67430 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 428 9 0 8 3.6 CCCN(CCC)c1nc2c(c(-c3c(OC)cc(OC)cc3OC)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760260 67430 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 428 9 0 8 3.6 CCCN(CCC)c1nc2c(c(-c3c(OC)cc(OC)cc3OC)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
57395432 76758 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)c2nc(-c3ccc(OC)cc3C)c(C)cn12 10.1016/j.bmc.2011.11.015
CHEMBL1939578 76758 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 337 5 0 4 5.2 CCC(CC)c1nc(C)c2nc(-c3ccc(OC)cc3C)c(C)cn12 10.1016/j.bmc.2011.11.015
24768337 172794 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 429 9 1 8 3.1 CCCN(CCOC)c1nc(C)nc2c1NC(=O)CN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
CHEMBL425476 172794 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 429 9 1 8 3.1 CCCN(CCOC)c1nc(C)nc2c1NC(=O)CN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
11235455 182245 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 5 1 6 3.5 CCOc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL457710 182245 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 5 1 6 3.5 CCOc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
44589349 182896 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 367 3 0 7 3.3 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-n4cccn4)n3)ccnc21 10.1021/jm800743q
CHEMBL459181 182896 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 367 3 0 7 3.3 Cc1cc(C#N)ccc1N1CCc2c(-n3ccc(-n4cccn4)n3)ccnc21 10.1021/jm800743q
53358606 137371 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 386 4 1 4 4.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2cc3c(n2)CCCC3)CC1 nan
CHEMBL3681376 137371 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 386 4 1 4 4.1 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2cc3c(n2)CCCC3)CC1 nan
58223385 134633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 CCOCc1cc(OC)c(-c2csc3c(N(CCOC)CC4CC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664568 134633 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 CCOCc1cc(OC)c(-c2csc3c(N(CCOC)CC4CC4)c(OC)nn23)c(OC)c1 nan
58223464 134640 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 5.0 CCOCc1cc(OC)c(-c2csc3c(N(CC4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664575 134640 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 5.0 CCOCc1cc(OC)c(-c2csc3c(N(CC4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
56663335 72079 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 10 1 6 5.7 CCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
CHEMBL1828891 72079 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 10 1 6 5.7 CCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
21912361 104815 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 331 6 0 3 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(F)cc2C)c1C 10.1021/jm070578k
CHEMBL273068 104815 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 331 6 0 3 5.8 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(F)cc2C)c1C 10.1021/jm070578k
11948286 163448 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4069551 163448 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
11201828 182731 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 453 3 1 6 3.7 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1C(F)(F)F)CC2 10.1021/jm800744m
CHEMBL458810 182731 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 453 3 1 6 3.7 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1C(F)(F)F)CC2 10.1021/jm800744m
42618212 190871 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL482542 190871 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 395 7 0 7 4.1 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
57786096 171874 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 475 4 0 6 5.8 Cc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4227177 171874 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 475 4 0 6 5.8 Cc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
70686154 82362 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 466 9 0 7 5.5 CCN(c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12)C1CCOCC1 10.1016/j.bmcl.2012.05.066
CHEMBL2046530 82362 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 466 9 0 7 5.5 CCN(c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12)C1CCOCC1 10.1016/j.bmcl.2012.05.066
11476167 196483 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 439 4 0 7 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCCS5(=O)=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL515503 196483 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 439 4 0 7 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCCS5(=O)=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
10184943 73476 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 490 5 0 4 6.6 CCc1nc2c(n1Cc1ccc(-c3ccccc3)cc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL185541 73476 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 490 5 0 4 6.6 CCc1nc2c(n1Cc1ccc(-c3ccccc3)cc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223455 131202 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 9 0 8 4.7 COc1cc(C)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
CHEMBL3639634 131202 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 9 0 8 4.7 COc1cc(C)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
58223403 134650 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 483 10 0 8 5.2 COc1cc(C2CC2)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
CHEMBL3664585 134650 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 483 10 0 8 5.2 COc1cc(C2CC2)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
58223493 134669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 10 0 9 5.2 CCCN(c1ccccn1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664603 134669 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 10 0 9 5.2 CCCN(c1ccccn1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
56683762 72274 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830518 72274 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 0 7 4.2 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
46890979 13611 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 352 4 1 5 4.3 Cc1nc(Nc2c(C)cc(Cl)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1084025 13611 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 352 4 1 5 4.3 Cc1nc(Nc2c(C)cc(Cl)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
46891189 13660 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 4 1 6 4.2 Cc1nc(Nc2cc(C(F)(F)F)c(C#N)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1084242 13660 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 397 4 1 6 4.2 Cc1nc(Nc2cc(C(F)(F)F)c(C#N)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
54586829 67428 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 380 6 0 5 4.5 CCCN(CCC)c1nc2c(c(-c3ccc(C)cc3C)c(C)n2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760258 67428 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 380 6 0 5 4.5 CCCN(CCC)c1nc2c(c(-c3ccc(C)cc3C)c(C)n2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
21984580 84327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 433 8 0 5 5.6 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CCCO1 10.1021/jm300259r
CHEMBL2087560 84327 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 433 8 0 5 5.6 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CCCO1 10.1021/jm300259r
60155991 84354 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 515 12 0 9 4.8 COCCN(CC1CCOCC1)c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
CHEMBL2087801 84354 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 515 12 0 9 4.8 COCCN(CC1CCOCC1)c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
45273018 203306 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 381 6 0 5 4.7 CCN(c1c(Cl)cc(OC)cc1Cl)c1nccn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
CHEMBL563618 203306 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 381 6 0 5 4.7 CCN(c1c(Cl)cc(OC)cc1Cl)c1nccn([C@H](C)C2CC2)c1=O 10.1021/jm900301y
44589302 196567 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 425 5 0 7 5.0 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)F)c1 10.1021/jm800743q
CHEMBL516175 196567 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 425 5 0 7 5.0 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)F)c1 10.1021/jm800743q
56677029 72081 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 429 11 1 6 6.1 CCCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
CHEMBL1828893 72081 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 429 11 1 6 6.1 CCCCc1c(Nc2ccc(OC)cc2Cl)nc2ccnn2c1N(CCC)CCC 10.1016/j.bmc.2011.08.055
10379 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1016/j.bmc.2016.11.011
9884366 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1016/j.bmc.2016.11.011
CHEMBL482950 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1016/j.bmc.2016.11.011
DB12572 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by [125I]-CRF addition measured after 1 hr by liquid scintillation counting method
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1016/j.bmc.2016.11.011
24805438 104785 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(CC)Oc1nc(C)cc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
CHEMBL272893 104785 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(CC)Oc1nc(C)cc(Oc2c(C)cc(C)cc2C)c1C 10.1021/jm070578k
44589221 182424 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 375 3 1 7 4.1 Cc1cc(O)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL458115 182424 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 375 3 1 7 4.1 Cc1cc(O)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
58223394 134635 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 14 0 9 4.9 CCOCc1cc(OC)c(-c2csc3c(N(CCCOC)CC4CC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664570 134635 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 14 0 9 4.9 CCOCc1cc(OC)c(-c2csc3c(N(CCCOC)CC4CC4)c(OC)nn23)c(OC)c1 nan
54582098 67816 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 388 9 0 8 2.6 COCCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762823 67816 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 388 9 0 8 2.6 COCCN(CCCF)c1nc(C)nc2c(-c3ccc(OC)nc3)c(C)nn12 10.1016/j.bmcl.2011.02.050
10075105 84341 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 511 11 0 8 5.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087574 84341 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 511 11 0 8 5.5 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
9970050 71514 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 380 6 1 6 4.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
CHEMBL1819064 71514 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 380 6 1 6 4.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)COC2 10.1016/j.bmc.2011.07.055
44190055 202872 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 5 2 5 3.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@@H](CO)C3CC3)c2=O)c(C)c1 10.1021/jm900301y
CHEMBL560823 202872 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 5 2 5 3.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@@H](CO)C3CC3)c2=O)c(C)c1 10.1021/jm900301y
53357140 137369 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 554 7 3 4 7.1 COc1ccc(-c2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2C)c(Cl)c1 nan
CHEMBL3681374 137369 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 554 7 3 4 7.1 COc1ccc(-c2c(NC[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n[nH]c2C)c(Cl)c1 nan
145968888 171937 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4228089 171937 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
58223459 134644 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC(C)OC)c(OC)nn23)c(OC)c1 nan
CHEMBL3664579 134644 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC(C)OC)c(OC)nn23)c(OC)c1 nan
58223427 134670 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 10 0 9 5.2 CCCN(c1cccnc1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664604 134670 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 10 0 9 5.2 CCCN(c1cccnc1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
44191107 201583 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 367 5 1 5 4.6 COc1cc(Cl)c(C)cc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
CHEMBL538866 201583 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 367 5 1 5 4.6 COc1cc(Cl)c(C)cc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1021/jm900302q
57786134 171901 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 387 4 0 3 6.1 CCN(CC)c1cccc2nc3n(c12)CCCC3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4227554 171901 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 387 4 0 3 6.1 CCN(CC)c1cccc2nc3n(c12)CCCC3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
44589291 182261 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 454 5 1 9 2.9 COc1cc(-n2cccn2)ccc1N1CCc2c(-n3ccc(-n4cc[nH]c4=O)n3)cc(C)nc21 10.1021/jm800744m
CHEMBL457742 182261 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 454 5 1 9 2.9 COc1cc(-n2cccn2)ccc1N1CCc2c(-n3ccc(-n4cc[nH]c4=O)n3)cc(C)nc21 10.1021/jm800744m
44589330 182258 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 398 3 0 6 4.5 N#Cc1ccc(N2CCc3c(-n4ccc(-c5ccccn5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
CHEMBL457740 182258 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 398 3 0 6 4.5 N#Cc1ccc(N2CCc3c(-n4ccc(-c5ccccn5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
90654069 135593 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 9 2 9 3.3 CCc1sc2c(NC(=O)C3(O)CC3)c(OC)nn2c1-c1c(OC)cc(COC)cc1OC nan
CHEMBL3669433 135593 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 9 2 9 3.3 CCc1sc2c(NC(=O)C3(O)CC3)c(OC)nn2c1-c1c(OC)cc(COC)cc1OC nan
10177704 71510 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 378 6 1 5 5.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819060 71510 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 378 6 1 5 5.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
10178898 71515 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 396 6 1 6 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CSC2 10.1016/j.bmc.2011.07.055
CHEMBL1819065 71515 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 396 6 1 6 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CSC2 10.1016/j.bmc.2011.07.055
10222795 71531 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 402 5 1 4 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(Cl)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819082 71531 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 402 5 1 4 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(Cl)cc4Cl)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
11751039 182659 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 4 1 7 3.3 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(-n3cccn3)cc1C)CC2 10.1021/jm800744m
CHEMBL458626 182659 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 4 1 7 3.3 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(-n3cccn3)cc1C)CC2 10.1021/jm800744m
21984783 84326 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 433 8 0 5 5.4 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CCOC1 10.1021/jm300259r
CHEMBL2087559 84326 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 433 8 0 5 5.4 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CC1CC1)CC1CCOC1 10.1021/jm300259r
10135080 71523 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 391 6 1 5 5.2 CCC(CC)Nc1c2c(nc3c(-c4ccc(N(C)C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819073 71523 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 391 6 1 5 5.2 CCC(CC)Nc1c2c(nc3c(-c4ccc(N(C)C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
42618205 186949 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 353 5 0 6 3.9 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)c(C)c3C)c(C)nn12 10.1021/jm9000242
CHEMBL474906 186949 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 353 5 0 6 3.9 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)c(C)c3C)c(C)nn12 10.1021/jm9000242
54582962 67426 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 364 2 0 5 3.9 Cc1cc(C)c(-c2cn(C)c3nc(N4CCCCC4)n(C)c(=O)c23)c(C)c1 10.1016/j.bmcl.2011.02.086
CHEMBL1760256 67426 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 364 2 0 5 3.9 Cc1cc(C)c(-c2cn(C)c3nc(N4CCCCC4)n(C)c(=O)c23)c(C)c1 10.1016/j.bmcl.2011.02.086
10296796 70535 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 436 7 0 4 6.5 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)C(C)N2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL180151 70535 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 436 7 0 4 6.5 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)C(C)N2c1ccc(Cl)cc1Cl 10.1021/jm049787k
44589278 182244 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 501 5 0 10 2.9 CS(=O)(=O)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(S(C)(=O)=O)c1 10.1021/jm800743q
CHEMBL457708 182244 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 501 5 0 10 2.9 CS(=O)(=O)c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(S(C)(=O)=O)c1 10.1021/jm800743q
58223475 134609 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 11 0 8 5.9 CCCN(CCC)c1c(C)nn2c(-c3c(OC)cc(COC)cc3OC)c(SC)sc12 nan
CHEMBL3664544 134609 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 11 0 8 5.9 CCCN(CCC)c1c(C)nn2c(-c3c(OC)cc(COC)cc3OC)c(SC)sc12 nan
58223398 134651 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 471 9 0 8 5.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664586 134651 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 471 9 0 8 5.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCOCC1 nan
46891036 14176 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 422 5 1 6 4.9 Cc1nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1086511 14176 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 422 5 1 6 4.9 Cc1nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
44189948 202202 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 6 1 4 5.0 CCC(CC)Cn1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL552237 202202 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 347 6 1 4 5.0 CCC(CC)Cn1cc(Cl)nc(Nc2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
57786117 171899 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 402 4 0 4 5.3 CCN(CC)c1cccc2nc3n(c12)CCC(=O)N3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4227537 171899 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 402 4 0 4 5.3 CCN(CC)c1cccc2nc3n(c12)CCC(=O)N3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
3499 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2007.06.077
9909468 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2007.06.077
CHEMBL44698 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.bmcl.2007.06.077
44444314 101032 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 395 7 0 4 6.3 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)c(F)c1)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL250182 101032 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 395 7 0 4 6.3 CCCC(CCC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)c(F)c1)CC2 10.1016/j.bmcl.2007.06.077
44444336 101269 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 374 5 0 5 4.8 CCC(COC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL251551 101269 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 374 5 0 5 4.8 CCC(COC)n1cc2c3c(nc(C)cc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
3499 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800744m
9909468 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800744m
CHEMBL44698 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800744m
3499 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800743q
9909468 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800743q
CHEMBL44698 8230 28 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm800743q
44589328 196520 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 444 4 0 8 4.5 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)n1 10.1021/jm800743q
CHEMBL515843 196520 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 444 4 0 8 4.5 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)n1 10.1021/jm800743q
21912363 104277 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 4 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C=O)cc2C)c1C 10.1021/jm070578k
CHEMBL270343 104277 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 4 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C=O)cc2C)c1C 10.1021/jm070578k
21912239 104483 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 1 4 5.9 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(C)(C)O)cc2C)c1C 10.1021/jm070578k
CHEMBL271373 104483 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 1 4 5.9 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(C)(C)O)cc2C)c1C 10.1021/jm070578k
54581053 67817 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 389 9 0 9 2.0 COCCN(CCCF)c1nc(C)nc2c(-c3cnc(OC)nc3)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762824 67817 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 389 9 0 9 2.0 COCCN(CCCF)c1nc(C)nc2c(-c3cnc(OC)nc3)c(C)nn12 10.1016/j.bmcl.2011.02.050
71451516 88298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 11 0 7 4.9 CCN(CCOC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160172 88298 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 454 11 0 7 4.9 CCN(CCOC)c1ccc(OC)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
10376 9704 4 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
9801039 9704 4 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
CHEMBL1819077 9704 4 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
42618202 196546 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 433 6 0 7 4.0 CCN(CC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
CHEMBL516026 196546 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 433 6 0 7 4.0 CCN(CC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
71455126 88764 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 395 8 1 6 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165195 88764 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 395 8 1 6 4.2 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
44190825 201925 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 425 4 1 4 5.9 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL550215 201925 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 425 4 1 4 5.9 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
11948286 163448 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4069551 163448 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 410 5 0 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
11363701 74188 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 482 6 1 5 6.0 CCN(Cc1ccco1)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
CHEMBL188858 74188 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 482 6 1 5 6.0 CCN(Cc1ccco1)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1021/jm049737f
54754516 72078 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 1 6 5.3 CCCN(CCC)c1c(CC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828890 72078 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 1 6 5.3 CCCN(CCC)c1c(CC)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
9908904 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm200365y
CHEMBL474287 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm200365y
CHEMBL475306 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm200365y
57402456 76784 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 4 0 5 4.1 CCC(C)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939603 76784 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 4 0 5 4.1 CCC(C)c1cc(C)n2nc(-c3c(C)cc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
24768329 92381 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 368 7 1 5 4.9 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(OC)cc1C 10.1021/jm0611410
CHEMBL228227 92381 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 368 7 1 5 4.9 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(OC)cc1C 10.1021/jm0611410
3499 8230 28 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9000242
9909468 8230 28 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9000242
CHEMBL44698 8230 28 None - 1 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9000242
9908904 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL474287 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475306 187266 4 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
11181033 18546 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 383 7 1 6 3.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1C 10.1021/jm049737f
CHEMBL1181692 18546 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 383 7 1 6 3.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1C 10.1021/jm049737f
CHEMBL188861 18546 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 383 7 1 6 3.8 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1C 10.1021/jm049737f
44591727 198250 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 381 7 0 6 4.7 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL519339 198250 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 381 7 0 6 4.7 CCCCN(CC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3C)c(C)nn12 10.1021/jm9000242
56961969 88771 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 443 9 1 7 3.5 COCC(COC)n1cc(Br)nc(Nc2c(C)cc(OCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165201 88771 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 443 9 1 7 3.5 COCC(COC)n1cc(Br)nc(Nc2c(C)cc(OCF)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
44191186 202394 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 414 6 1 6 4.7 C[C@H](C1CC1)n1cc(C#N)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL556089 202394 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 414 6 1 6 4.7 C[C@H](C1CC1)n1cc(C#N)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1021/jm900302q
56683688 72088 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 413 10 0 6 5.3 C=CCN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
CHEMBL1828900 72088 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 413 10 0 6 5.3 C=CCN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
57398970 76765 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 403 7 1 6 4.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939585 76765 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 403 7 1 6 4.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
46891493 13337 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COC[C@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083012 13337 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COC[C@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
9820671 195597 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL506214 195597 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 1 7 3.9 CC[C@@H](C)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
71580313 95213 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 424 8 1 6 4.4 Cc1cc(C#N)cc(Cl)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
CHEMBL2349564 95213 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 424 8 1 6 4.4 Cc1cc(C#N)cc(Cl)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
57397279 76774 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC(F)F)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939594 76774 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3ccc(OC(F)F)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
10379 9833 39 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cellsDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
9884366 9833 39 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cellsDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
CHEMBL482950 9833 39 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cellsDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
DB12572 9833 39 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cellsDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
42618222 186412 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC[C@H](C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474289 186412 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 1 7 3.7 CCC[C@H](C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
57395433 76763 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 387 6 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939583 76763 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 387 6 0 5 5.1 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
44190341 202903 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 373 6 0 4 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(N(CC)c2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL561035 202903 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 373 6 0 4 5.3 CC[C@H](C1CC1)n1cc(Cl)nc(N(CC)c2c(C)cc(C)cc2C)c1=O 10.1021/jm900301y
9908904 187266 4 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL474287 187266 4 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475306 187266 4 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to CRF1 receptor in human IMR32 cellsBinding affinity to CRF1 receptor in human IMR32 cells
ChEMBL 399 9 0 8 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
56659949 72282 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 381 6 1 5 6.0 CCc1cc(Cl)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
CHEMBL1830525 72282 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 381 6 1 5 6.0 CCc1cc(Cl)ccc1Nc1nc2ccnn2c2c1ccn2C(CC)CC 10.1016/j.bmc.2011.08.055
71580427 95219 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 346 6 1 6 3.2 COc1nc(C)c(Nc2nc(C)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
CHEMBL2349571 95219 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 346 6 1 6 3.2 COc1nc(C)c(Nc2nc(C)cn([C@@H](CF)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2013.02.009
58280028 146701 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 463 10 2 8 4.1 CCCCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
CHEMBL3799560 146701 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 463 10 2 8 4.1 CCCCNC(=O)OC[C@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2016.03.067
46881836 14516 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1089038 14516 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 414 8 1 7 3.9 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cc(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.01.129
44191108 203460 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
CHEMBL564639 203460 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 331 4 1 4 4.5 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1C 10.1021/jm900302q
57400682 76777 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 359 4 0 5 4.2 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939597 76777 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 359 4 0 5 4.2 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
127046470 146396 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccncc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3797551 146396 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccncc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
42618234 195055 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 0 7 3.7 CCCCN(CC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL500013 195055 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 0 7 3.7 CCCCN(CC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
42618186 186775 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 0 7 3.4 C=CCN(C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL474699 186775 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 6 0 7 3.4 C=CCN(C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
42618203 186031 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 493 10 0 9 3.3 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
CHEMBL472874 186031 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 493 10 0 9 3.3 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
58223391 134624 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 13 0 9 4.5 CCCCN(CCOC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664559 134624 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 13 0 9 4.5 CCCCN(CCOC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
60155710 84330 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(C)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087563 84330 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 463 9 0 6 5.5 CCc1nn2c(-c3c(C)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
60155795 84338 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 451 9 0 6 5.5 CCCN(CC1CCOCC1)c1c(CC)nn2c(-c3c(OC)cc(C)cc3OC)cccc12 10.1021/jm300259r
CHEMBL2087571 84338 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 451 9 0 6 5.5 CCCN(CC1CCOCC1)c1c(CC)nn2c(-c3c(OC)cc(C)cc3OC)cccc12 10.1021/jm300259r
21912363 104277 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 4 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C=O)cc2C)c1C 10.1021/jm070578k
CHEMBL270343 104277 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 4 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C=O)cc2C)c1C 10.1021/jm070578k
21912239 104483 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 1 4 5.9 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(C)(C)O)cc2C)c1C 10.1021/jm070578k
CHEMBL271373 104483 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 1 4 5.9 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C(C)(C)O)cc2C)c1C 10.1021/jm070578k
53358377 131224 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 388 5 1 4 4.7 Cc1cc(C(C)C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3639802 131224 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 388 5 1 4 4.7 Cc1cc(C(C)C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
11383860 73797 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
CHEMBL187039 73797 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
21984555 84324 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 407 9 0 5 5.1 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CCOC)CC1CC1 10.1021/jm300259r
CHEMBL2087557 84324 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 407 9 0 5 5.1 CCc1nn2c(-c3c(C)cc(C)cc3OC)cccc2c1N(CCOC)CC1CC1 10.1021/jm300259r
71455051 88288 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 444 9 0 5 6.2 CCN(CC)c1ccc(C(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160162 88288 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 444 9 0 5 6.2 CCN(CC)c1ccc(C(F)F)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
56670201 72086 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 10 0 6 5.6 CCCN(CCC)c1cc(N(CCC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828898 72086 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 415 10 0 6 5.6 CCCN(CCC)c1cc(N(CCC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56659947 72272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 374 7 1 7 4.2 CCC(CC)Nc1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830516 72272 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 374 7 1 7 4.2 CCC(CC)Nc1cc(N(C)c2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
56663414 72278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
CHEMBL1830521 72278 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 401 9 0 6 5.2 CCCN(CCC)c1cc(N(CC)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
58730488 84331 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.2 CCc1nn2c(-c3c(OC)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087564 84331 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 479 10 0 7 5.2 CCc1nn2c(-c3c(OC)cc(OC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
25150449 182540 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 401 4 0 7 5.0 COc1ccc(-n2ccc3c(-n4ccc(-c5nccs5)n4)cc(C)nc32)c(C)c1 10.1021/jm800743q
CHEMBL458353 182540 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 401 4 0 7 5.0 COc1ccc(-n2ccc3c(-n4ccc(-c5nccs5)n4)cc(C)nc32)c(C)c1 10.1021/jm800743q
58223397 134623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 8 0 8 4.8 COc1cc(C)cc(OC)c1-c1csc2c(N(CC3CC3)C3CCOCC3)c(OC)nn12 nan
CHEMBL3664558 134623 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 8 0 8 4.8 COc1cc(C)cc(OC)c1-c1csc2c(N(CC3CC3)C3CCOCC3)c(OC)nn12 nan
71462615 89379 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 11 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCO4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179182 89379 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 11 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCO4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
24768335 92267 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 428 9 1 7 3.7 CCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
CHEMBL227028 92267 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 428 9 1 7 3.7 CCCN(CCOC)c1cc(C)nc2c1NC(=O)CN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
10202622 130600 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 424 7 0 5 4.9 CCCC(COC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL362413 130600 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 424 7 0 5 4.9 CCCC(COC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223445 134621 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 471 10 0 8 4.9 CCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664556 134621 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 471 10 0 8 4.9 CCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 nan
58896479 183048 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 496 6 1 5 8.1 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(CC(C)(C)C)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4566348 183048 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 496 6 1 5 8.1 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(CC(C)(C)C)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4595038 183048 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 496 6 1 5 8.1 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(CC(C)(C)C)c3ccc(Cl)cc3)c2n1C 10.1016/j.bmc.2016.08.005
145959453 168934 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 370 4 1 7 3.3 CCN(CC)c1nc(C)nc2c1s/c(=N/N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
CHEMBL4161963 168934 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 370 4 1 7 3.3 CCN(CC)c1nc(C)nc2c1s/c(=N/N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
58223386 134625 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 10 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664560 134625 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 10 0 9 4.6 COCc1cc(OC)c(-c2csc3c(N(CC4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
58223431 134636 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 10 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC(C)C)C4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664571 134636 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 10 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC(C)C)C4CCOC4)c(OC)nn23)c(OC)c1 nan
58223396 134673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 11 0 9 4.3 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664607 134673 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 11 0 9 4.3 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223461 134674 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.3 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
CHEMBL3664608 134674 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.3 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
10182058 72032 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 444 5 0 5 5.0 CCc1nc2c(n1Cc1ccc(OC)cc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL182779 72032 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 444 5 0 5 5.0 CCc1nc2c(n1Cc1ccc(OC)cc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
10137474 71380 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 428 4 0 4 5.3 CCc1nc2c(n1Cc1ccccc1C)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL181699 71380 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 428 4 0 4 5.3 CCc1nc2c(n1Cc1ccccc1C)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
51352159 89394 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 485 10 0 8 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 nan
CHEMBL2179197 89394 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 485 10 0 8 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 nan
71455473 89393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 470 9 0 9 4.7 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179196 89393 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 470 9 0 9 4.7 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
51352159 89394 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 485 10 0 8 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179197 89394 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 485 10 0 8 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300864p
57786009 171714 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 507 6 0 8 5.2 COc1nc(C)nc(OC)c1N1CCCn2c1nc1c(Cl)ccc(C(OC(F)F)C(F)(F)F)c12 10.1016/j.bmc.2018.01.020
CHEMBL4224781 171714 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 507 6 0 8 5.2 COc1nc(C)nc(OC)c1N1CCCn2c1nc1c(Cl)ccc(C(OC(F)F)C(F)(F)F)c12 10.1016/j.bmc.2018.01.020
24768323 104826 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 0 5 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C(=O)OC 10.1021/jm070578k
CHEMBL273117 104826 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 0 5 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C(=O)OC 10.1021/jm070578k
70692631 82675 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Anatgonist activity at CRF1 receptor (unknown origin)Anatgonist activity at CRF1 receptor (unknown origin)
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.ejmech.2021.114085
CHEMBL2049190 82675 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Anatgonist activity at CRF1 receptor (unknown origin)Anatgonist activity at CRF1 receptor (unknown origin)
ChEMBL 378 7 2 4 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)[nH]c12 10.1016/j.ejmech.2021.114085
58223442 134667 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664601 134667 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
58223478 135591 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.8 COCc1cc(OC)c(-c2csc3c(N(CC4=CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3669431 135591 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.8 COCc1cc(OC)c(-c2csc3c(N(CC4=CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 nan
60155888 84349 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 481 9 0 7 5.7 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(SC)nn12 10.1021/jm300259r
CHEMBL2087796 84349 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 481 9 0 7 5.7 COc1cc(C)cc(OC)c1-c1cccc2c(N(CC3CCOCC3)CC3CC3)c(SC)nn12 10.1021/jm300259r
24768323 104826 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 0 5 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C(=O)OC 10.1021/jm070578k
CHEMBL273117 104826 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 371 7 0 5 5.5 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1C(=O)OC 10.1021/jm070578k
70696716 82681 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 437 11 1 6 6.1 CCCN(CCC)c1cccc2nc(Nc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049197 82681 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 437 11 1 6 6.1 CCCN(CCC)c1cccc2nc(Nc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
58223502 89380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 12 0 9 4.1 COCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL2179183 89380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 12 0 9 4.1 COCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223374 134638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 CCOCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664573 134638 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 CCOCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223416 134659 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 485 11 0 8 5.8 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664593 134659 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 485 11 0 8 5.8 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCCC1 nan
71455472 89378 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 11 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179181 89378 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 487 11 0 9 4.5 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
58223502 89380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 461 12 0 9 4.1 COCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 10.1021/jm300864p
CHEMBL2179183 89380 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 461 12 0 9 4.1 COCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 10.1021/jm300864p
137656239 165309 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 466 7 2 6 4.9 CCN(CCO)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4091442 165309 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 466 7 2 6 4.9 CCN(CCO)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
44156254 171750 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 476 5 0 6 5.8 COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4225373 171750 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 476 5 0 6 5.8 COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
57786307 172003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 475 5 0 5 6.4 COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)c1 10.1016/j.bmc.2018.01.020
CHEMBL4229125 172003 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 475 5 0 5 6.4 COc1ccc(N2CCCn3c2nc2c(Cl)ccc(C(OC(F)F)C(F)(F)F)c23)c(C)c1 10.1016/j.bmc.2018.01.020
58223379 134626 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 477 9 0 8 5.0 COc1cc(Cl)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
CHEMBL3664561 134626 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 477 9 0 8 5.0 COc1cc(Cl)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
9827578 84336 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 507 12 0 7 5.8 CCOCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(CC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087569 84336 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 507 12 0 7 5.8 CCOCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(CC)nn23)c(OC)c1 10.1021/jm300259r
22177864 71527 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 410 7 1 6 5.5 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4SC)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819078 71527 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 410 7 1 6 5.5 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4SC)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
56665181 71534 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 386 6 1 5 5.6 CCC(CC)Nc1c(C)c(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL1819085 71534 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 386 6 1 5 5.6 CCC(CC)Nc1c(C)c(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
53357923 137391 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 461 5 1 3 6.1 CCc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1Cl nan
CHEMBL3681396 137391 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 461 5 1 3 6.1 CCc1nn(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)c(C)c1Cl nan
44392688 73089 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL184930 73089 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptorInhibition of CRF-stimulated cAMP production in cells expressing CRF1 receptor
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
11237255 19026 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 380 7 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1 10.1021/jm049737f
CHEMBL1184638 19026 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 380 7 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1 10.1021/jm049737f
CHEMBL361296 19026 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 380 7 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1 10.1021/jm049737f
10112758 71518 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 418 7 1 5 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C4CCC4)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819068 71518 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 418 7 1 5 6.1 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C4CCC4)nn13)CCC2 10.1016/j.bmc.2011.07.055
71580315 95215 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 444 8 1 6 4.8 N#Cc1cc(Cl)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
CHEMBL2349566 95215 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 444 8 1 6 4.8 N#Cc1cc(Cl)c(Nc2nc(Cl)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
56961966 88766 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 421 8 1 7 3.8 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165197 88766 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 421 8 1 7 3.8 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
57400681 76775 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 4 0 5 3.8 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939595 76775 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 339 4 0 5 3.8 CCC(C)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
46891154 14112 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 328 5 1 6 3.3 COc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
CHEMBL1086233 14112 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 328 5 1 6 3.3 COc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2010.04.121
42618177 191134 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 383 7 1 7 4.3 CCC(CC)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL484408 191134 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 383 7 1 7 4.3 CCC(CC)Nc1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
3496 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
9862166 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
CHEMBL270948 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
42618224 186055 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 1 7 4.1 CCCCC(C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL473070 186055 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 1 7 4.1 CCCCC(C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
3496 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9862166 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270948 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
3496 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9862166 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270948 7963 42 None -1 2 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 326 6 1 3 6.0 CCC(Nc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
127047521 146797 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3800125 146797 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
25114821 76772 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939592 76772 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
127047518 146363 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 406 7 1 8 3.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(C)=O)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3797368 146363 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 406 7 1 8 3.2 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(C)=O)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
56961968 88767 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 439 9 1 7 4.1 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OCF)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165198 88767 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 439 9 1 7 4.1 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(OCF)cc2Cl)c1=O 10.1016/j.bmcl.2012.08.112
9841231 104509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 347 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070578k
CHEMBL271546 104509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 347 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070578k
54584993 67812 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 388 8 0 8 2.5 COCCN(CCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762819 67812 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 388 8 0 8 2.5 COCCN(CCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
9841231 104509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 347 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070578k
CHEMBL271546 104509 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 347 6 0 3 6.3 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070578k
3495 7958 28 None - 1 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
5311055 7958 28 None - 1 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
CHEMBL9946 7958 28 None - 1 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
44190559 202933 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 378 5 1 6 3.4 C#Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
CHEMBL561225 202933 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 378 5 1 6 3.4 C#Cc1cn([C@H](C)C2CC2)c(=O)c(Nc2ccc(OC)nc2C(F)(F)F)n1 10.1021/jm900301y
21912379 162485 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 390 6 1 3 6.5 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070579c
CHEMBL405198 162485 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 390 6 1 3 6.5 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070579c
21912379 162485 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 390 6 1 3 6.5 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070579c
CHEMBL405198 162485 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 390 6 1 3 6.5 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Br)cc2C)c1C 10.1021/jm070579c
57397278 76767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 379 6 0 5 5.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939587 76767 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 379 6 0 5 5.0 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
42618226 186083 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 0 7 3.7 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL473277 186083 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 368 7 0 7 3.7 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
54584992 67811 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 358 6 0 7 2.9 CCN(CCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
CHEMBL1762818 67811 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 358 6 0 7 2.9 CCN(CCF)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1016/j.bmcl.2011.02.050
24768343 149576 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 7 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
CHEMBL389288 149576 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 7 1 5 4.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
44190241 202873 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 6 1 6 3.5 COC[C@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL560827 202873 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 6 1 6 3.5 COC[C@H](C)n1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
25115057 76768 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 399 6 0 5 5.4 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939588 76768 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 399 6 0 5 5.4 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3Cl)n(C3CC3)c(=O)c12 10.1016/j.bmc.2011.11.015
10255153 84334 8 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087549 84334 8 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
CHEMBL2087567 84334 8 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 493 11 0 7 5.4 CCc1nn2c(-c3c(OC)cc(COC)cc3OC)cccc2c1N(CC1CCOCC1)CC1CC1 10.1021/jm300259r
71453734 89376 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCOC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179179 89376 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCOC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
57786200 171999 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 499 4 0 4 7.4 FC(F)OC(c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl)C(F)(F)F 10.1016/j.bmc.2018.01.020
CHEMBL4229070 171999 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 499 4 0 4 7.4 FC(F)OC(c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl)C(F)(F)F 10.1016/j.bmc.2018.01.020
58896503 183321 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 484 8 1 6 6.7 COCCN(c1ccc(Cl)cc1)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.08.005
CHEMBL4540030 183321 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 484 8 1 6 6.7 COCCN(c1ccc(Cl)cc1)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.08.005
CHEMBL4597163 183321 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 484 8 1 6 6.7 COCCN(c1ccc(Cl)cc1)c1cccc2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.08.005
10113560 72096 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 430 8 0 4 6.5 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049787k
CHEMBL182914 72096 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 430 8 0 4 6.5 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049787k
3520 10041 54 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
9821250 10041 54 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
CHEMBL309138 10041 54 None 1 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
11372928 177049 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 7 0 6 4.5 CCCN(CCC)c1c(F)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL444614 177049 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 7 0 6 4.5 CCCN(CCC)c1c(F)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
9865060 70317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 387 6 0 5 5.8 CCCC(CCC)n1cc2c3c(nc(C)nc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL180025 70317 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 387 6 0 5 5.8 CCCC(CCC)n1cc2c3c(nc(C)nc31)N(c1ccc(C#N)cc1C)CC2 10.1016/j.bmcl.2007.06.077
44444318 101185 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 367 5 0 4 5.5 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)c(F)c1)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL250996 101185 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 367 5 0 4 5.5 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)c(F)c1)CC2 10.1016/j.bmcl.2007.06.077
11475476 181771 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 413 4 1 6 3.2 CCc1cc(C#N)ccc1N1CCc2c(-n3ccc(N4CCNC4=O)n3)cc(C)nc21 10.1021/jm800744m
CHEMBL456660 181771 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 413 4 1 6 3.2 CCc1cc(C#N)ccc1N1CCc2c(-n3ccc(N4CCNC4=O)n3)cc(C)nc21 10.1021/jm800744m
58223494 134611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 4.8 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664546 134611 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 4.8 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CC4)CC4CCOC4)c(OC)nn23)c(OC)c1 nan
58223415 134616 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 10 0 9 4.2 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOC1 nan
CHEMBL3664551 134616 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 461 10 0 9 4.2 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOC1 nan
58223501 134668 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 12 0 9 4.9 CCCN(CC1CCOC1)c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664602 134668 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 12 0 9 4.9 CCCN(CC1CCOC1)c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58801661 84340 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 495 11 0 8 4.8 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087573 84340 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 495 11 0 8 4.8 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300259r
46890981 13613 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 358 7 1 7 2.9 COCC(C1CC1)n1nc(C)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1084027 13613 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 358 7 1 7 2.9 COCC(C1CC1)n1nc(C)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
11361847 70672 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 408 5 0 4 5.5 CCc1nc2c(n1C(CC)C(C)C)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL180491 70672 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 408 5 0 4 5.5 CCc1nc2c(n1C(CC)C(C)C)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223387 134619 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 5.0 COc1cc(C(C)OC)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
CHEMBL3664554 134619 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 501 11 0 9 5.0 COc1cc(C(C)OC)cc(OC)c1-c1csc2c(N(CC3CC3)CC3CCOC3)c(OC)nn12 nan
58223495 134657 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 9 0 9 4.4 COCc1cc(OC)c(-c2csc3c(N(C4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664591 134657 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 9 0 9 4.4 COCc1cc(OC)c(-c2csc3c(N(C4CCC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
58223451 134664 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 456 9 0 9 4.4 COCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664598 134664 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 456 9 0 9 4.4 COCCN(c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12)C1CCCC1 nan
58223407 134672 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 480 10 0 9 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)c4cccnc4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664606 134672 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 480 10 0 9 5.2 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)c4cccnc4)c(OC)nn23)c(OC)c1 nan
60155540 84347 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 490 10 0 8 4.7 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C#N)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087794 84347 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 490 10 0 8 4.7 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4CC4)c(C#N)nn23)c(OC)c1 10.1021/jm300259r
44237814 89385 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 11 0 9 5.0 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179188 89385 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 11 0 9 5.0 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
155553483 180970 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 508 7 1 6 7.0 COc1cccc(N(c2cccc3nc(Nc4c(C)cc(Br)cc4OC)n(C)c23)C(C)C)c1 10.1016/j.bmc.2016.08.005
CHEMBL4547748 180970 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 508 7 1 6 7.0 COc1cccc(N(c2cccc3nc(Nc4c(C)cc(Br)cc4OC)n(C)c23)C(C)C)c1 10.1016/j.bmc.2016.08.005
10157505 130633 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 5 0 4 5.3 CCCC(C)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL362601 130633 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 5 0 4 5.3 CCCC(C)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223477 134637 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 482 11 0 9 5.0 CCCN(Cc1ccncc1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664572 134637 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 482 11 0 9 5.0 CCCN(Cc1ccncc1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223420 134671 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 486 11 0 9 5.1 COCc1cc(OC)c(-c2csc3c(N(CCCF)c4cccnc4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664605 134671 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 486 11 0 9 5.1 COCc1cc(OC)c(-c2csc3c(N(CCCF)c4cccnc4)c(OC)nn23)c(OC)c1 nan
71580428 95220 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 397 8 1 8 3.1 COc1nc(C)c(Nc2nc(Cl)cn(C(CCF)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2013.02.009
CHEMBL2349572 95220 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 397 8 1 8 3.1 COc1nc(C)c(Nc2nc(Cl)cn(C(CCF)C3CC3)c2=O)c(OC)n1 10.1016/j.bmcl.2013.02.009
137635682 162779 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 480 7 2 6 5.3 CCN(CC(C)O)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4061900 162779 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 480 7 2 6 5.3 CCN(CC(C)O)c1ccc(Br)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
155565844 182396 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 535 7 2 6 6.3 CNC(=O)c1cccc(N(c2cccc3nc(Nc4c(C)cc(Br)cc4OC)n(C)c23)C(C)C)c1 10.1016/j.bmc.2016.08.005
CHEMBL4580457 182396 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 535 7 2 6 6.3 CNC(=O)c1cccc(N(c2cccc3nc(Nc4c(C)cc(Br)cc4OC)n(C)c23)C(C)C)c1 10.1016/j.bmc.2016.08.005
44589203 182736 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 389 4 0 7 4.4 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C)c1 10.1021/jm800743q
CHEMBL458825 182736 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 389 4 0 7 4.4 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C)c1 10.1021/jm800743q
90654667 116849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 386 9 1 5 6.2 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SCC 10.1016/j.ejmech.2014.03.040
CHEMBL3235703 116849 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 386 9 1 5 6.2 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)c1SCC 10.1016/j.ejmech.2014.03.040
10432407 73091 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 422 7 0 4 6.1 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL184938 73091 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 422 7 0 4 6.1 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
10271870 130211 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 392 4 0 4 4.9 CCc1nc2c(n1C(C)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL361745 130211 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 392 4 0 4 4.9 CCc1nc2c(n1C(C)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
10112643 73126 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 416 6 0 4 6.0 CCc1nc2c(n1C(CC)C(C)C)C(=O)N(C)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049787k
CHEMBL185103 73126 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 416 6 0 4 6.0 CCc1nc2c(n1C(CC)C(C)C)C(=O)N(C)CN2c1ccc(C(C)C)cc1Cl 10.1021/jm049787k
58896411 182984 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assay
ChEMBL 464 7 1 6 6.8 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cc1 10.1016/j.bmc.2016.08.005
CHEMBL4593848 182984 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assayAntagonist activity at human CRF1 receptor expressed in CHO cells assessed as inhibition of CRF-stimulated adenylate cyclase activity measured after 4 hrs by Steady-Glo luciferase assay
ChEMBL 464 7 1 6 6.8 COc1ccc(N(c2cccc3nc(Nc4c(C)cc(Cl)cc4OC)n(C)c23)C(C)C)cc1 10.1016/j.bmc.2016.08.005
58223488 134615 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 10 0 9 4.2 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664550 134615 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 473 10 0 9 4.2 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)C4CCOC4)c(OC)nn23)c(OC)c1 nan
58223480 134618 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 8 0 8 4.8 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664553 134618 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 445 8 0 8 4.8 CCCN(c1c(OC)nn2c(-c3c(OC)cc(C)cc3OC)csc12)C1CCOCC1 nan
11374063 182893 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 5 1 6 3.7 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C(F)F)c1 10.1021/jm800744m
CHEMBL459173 182893 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 440 5 1 6 3.7 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C(F)F)c1 10.1021/jm800744m
44589238 183791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 409 4 0 7 4.7 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
CHEMBL462789 183791 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 409 4 0 7 4.7 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(Cl)c1 10.1021/jm800743q
70692630 82673 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Anatgonist activity at CRF1 receptor (unknown origin)Anatgonist activity at CRF1 receptor (unknown origin)
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.ejmech.2021.114085
CHEMBL2049188 82673 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Anatgonist activity at CRF1 receptor (unknown origin)Anatgonist activity at CRF1 receptor (unknown origin)
ChEMBL 376 7 1 4 6.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)nc12 10.1016/j.ejmech.2021.114085
58223497 134628 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 COCCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664563 134628 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 13 0 9 4.5 COCCCN(CC1CC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223377 134632 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 13 0 9 4.5 CCCN(CCCOC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664567 134632 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 463 13 0 9 4.5 CCCN(CCCOC)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
21984746 84323 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 365 8 0 4 5.5 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3C)cccc12 10.1021/jm300259r
CHEMBL2087556 84323 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 365 8 0 4 5.5 CCCN(CCC)c1c(CC)nn2c(-c3ccc(OC)cc3C)cccc12 10.1021/jm300259r
24768341 92379 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 378 6 1 6 3.7 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1C 10.1021/jm0611410
CHEMBL228223 92379 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 378 6 1 6 3.7 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(C#N)cc1C 10.1021/jm0611410
58223474 134661 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4cccnc4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664595 134661 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4cccnc4)c(OC)nn23)c(OC)c1 nan
42618210 186590 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 5 0 7 3.3 CCN(CC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474493 186590 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 367 5 0 7 3.3 CCN(CC)c1nc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm900025h
145969226 171776 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
CHEMBL4225709 171776 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 491 5 0 7 5.5 COc1nc(C)c(N2CCCn3c2nc2c(Cl)ccc([C@@H](OC(F)F)C(F)(F)F)c23)c(C)n1 10.1016/j.bmc.2018.01.020
44589115 182247 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 458 4 0 8 5.0 O=[N+]([O-])c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
CHEMBL457714 182247 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 458 4 0 8 5.0 O=[N+]([O-])c1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
155520133 180019 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 492 8 1 6 7.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3cccc(OC(C)C)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4524490 180019 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 492 8 1 6 7.6 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3cccc(OC(C)C)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
90654668 116850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 418 11 1 7 4.7 CCSc1c(Nc2c(C)cc(C)cc2C)nc(C)nc1N(CCOC)CCOC 10.1016/j.ejmech.2014.03.040
CHEMBL3235705 116850 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysisDisplacement of [125I]Tyr0sauvagine from human CRF1 receptor expressed in HEK293 cell membrane after 120 mins by gamma scintillation counting analysis
ChEMBL 418 11 1 7 4.7 CCSc1c(Nc2c(C)cc(C)cc2C)nc(C)nc1N(CCOC)CCOC 10.1016/j.ejmech.2014.03.040
58223491 134642 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 13 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CCOC(C)C)CC4CC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664577 134642 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 13 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CCOC(C)C)CC4CC4)c(OC)nn23)c(OC)c1 nan
22177860 71519 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 432 6 1 5 5.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C(F)(F)F)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819069 71519 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 432 6 1 5 5.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C(F)(F)F)nn13)CCC2 10.1016/j.bmc.2011.07.055
67364197 137381 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 519 5 1 5 6.2 Cc1cc(-c2ccc3c(c2)OCO3)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3681386 137381 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 519 5 1 5 6.2 Cc1cc(-c2ccc3c(c2)OCO3)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
56678852 71533 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 372 6 1 5 5.3 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL1819084 71533 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 372 6 1 5 5.3 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3Cl)c(C)nn12 10.1016/j.bmc.2011.07.055
10112776 172993 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 418 5 0 4 5.3 CCc1nc2c(n1C(C1CC1)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL426607 172993 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 418 5 0 4 5.3 CCc1nc2c(n1C(C1CC1)C1CC1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
42618201 186030 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 447 7 1 7 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
CHEMBL472873 186030 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 447 7 1 7 4.8 CCC(CC)Nc1nc(C)nc2c(-c3cc(OC)c(OC)cc3Br)c(C)nn12 10.1021/jm9000242
42618167 187432 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 339 5 0 6 3.6 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL475505 187432 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 339 5 0 6 3.6 CCN(CC)c1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
10379 9833 39 None - 1 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1124/dmd.111.043596
9884366 9833 39 None - 1 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1124/dmd.111.043596
CHEMBL482950 9833 39 None - 1 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1124/dmd.111.043596
DB12572 9833 39 None - 1 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity at human CRF1 receptorAntagonist activity at human CRF1 receptor
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1124/dmd.111.043596
11552261 72284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 361 5 1 5 5.7 CCC(CC)n1ccc2c(Nc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830527 72284 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 361 5 1 5 5.7 CCC(CC)n1ccc2c(Nc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
10379 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm200365y
9884366 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm200365y
CHEMBL482950 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm200365y
DB12572 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm200365y
10379 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
9884366 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
CHEMBL482950 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
DB12572 9833 39 None - 1 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 10.1021/jm900025h
46891032 13441 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083420 13441 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46891091 13594 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083948 13594 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 434 8 1 7 4.2 COCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46891034 14174 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 420 5 1 5 5.4 CCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1086509 14174 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 420 5 1 5 5.4 CCC(C1CC1)n1nc(C)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
44190240 203519 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 4 1 5 4.8 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
CHEMBL565144 203519 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 382 4 1 5 4.8 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C#N)cc2Cl)c1=O 10.1021/jm900301y
24768327 104813 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 392 7 2 6 4.4 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)OC 10.1021/jm070579c
CHEMBL273040 104813 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 392 7 2 6 4.4 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)OC 10.1021/jm070579c
24768327 104813 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 392 7 2 6 4.4 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)OC 10.1021/jm070579c
CHEMBL273040 104813 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 392 7 2 6 4.4 CC[C@@H](CO)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C(=O)OC 10.1021/jm070579c
42618185 186595 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 0 7 3.6 CCCN(C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL474499 186595 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 369 6 0 7 3.6 CCCN(C)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
52918269 67815 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 397 8 0 8 3.2 COc1ccc(-c2c(C)nn3c(N(CCC#N)CCCF)nc(C)nc23)c(C)n1 10.1016/j.bmcl.2011.02.050
CHEMBL1762822 67815 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 397 8 0 8 3.2 COc1ccc(-c2c(C)nn3c(N(CCC#N)CCCF)nc(C)nc23)c(C)n1 10.1016/j.bmcl.2011.02.050
46891289 13655 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 343 6 1 7 3.1 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1084205 13655 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 343 6 1 7 3.1 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(OC)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
46891553 14115 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COC[C@H](C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1086240 14115 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 395 8 1 8 2.9 COC[C@H](C1CC1)n1nc(C)nc(Nc2cc(C)c(OC(F)F)nc2C)c1=O 10.1016/j.bmcl.2010.04.121
44191014 201805 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 441 5 1 5 5.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL549320 201805 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 441 5 1 5 5.8 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(OC(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
44190335 202854 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 5 1 4 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(C)cc2C)c1=O 10.1021/jm900301y
CHEMBL560633 202854 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 331 5 1 4 4.6 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2ccc(C)cc2C)c1=O 10.1021/jm900301y
42618228 187438 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 370 7 0 8 2.6 CCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL475507 187438 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 370 7 0 8 2.6 CCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
46891230 13165 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082300 13165 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 369 5 1 7 3.1 COc1ccc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
127047692 146635 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 441 8 1 8 4.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799211 146635 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 441 8 1 8 4.1 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cccnc3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
44190557 203311 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 379 5 1 7 3.3 COc1ccc(Nc2nc(C#N)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
CHEMBL563652 203311 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 379 5 1 7 3.3 COc1ccc(Nc2nc(C#N)cn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1021/jm900301y
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm200365y
127047549 146740 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 466 8 1 9 4.0 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cc(C#N)ccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799801 146740 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 466 8 1 9 4.0 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3cc(C#N)ccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
46881790 14038 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 387 5 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1N1CCCC1 10.1016/j.bmcl.2010.01.129
CHEMBL1085930 14038 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 387 5 1 6 4.2 Cc1cc(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)nc1N1CCCC1 10.1016/j.bmcl.2010.01.129
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070579c
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
10377 7962 27 None -1 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
9818802 7962 27 None -1 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
CHEMBL270738 7962 27 None -1 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of CRF1 receptorInhibition of CRF1 receptor
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1021/jm070578k
24768333 92359 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 400 8 1 8 2.9 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm0611410
CHEMBL228169 92359 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 400 8 1 8 2.9 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(OC)nc1OC 10.1021/jm0611410
46891157 13265 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 323 4 1 6 3.2 Cc1nc(Nc2cc(C)c(C#N)cc2C)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082705 13265 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 323 4 1 6 3.2 Cc1nc(Nc2cc(C)c(C#N)cc2C)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
44589305 195482 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 390 4 0 8 3.8 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C)n1 10.1021/jm800743q
CHEMBL504383 195482 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 390 4 0 8 3.8 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C)n1 10.1021/jm800743q
10294046 71528 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 394 7 1 6 4.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)c(OC)c4)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819079 71528 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 394 7 1 6 4.8 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)c(OC)c4)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
58223382 89375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 519 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(F)CCOCC4)c(OC)nn23)c(OC)c1 nan
CHEMBL2179178 89375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 519 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(F)CCOCC4)c(OC)nn23)c(OC)c1 nan
58223515 134653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 12 0 9 5.0 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664588 134653 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 12 0 9 5.0 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCCC1 nan
58223449 134654 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 8 0 8 5.0 CCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664589 134654 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 457 8 0 8 5.0 CCN(c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12)C1CCOCC1 nan
58223517 134660 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4ccncc4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664594 134660 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4ccncc4)c(OC)nn23)c(OC)c1 nan
56673724 72075 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 373 8 1 6 4.8 CCCN(CCC)c1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828888 72075 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 373 8 1 6 4.8 CCCN(CCC)c1cc(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
58223382 89375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 519 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(F)CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179178 89375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 519 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4(F)CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
21912450 104788 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 1 4 5.2 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(CO)cc2C)c1C 10.1021/jm070578k
CHEMBL272904 104788 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 1 4 5.2 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(CO)cc2C)c1C 10.1021/jm070578k
21912450 104788 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 1 4 5.2 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(CO)cc2C)c1C 10.1021/jm070578k
CHEMBL272904 104788 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 343 7 1 4 5.2 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(CO)cc2C)c1C 10.1021/jm070578k
58223461 134674 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.3 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
CHEMBL3664608 134674 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 11 0 9 4.3 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
71455050 88287 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(Cl)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160161 88287 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(Cl)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
22177936 71520 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 424 8 1 6 5.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(CSC)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819070 71520 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 424 8 1 6 5.7 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(CSC)nn13)CCC2 10.1016/j.bmc.2011.07.055
10495051 193955 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 308 3 1 4 4.4 CCNc1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
CHEMBL49217 193955 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 308 3 1 4 4.4 CCNc1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
10161139 71971 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 450 8 0 4 6.9 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)C(CC)N2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL182497 71971 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 450 8 0 4 6.9 CCCC(CCC)n1c(CC)nc2c1C(=O)N(C)C(CC)N2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223442 134667 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664601 134667 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OCC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
44478733 89390 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 479 9 0 8 5.3 CCCN(c1c(OC)nn2c(-c3c(Cl)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179193 89390 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 479 9 0 8 5.3 CCCN(c1c(OC)nn2c(-c3c(Cl)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
44191106 203137 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 435 5 1 6 4.3 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(S(C)(=O)=O)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL562492 203137 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 435 5 1 6 4.3 C[C@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(S(C)(=O)=O)cc2Cl)c1=O 10.1021/jm900302q
44444335 101241 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 349 5 0 4 5.4 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL251344 101241 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 349 5 0 4 5.4 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC)cc1)CC2 10.1016/j.bmcl.2007.06.077
53358379 137379 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 394 4 1 4 4.2 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)cnc3C)CC2)n1 nan
CHEMBL3681384 137379 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 394 4 1 4 4.2 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(C(F)(F)F)cnc3C)CC2)n1 nan
58223511 134620 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 459 9 0 8 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(CC)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664555 134620 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 459 9 0 8 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(CC)cc3OC)csc12)C1CCOCC1 nan
70681899 82360 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 480 10 0 7 5.8 CCN(CC1CCOCC1)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046528 82360 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 480 10 0 7 5.8 CCN(CC1CCOCC1)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
11271502 146184 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 476 10 1 7 4.5 COCCN(CCOC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793560 146184 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 476 10 1 7 4.5 COCCN(CCOC)c1cccc2nc(Nc3c(C)cc(Br)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
71457262 89388 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 11 0 9 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179191 89388 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 11 0 9 5.0 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
46881745 13993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 332 4 1 5 3.9 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
CHEMBL1085683 13993 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 332 4 1 5 3.9 Cc1cc(C)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)c(C)n1 10.1016/j.bmcl.2010.01.129
58223516 134663 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 493 11 0 8 5.7 COCCCN(c1c(OC)nn2c(-c3c(Cl)cc(COC)cc3OC)csc12)C1CCCC1 nan
CHEMBL3664597 134663 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 493 11 0 8 5.7 COCCCN(c1c(OC)nn2c(-c3c(Cl)cc(COC)cc3OC)csc12)C1CCCC1 nan
57786313 171763 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 418 3 0 4 6.6 CCC(C#N)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4225575 171763 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 418 3 0 4 6.6 CCC(C#N)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
11223423 196321 30 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 404 4 1 6 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL514270 196321 30 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 404 4 1 6 3.1 COc1ccc(N2CCc3c(-n4ccc(N5CCNC5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
53358376 137383 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 376 5 2 5 3.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(CO)cc2C)CC1 nan
CHEMBL3681388 137383 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 376 5 2 5 3.0 Cc1ncc(Cl)cc1C(=O)N[C@H]1CC[C@H](Cn2nc(CO)cc2C)CC1 nan
56683764 72277 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
CHEMBL1830520 72277 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 0 6 4.8 CCCN(CCC)c1cc(N(C)c2ccc(OC)cc2Cl)nc2nccn12 10.1016/j.bmc.2011.08.055
71449705 88283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(OC)c2nc(-c3c(Cl)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160157 88283 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(OC)c2nc(-c3c(Cl)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
127047520 146846 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3800457 146846 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 469 8 1 9 3.9 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COC(=O)c3ccccn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
3520 10041 54 None 1 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
9821250 10041 54 None 1 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
CHEMBL309138 10041 54 None 1 2 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes preincubated for 1 hr followed by compound washout for 2 hrs and subsequent addition of [125I]-CRF measured after 1 hr by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmc.2016.11.011
53357658 137386 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 429 5 1 4 4.9 COc1cc(C)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
CHEMBL3681391 137386 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 429 5 1 4 4.9 COc1cc(C)nn1C[C@H]1CC[C@H](NC(=O)c2cc(C(F)(F)F)ccc2Cl)CC1 nan
11317069 181760 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 458 4 1 6 4.0 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(OC(F)(F)F)cc1C)CC2 10.1021/jm800744m
CHEMBL456640 181760 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 458 4 1 6 4.0 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(OC(F)(F)F)cc1C)CC2 10.1021/jm800744m
11350078 196566 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 399 3 1 6 3.0 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1C)CC2 10.1021/jm800744m
CHEMBL516170 196566 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 399 3 1 6 3.0 Cc1cc(-n2ccc(N3CCNC3=O)n2)c2c(n1)N(c1ccc(C#N)cc1C)CC2 10.1021/jm800744m
70692632 82676 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 392 7 1 5 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)n(C)c12 10.1016/j.bmcl.2012.05.066
CHEMBL2049191 82676 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 392 7 1 5 5.2 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(=O)n(C)c12 10.1016/j.bmcl.2012.05.066
46890980 13612 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 328 5 1 6 3.3 COc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.04.121
CHEMBL1084026 13612 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 328 5 1 6 3.3 COc1cc(C)c(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)c1 10.1016/j.bmcl.2010.04.121
44397042 19042 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 408 6 2 5 4.6 CCC(CNc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl)OC 10.1021/jm049737f
CHEMBL1184732 19042 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 408 6 2 5 4.6 CCC(CNc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl)OC 10.1021/jm049737f
CHEMBL365868 19042 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 408 6 2 5 4.6 CCC(CNc1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl)OC 10.1021/jm049737f
56683761 72269 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 431 11 0 7 4.8 CCCN(CCC)c1cc(N(CCOC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830513 72269 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 431 11 0 7 4.8 CCCN(CCC)c1cc(N(CCOC)c2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
71451919 89373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179176 89373 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC4CCOCC4)CC4CC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
46891389 13258 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COC[C@@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082671 13258 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COC[C@@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
58896587 180148 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 449 6 1 6 6.5 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(C)cn3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4527586 180148 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 449 6 1 6 6.5 COc1cc(Cl)cc(C)c1Nc1nc2cccc(N(c3ccc(C)cn3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
155548925 180594 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 503 6 1 6 6.8 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C#N)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4538409 180594 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 503 6 1 6 6.8 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C#N)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
53358268 137382 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 376 5 2 5 3.0 Cc1cc(CO)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3681387 137382 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 376 5 2 5 3.0 Cc1cc(CO)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
11703582 72285 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 378 7 0 6 5.4 CCc1ccc(Oc2nc3ccnn3c3c2ccn3C(CC)CC)c(OC)c1 10.1016/j.bmc.2011.08.055
CHEMBL1830528 72285 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 378 7 0 6 5.4 CCc1ccc(Oc2nc3ccnn3c3c2ccn3C(CC)CC)c(OC)c1 10.1016/j.bmc.2011.08.055
10376 9704 4 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma countingDisplacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
9801039 9704 4 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma countingDisplacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
CHEMBL1819077 9704 4 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma countingDisplacement of [125I]CRF from corticotropin-releasing factor receptor 1 in rat brain membranes after 2 hrs by gamma counting
ChEMBL 398 6 1 5 5.5 CCC(Nc1c2CCCc2nc2n1nc(c2c1ccc(cc1Cl)OC)C)CC 10.1016/j.bmc.2011.07.055
56668633 71535 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
CHEMBL1819086 71535 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)CCO2 10.1016/j.bmc.2011.07.055
42618221 186411 11 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL474288 186411 11 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 340 5 1 7 3.3 CC[C@H](C)Nc1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
56670271 72283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 360 5 0 4 5.6 CCC(CC)n1ccc2c(Cc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
CHEMBL1830526 72283 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 360 5 0 4 5.6 CCC(CC)n1ccc2c(Cc3c(C)cc(C)cc3C)nc3ccnn3c21 10.1016/j.bmc.2011.08.055
57786006 171742 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 422 4 0 4 6.4 CCN(CC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4225254 171742 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 422 4 0 4 6.4 CCN(CC)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
11407418 73495 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 416 6 1 4 4.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccccc1Br 10.1021/jm049737f
CHEMBL185648 73495 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 416 6 1 4 4.9 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccccc1Br 10.1021/jm049737f
46891492 13336 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COC[C@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1083011 13336 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 398 7 1 7 3.6 COC[C@H](C1CC1)n1nc(C)nc(Nc2c(Cl)cc(OC)cc2Cl)c1=O 10.1016/j.bmcl.2010.04.121
46891441 13840 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n([C@@H](C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1084988 13840 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n([C@@H](C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
10405373 104178 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 346 6 1 3 6.4 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070579c
CHEMBL269833 104178 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 346 6 1 3 6.4 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070579c
10405373 104178 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 346 6 1 3 6.4 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070579c
CHEMBL269833 104178 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 346 6 1 3 6.4 CCC(CC)Nc1cc(C)nc(Oc2c(C)cc(Cl)cc2C)c1C 10.1021/jm070579c
54754515 72074 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 373 7 2 6 5.0 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828887 72074 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 373 7 2 6 5.0 CCC(CC)Nc1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
71580314 95214 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 404 8 1 6 4.1 Cc1cc(C#N)cc(C)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
CHEMBL2349565 95214 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 404 8 1 6 4.1 Cc1cc(C#N)cc(C)c1Nc1nc(Cl)cn([C@@H](COCCF)C2CC2)c1=O 10.1016/j.bmcl.2013.02.009
24758075 76757 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 350 5 0 4 5.3 CCC(CC)c1cc(C)n2nc(-c3cnc(N(C)C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
CHEMBL1939577 76757 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 350 5 0 4 5.3 CCC(CC)c1cc(C)n2nc(-c3cnc(N(C)C)cc3C)c(C)cc12 10.1016/j.bmc.2011.11.015
58012370 164939 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 433 8 1 4 7.6 CCCC(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4087369 164939 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 433 8 1 4 7.6 CCCC(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
46891440 13169 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
CHEMBL1082309 13169 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn([C@@H](C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
44191185 202714 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 416 4 1 5 5.2 C[C@H](C1CC1)n1cc(C#N)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL559443 202714 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 416 4 1 5 5.2 C[C@H](C1CC1)n1cc(C#N)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
127030925 146271 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 386 6 1 5 5.4 CCN(CC)c1ccc(C)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794475 146271 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 386 6 1 5 5.4 CCN(CC)c1ccc(C)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
10713700 108687 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 362 5 0 4 5.4 C/C=C/CN(CC)c1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
CHEMBL300935 108687 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membraneInhibition of binding of 70 pM [125I]-Try0-o-Corticotropin-releasing Factor (CFR) to Corticotropin releasing hormone receptor 1 in Rat brain membrane
ChEMBL 362 5 0 4 5.4 C/C=C/CN(CC)c1nc(C)nc2c1c(C)cn2-c1c(C)cc(C)cc1C 10.1021/jm960861b
71580216 95210 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 440 9 1 7 4.1 COc1cc(Cl)c(Nc2nc(C#N)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
CHEMBL2349561 95210 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma countingDisplacement of [125I]-o-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting
ChEMBL 440 9 1 7 4.1 COc1cc(Cl)c(Nc2nc(C#N)cn([C@@H](COCCF)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2013.02.009
127047691 146458 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 466 8 1 9 4.0 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccc(C#N)cn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3797955 146458 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 466 8 1 9 4.0 COc1nc(C)c(Nc2nc(Cl)cn([C@H](COc3ccc(C#N)cn3)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
56961967 88770 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 425 8 1 7 3.2 COCC(COC)n1cc(Br)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
CHEMBL2165200 88770 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counterDisplacement of [125I]-o-CRF from CRFR1 in rat frontal cortex after 2 hrs by gamma counter
ChEMBL 425 8 1 7 3.2 COCC(COC)n1cc(Br)nc(Nc2c(C)cc(OC)cc2C)c1=O 10.1016/j.bmcl.2012.08.112
57400679 76764 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 383 7 1 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939584 76764 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 383 7 1 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CCO)c(=O)c12 10.1016/j.bmc.2011.11.015
57393714 76778 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 5 0 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939598 76778 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 5 0 6 3.7 CCC(CC)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
44191105 202027 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 425 4 1 4 5.9 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL551029 202027 1 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 425 4 1 4 5.9 C[C@@H](C1CC1)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
58012303 163570 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 409 5 1 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4070898 163570 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 409 5 1 3 7.5 CCC(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
42618190 186058 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 429 10 0 9 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
CHEMBL473076 186058 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 429 10 0 9 2.8 COCCN(CCOC)c1nc(C)nc2c(-c3c(C)cc(OC)cc3OC)c(C)nn12 10.1021/jm9000242
60141295 82363 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 410 9 0 6 5.3 CCN(CC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046534 82363 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 410 9 0 6 5.3 CCN(CC)c1cccc2nc(Oc3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.05.066
57912459 89392 5 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179195 89392 5 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 503 12 0 9 5.4 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COCC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
58223389 134614 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 505 12 0 10 4.5 CCCCN(CC1COCOC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664549 134614 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 505 12 0 10 4.5 CCCCN(CC1COCOC1)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
22178019 71529 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 412 7 1 5 5.8 CCOc1ccc(-c2c(C)nn3c(NC(CC)CC)c4c(nc23)CCC4)c(Cl)c1 10.1016/j.bmc.2011.07.055
CHEMBL1819080 71529 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 412 7 1 5 5.8 CCOc1ccc(-c2c(C)nn3c(NC(CC)CC)c4c(nc23)CCC4)c(Cl)c1 10.1016/j.bmc.2011.07.055
24768345 92305 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 395 7 1 6 4.0 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
CHEMBL227572 92305 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 395 7 1 6 4.0 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
22177924 71521 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819071 71521 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4ccc(C)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
46881791 14039 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 372 4 1 5 4.3 Cc1nc(C(F)(F)F)ccc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1085931 14039 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 372 4 1 5 4.3 Cc1nc(C(F)(F)F)ccc1Nc1nc(Cl)cn([C@H](C)C2CC2)c1=O 10.1016/j.bmcl.2010.01.129
58223439 134652 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.6 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
CHEMBL3664587 134652 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 475 12 0 9 4.6 COCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCC1 nan
58223408 134627 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 465 8 0 8 5.1 CCCN(c1c(OC)nn2c(-c3c(OC)cc(Cl)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664562 134627 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 465 8 0 8 5.1 CCCN(c1c(OC)nn2c(-c3c(OC)cc(Cl)cc3OC)csc12)C1CCOCC1 nan
58223434 135592 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 517 12 0 9 5.8 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC(C)C)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3669432 135592 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 517 12 0 9 5.8 CCCCN(c1c(OC)nn2c(-c3c(OC)cc(COC(C)C)cc3OC)csc12)C1CCOCC1 nan
46881746 13696 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 346 4 1 6 3.3 Cc1nc2c(cc1Nc1nc(Cl)cn([C@H](C)C3CC3)c1=O)COC2 10.1016/j.bmcl.2010.01.129
CHEMBL1084422 13696 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 346 4 1 6 3.3 Cc1nc2c(cc1Nc1nc(Cl)cn([C@H](C)C3CC3)c1=O)COC2 10.1016/j.bmcl.2010.01.129
21912204 104481 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 325 6 2 3 6.0 CCC(CC)Nc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
CHEMBL271368 104481 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 325 6 2 3 6.0 CCC(CC)Nc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
44589258 182457 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 395 3 0 8 3.8 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C#N)c1 10.1021/jm800743q
CHEMBL458177 182457 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 395 3 0 8 3.8 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C#N)c1 10.1021/jm800743q
70690480 82679 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 443 7 1 4 6.9 Cc1cc(C)c(Nc2nc3cccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2049195 82679 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 443 7 1 4 6.9 Cc1cc(C)c(Nc2nc3cccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
58223505 134662 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4ccccn4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664596 134662 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 500 12 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCCF)Cc4ccccn4)c(OC)nn23)c(OC)c1 nan
70688433 82678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 399 7 1 3 6.8 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)CC4CC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2049194 82678 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 399 7 1 3 6.8 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)CC4CC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
71450106 89377 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCCO4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179180 89377 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4CCCCO4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
155541854 179824 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 549 7 1 6 6.6 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(=O)N(C)C)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4519158 179824 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 549 7 1 6 6.6 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(C(=O)N(C)C)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
10127304 72023 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 436 7 0 6 4.9 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL182744 72023 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 436 7 0 6 4.9 CCCC(CCC)n1c(CC)nc2c1c(=O)n(C)c(=O)n2-c1ccc(Cl)cc1Cl 10.1021/jm049787k
9843355 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptorInhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL1178813 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptorInhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL44169 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptorInhibition of corticotropin releasing factor receptor mediated increase in cAMP level using HEK293 cells expressing h-CRF1 receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
21912204 104481 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 325 6 2 3 6.0 CCC(CC)Nc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
CHEMBL271368 104481 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counterDisplacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
ChEMBL 325 6 2 3 6.0 CCC(CC)Nc1cc(C)nc(Nc2c(C)cc(C)cc2C)c1C 10.1021/jm070579c
58223421 89261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 10 0 8 5.5 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 nan
CHEMBL2177105 89261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 499 10 0 8 5.5 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 nan
58223447 134665 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 11 0 9 5.3 CCCN(c1c(OCC)nn2c(-c3c(OC)cc(OCC)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664599 134665 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 11 0 9 5.3 CCCN(c1c(OCC)nn2c(-c3c(OC)cc(OCC)cc3OC)csc12)C1CCOCC1 nan
58223421 89261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 499 10 0 8 5.5 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2177105 89261 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 499 10 0 8 5.5 COCc1cc(OC)c(-c2c(C)sc3c(N(CC4CCOCC4)CC4CC4)c(C)nn23)c(OC)c1 10.1021/jm300864p
44190056 203124 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 7 1 5 4.7 CCC(CC)Cn1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
CHEMBL562435 203124 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 363 7 1 5 4.7 CCC(CC)Cn1cc(Cl)nc(Nc2cc(C)c(OC)cc2C)c1=O 10.1021/jm900301y
9865624 22316 12 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm040058e
CHEMBL121896 22316 12 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm040058e
56663337 72087 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 427 10 0 6 5.7 C=C(C)CN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
CHEMBL1828899 72087 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 427 10 0 6 5.7 C=C(C)CN(c1cc(N(CCC)CCC)n2nccc2n1)c1ccc(OC)cc1Cl 10.1016/j.bmc.2011.08.055
70690301 82359 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 506 11 0 7 6.1 COCc1cc(OC)c(Oc2nc3cccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2046527 82359 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 506 11 0 7 6.1 COCc1cc(OC)c(Oc2nc3cccc(N(CC4CCOCC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.05.066
58223384 134658 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 9 5.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC(C)C)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3664592 134658 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 9 5.4 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC(C)C)cc3OC)csc12)C1CCOCC1 nan
58896519 146162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 367 7 1 4 6.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)sc12 10.1021/acs.jmedchem.5b01715
CHEMBL3793190 146162 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 367 7 1 4 6.6 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)sc12 10.1021/acs.jmedchem.5b01715
54582017 67422 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 352 4 0 5 3.7 CCN(CC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760252 67422 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 352 4 0 5 3.7 CCN(CC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
70686532 83386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 408 8 0 5 5.5 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063372 83386 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 408 8 0 5 5.5 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70692469 82357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 376 7 0 3 6.9 CCCN(CCC)c1cccc2nc(Oc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2046525 82357 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 376 7 0 3 6.9 CCCN(CCC)c1cccc2nc(Oc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
9843355 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL1178813 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL44169 18002 2 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.Inhibition of corticotropin releasing factor receptor mediated increase in cAMP level using rat cortical homogenates in vitro.
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
44444325 101101 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 417 5 0 4 6.6 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC(F)(F)F)cc1C)CC2 10.1016/j.bmcl.2007.06.077
CHEMBL250603 101101 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membraneDisplacement of [125I]CRF from human recombinant CRF1 receptor expressed in CHO cell membrane
ChEMBL 417 5 0 4 6.6 CCC(CC)n1cc2c3c(nc(C)cc31)N(c1ccc(OC(F)(F)F)cc1C)CC2 10.1016/j.bmcl.2007.06.077
11200917 196487 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 4 0 6 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCN(C)C5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
CHEMBL515532 196487 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 418 4 0 6 3.5 COc1ccc(N2CCc3c(-n4ccc(N5CCN(C)C5=O)n4)cc(C)nc32)c(C)c1 10.1021/jm800744m
11383650 72076 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
CHEMBL1828889 72076 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 387 8 1 6 5.1 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ccnn12 10.1016/j.bmc.2011.08.055
56659948 72273 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 1 7 4.5 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
CHEMBL1830517 72273 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 388 8 1 7 4.5 CCCN(CCC)c1c(C)c(Nc2ccc(OC)cc2Cl)nc2ncnn12 10.1016/j.bmc.2011.08.055
42618200 190944 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 449 10 0 9 3.2 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
CHEMBL482983 190944 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 449 10 0 9 3.2 COCCN(CCOC)c1nc(C)nc2c(-c3cc(OC)c(OC)cc3Cl)c(C)nn12 10.1021/jm9000242
42618233 190994 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 0 7 3.4 CCCCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL483350 190994 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 354 6 0 7 3.4 CCCCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
24768344 92317 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 380 7 1 5 5.1 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
CHEMBL227731 92317 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 380 7 1 5 5.1 CCCCN(CC)c1cc(C)nc2c1NCCN2c1ccc(C(C)=O)cc1C 10.1021/jm0611410
44191110 202404 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 371 5 1 5 4.4 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1F 10.1021/jm900302q
CHEMBL556255 202404 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 371 5 1 5 4.4 COc1cc(Cl)c(Nc2nc(Cl)cn([C@H](C)C3CC3)c2=O)cc1F 10.1021/jm900302q
46891340 13252 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
CHEMBL1082665 13252 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 368 5 1 6 4.0 COc1cc(Cl)c(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(Cl)c1 10.1016/j.bmcl.2010.04.121
25114821 76772 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from rat CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from rat CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939592 76772 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from rat CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from rat CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 390 6 0 6 4.2 CCC(CC)c1cc(C)n2nc(-c3cnc(OC(F)F)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
3520 10041 54 None 1 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/acs.jmedchem.5b01715
9821250 10041 54 None 1 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/acs.jmedchem.5b01715
CHEMBL309138 10041 54 None 1 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/acs.jmedchem.5b01715
42618227 196346 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 400 9 0 9 2.2 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL514465 196346 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 400 9 0 9 2.2 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
44191011 203026 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 459 7 1 6 4.8 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
CHEMBL561757 203026 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration techniqueDisplacement of [125I]ovine-CRF from CRF1 receptor in rat frontal cortex by rapid filtration technique
ChEMBL 459 7 1 6 4.8 COCC(COC)n1cc(Cl)nc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)c1=O 10.1021/jm900302q
57400680 76771 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3cnc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939591 76771 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 354 5 0 6 3.6 CCC(CC)c1cc(C)n2nc(-c3cnc(OC)cc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
46891388 13257 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1082670 13257 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 383 6 1 7 3.5 CCOc1ccc(Nc2nc(C)nn([C@H](C)C3CC3)c2=O)c(C(F)(F)F)n1 10.1016/j.bmcl.2010.04.121
24964079 165743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 401 5 0 4 6.8 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(C#N)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL4096045 165743 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 401 5 0 4 6.8 CCC(CC)c1ccc(Cl)c2nc(Oc3c(C)cc(C#N)cc3Cl)n(C)c12 10.1016/j.bmc.2016.11.011
57402455 76776 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 345 3 0 5 3.8 COc1ccc(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(Cl)c1 10.1016/j.bmc.2011.11.015
CHEMBL1939596 76776 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 345 3 0 5 3.8 COc1ccc(-c2nn3c(C)cc(C(C)C)c3c(=O)n2C)c(Cl)c1 10.1016/j.bmc.2011.11.015
24758076 76756 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 380 7 0 4 6.1 CCc1cc(OC)c(OC)cc1-c1nn2c(C)cc(C(CC)CC)c2cc1C 10.1016/j.bmc.2011.11.015
CHEMBL1939576 76756 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 380 7 0 4 6.1 CCc1cc(OC)c(OC)cc1-c1nn2c(C)cc(C(CC)CC)c2cc1C 10.1016/j.bmc.2011.11.015
58223396 134673 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 11 0 9 4.3 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
CHEMBL3664607 134673 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 487 11 0 9 4.3 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12 nan
58223425 134675 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 469 9 0 8 4.7 CCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12 nan
CHEMBL3664609 134675 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 469 9 0 8 4.7 CCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(C4CC4)cc3OC)csc12 nan
10222402 71512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 396 6 1 6 5.3 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCS2 10.1016/j.bmc.2011.07.055
CHEMBL1819062 71512 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 396 6 1 6 5.3 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4C)c(C)nn13)CCS2 10.1016/j.bmc.2011.07.055
42618173 196368 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 337 3 0 6 3.3 COc1ccc(-c2c(C)nn3c(N4CCCC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
CHEMBL514649 196368 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 337 3 0 6 3.3 COc1ccc(-c2c(C)nn3c(N4CCCC4)nc(C)nc23)c(C)c1 10.1021/jm9000242
70684376 83394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063382 83394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmcl.2012.07.047
70684376 83394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063382 83394 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 428 8 0 5 5.9 CCN(CC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(Cl)cc12 10.1016/j.bmc.2012.09.028
57400683 76781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 4 0 6 3.3 CCC(C)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939600 76781 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 353 4 0 6 3.3 CCC(C)c1cc(C)n2nc(-c3ccc(N(C)C)nc3C)n(C)c(=O)c12 10.1016/j.bmc.2011.11.015
42618231 180254 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 326 4 0 7 2.6 CCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
CHEMBL453001 180254 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 326 4 0 7 2.6 CCN(C)c1nc(C)nc2c(-c3ccc(OC)nc3C)c(C)nn12 10.1021/jm900025h
53357409 137380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 505 6 1 4 6.5 COc1ccc(-c2cc(C)n(C[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n2)cc1 nan
CHEMBL3681385 137380 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 505 6 1 4 6.5 COc1ccc(-c2cc(C)n(C[C@H]3CC[C@H](NC(=O)c4cc(C(F)(F)F)ccc4Cl)CC3)n2)cc1 nan
3499 8230 28 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluatedInhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
9909468 8230 28 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluatedInhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
CHEMBL44698 8230 28 None - 1 Human 7.1 pIC50 = 7.1 Binding
Inhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluatedInhibition of corticotropin releasing factor receptor mediated increase in adenylate cyclase activity was evaluated
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
22177795 71524 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)ccc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819074 71524 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 362 5 1 4 5.4 CCC(CC)Nc1c2c(nc3c(-c4cc(C)ccc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
51352161 135590 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 505 11 0 9 5.7 CCCCN(c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
CHEMBL3669430 135590 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 505 11 0 9 5.7 CCCCN(c1c(SC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 nan
71460919 89384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCC4CC4)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179187 89384 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 501 11 0 9 5.0 COCc1cc(OC)c(-c2csc3c(N(CCC4CC4)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
25150450 182722 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 510 3 1 7 5.4 Cc1cc(-n2ccc(-c3nccs3)n2)c2[nH]c(=O)n(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 10.1021/jm800743q
CHEMBL458780 182722 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 510 3 1 7 5.4 Cc1cc(-n2ccc(-c3nccs3)n2)c2[nH]c(=O)n(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c2n1 10.1021/jm800743q
58896438 146280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3ccc(C)cc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793744 146280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3ccc(C)cc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3794592 146280 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 350 7 1 4 5.6 CCCN(CCC)c1cccc2nc(Nc3ccc(C)cc3C)n(C)c12 10.1021/acs.jmedchem.5b01715
56668634 71537 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)OCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819088 71537 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 400 6 1 6 4.9 CCC(CC)Nc1c2c(nc3c(-c4ccc(OC)cc4Cl)c(C)nn13)OCC2 10.1016/j.bmc.2011.07.055
68581422 181365 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 503 6 1 6 6.8 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3ccc(C#N)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4556873 181365 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 503 6 1 6 6.8 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3ccc(C#N)cc3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
44589257 181593 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 452 4 0 8 5.7 N#Cc1cc(-c2cccs2)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
CHEMBL456241 181593 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 452 4 0 8 5.7 N#Cc1cc(-c2cccs2)ccc1N1CCc2c(-n3ccc(-c4nccs4)n3)ccnc21 10.1021/jm800743q
21912341 104731 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(OC(CC)CC)c(C)c(Oc2c(C)cc(C)cc2C)n1 10.1021/jm070578k
CHEMBL272619 104731 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(OC(CC)CC)c(C)c(Oc2c(C)cc(C)cc2C)n1 10.1021/jm070578k
10160760 130848 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 444 6 0 5 5.1 CCc1nc2c(n1COCc1ccccc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL363240 130848 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 444 6 0 5 5.1 CCc1nc2c(n1COCc1ccccc1)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
58223395 134643 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 13 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CCC(C)OC)CC4CC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664578 134643 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 489 13 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CCC(C)OC)CC4CC4)c(OC)nn23)c(OC)c1 nan
24768336 92303 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 414 9 1 7 4.1 CCCN(CCOC)c1cc(C)nc2c1NCCN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
CHEMBL227503 92303 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 414 9 1 7 4.1 CCCN(CCOC)c1cc(C)nc2c1NCCN2c1cc(OC)c(OC)cc1C 10.1021/jm0611410
44589202 182735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 438 3 0 7 5.0 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
CHEMBL458824 182735 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 438 3 0 7 5.0 N#Cc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
21912341 104731 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(OC(CC)CC)c(C)c(Oc2c(C)cc(C)cc2C)n1 10.1021/jm070578k
CHEMBL272619 104731 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1cc(OC(CC)CC)c(C)c(Oc2c(C)cc(C)cc2C)n1 10.1021/jm070578k
44589303 182798 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 375 4 0 7 4.1 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)cc1 10.1021/jm800743q
CHEMBL458980 182798 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 375 4 0 7 4.1 COc1ccc(N2CCc3c(-n4ccc(-c5nccs5)n4)ccnc32)cc1 10.1021/jm800743q
10159424 129591 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 424 5 0 5 4.6 CCc1nc2c(n1Cc1ccccc1C)C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
CHEMBL360532 129591 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 424 5 0 5 4.6 CCc1nc2c(n1Cc1ccccc1C)C(=O)N(C)CN2c1ccc(OC)cc1Cl 10.1021/jm049787k
58223376 134677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 513 11 0 9 4.7 COCc1cc(OC)c(-c2csc3c(N(CC4CCC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
CHEMBL3664610 134677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 513 11 0 9 4.7 COCc1cc(OC)c(-c2csc3c(N(CC4CCC4)CC4C5COCC54)c(OC)nn23)c(OC)c1 nan
70682293 83383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063369 83383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
70692846 83387 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 460 10 0 5 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
CHEMBL2063373 83387 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 460 10 0 5 6.3 COCc1cc(OC)c(-c2nc3c(C)ccc(N(CC4CC4)CC4CC4)c3cc2C)c(OC)c1 10.1016/j.bmcl.2012.07.047
70682293 83383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2063369 83383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 436 10 0 5 6.3 CCCN(CCC)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
70688432 82677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 375 7 1 3 6.8 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
CHEMBL2049193 82677 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 375 7 1 3 6.8 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)c(C)cc12 10.1016/j.bmcl.2012.05.066
67117558 146731 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 364 6 2 7 2.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](CO)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
CHEMBL3799741 146731 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 364 6 2 7 2.6 COc1nc(C)c(Nc2nc(Cl)cn([C@H](CO)C3CC3)c2=O)cc1C 10.1016/j.bmcl.2016.03.067
53357410 133316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
CHEMBL3652116 133316 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 360 4 1 4 3.8 Cc1cc(C)n(C[C@H]2CC[C@H](NC(=O)c3cc(Cl)cnc3C)CC2)n1 nan
58223512 134630 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 507 12 0 9 5.0 CCOCc1cc(OC)c(-c2csc3c(N(CCCF)C4CCOCC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664565 134630 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 507 12 0 9 5.0 CCOCc1cc(OC)c(-c2csc3c(N(CCCF)C4CCOCC4)c(OC)nn23)c(OC)c1 nan
90654176 134666 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 515 12 0 9 5.3 CCOc1nn2c(-c3c(OC)cc(COC)cc3OC)csc2c1N(CC1CCOCC1)CC1CC1 nan
CHEMBL3664600 134666 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 515 12 0 9 5.3 CCOc1nn2c(-c3c(OC)cc(COC)cc3OC)csc2c1N(CC1CCOCC1)CC1CC1 nan
58223489 135586 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 480 9 0 9 4.1 COc1cc(C#N)cc(OC)c1-c1csc2c(N(CC3CC3)CC3C4COCC43)c(OC)nn12 nan
CHEMBL3669427 135586 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 480 9 0 9 4.1 COc1cc(C#N)cc(OC)c1-c1csc2c(N(CC3CC3)CC3C4COCC43)c(OC)nn12 nan
70684375 83388 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 424 9 0 6 4.8 COCCN(C)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
CHEMBL2063374 83388 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrsDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs
ChEMBL 424 9 0 6 4.8 COCCN(C)c1ccc(C)c2nc(-c3c(OC)cc(COC)cc3OC)c(C)cc12 10.1016/j.bmcl.2012.07.047
145967853 171783 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 410 3 1 5 5.8 CCN(O)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
CHEMBL4225843 171783 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 410 3 1 5 5.8 CCN(O)c1ccc(Cl)c2nc3n(c12)CCCN3c1ccc(Cl)cc1Cl 10.1016/j.bmc.2018.01.020
44589318 184464 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 494 3 1 6 4.8 Cc1cc(-n2ccc(-n3cc[nH]c3=O)n2)c2c(n1)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1021/jm800744m
CHEMBL464185 184464 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cellsDisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells
ChEMBL 494 3 1 6 4.8 Cc1cc(-n2ccc(-n3cc[nH]c3=O)n2)c2c(n1)N(c1ccc(C(F)(F)F)cc1C(F)(F)F)CC2 10.1021/jm800744m
145955820 169453 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 355 4 1 6 4.0 CCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
CHEMBL4170184 169453 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting methodDisplacement of [125I]-Tyr0-sauvagine from human CRFR1 expressed in HEK293 cell membrane homogenates after 120 mins by gamma counting method
ChEMBL 355 4 1 6 4.0 CCN(CC)c1nc(C)nc2c1sc(=N)n2-c1c(C)cc(C)cc1C 10.1016/j.ejmech.2017.07.016
10272004 173023 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 6 0 4 5.5 CCCC(CCC)n1cnc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL426791 173023 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 394 6 0 4 5.5 CCCC(CCC)n1cnc2c1C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
10111139 71526 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4c(C)cc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819076 71526 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 6 1 5 5.4 CCC(CC)Nc1c2c(nc3c(-c4c(C)cc(OC)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
9819381 104474 3 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1c(OC(CC)CC)cc(C)nc1Oc1c(C)cc(C)cc1C 10.1021/jm070578k
CHEMBL271324 104474 3 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1c(OC(CC)CC)cc(C)nc1Oc1c(C)cc(C)cc1C 10.1021/jm070578k
9819381 104474 3 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1c(OC(CC)CC)cc(C)nc1Oc1c(C)cc(C)cc1C 10.1021/jm070578k
CHEMBL271324 104474 3 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 341 7 0 3 6.2 CCc1c(OC(CC)CC)cc(C)nc1Oc1c(C)cc(C)cc1C 10.1021/jm070578k
58280029 146534 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 528 9 2 10 4.6 COc1ccc(NC(=O)OC[C@H](C2CC2)n2cc(Cl)nc(Nc3cc(C)c(OC)nc3C)c2=O)c(C)n1 10.1016/j.bmcl.2016.03.067
CHEMBL3798497 146534 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysisDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate after 2 hrs by gamma counting analysis
ChEMBL 528 9 2 10 4.6 COc1ccc(NC(=O)OC[C@H](C2CC2)n2cc(Cl)nc(Nc3cc(C)c(OC)nc3C)c2=O)c(C)n1 10.1016/j.bmcl.2016.03.067
46891158 13266 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 337 5 1 6 3.5 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(C#N)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
CHEMBL1082706 13266 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 337 5 1 6 3.5 CCC(C1CC1)n1nc(C)nc(Nc2cc(C)c(C#N)cc2C)c1=O 10.1016/j.bmcl.2010.04.121
44190243 202882 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 5 1 4 5.0 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cccc2Cl)c1=O 10.1021/jm900301y
CHEMBL560896 202882 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 351 5 1 4 5.0 CC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)cccc2Cl)c1=O 10.1021/jm900301y
70909805 146092 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3792517 146092 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1021/acs.jmedchem.5b01715
70909805 146092 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
CHEMBL3792517 146092 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 434 8 1 5 6.6 CCCN(CCC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2016.11.011
127030314 146167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2018.01.020
CHEMBL3793277 146167 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 406 6 1 5 5.8 CCN(CC)c1ccc(Cl)c2nc(Nc3c(C)cc(Cl)cc3OC)n(C)c12 10.1016/j.bmc.2018.01.020
57392001 76762 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 6 0 5 4.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
CHEMBL1939582 76762 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counterDisplacement of [125I]CRF from human CRF1 receptor expressed in CHO-K1 cells after 2 hrs by gamma counter
ChEMBL 367 6 0 5 4.7 CCC(CC)c1cc(C)n2nc(-c3ccc(OC)cc3C)n(CC)c(=O)c12 10.1016/j.bmc.2011.11.015
42618174 200113 0 None - 1 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 385 8 1 8 2.8 COCC(COC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
CHEMBL524616 200113 0 None - 1 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyr0-ovine CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 385 8 1 8 2.8 COCC(COC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm9000242
24768324 104436 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1Br 10.1021/jm070578k
CHEMBL271125 104436 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1Br 10.1021/jm070578k
9820041 165011 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 355 8 0 3 6.6 CCCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL408824 165011 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 355 8 0 3 6.6 CCCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
24768324 104436 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1Br 10.1021/jm070578k
CHEMBL271125 104436 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 391 6 0 3 6.4 CCC(CC)Oc1cc(C)nc(Oc2c(C)cc(C)cc2C)c1Br 10.1021/jm070578k
9820041 165011 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 355 8 0 3 6.6 CCCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
CHEMBL408824 165011 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Displacement of [125]oCRF from rat cortex CRF1 receptorDisplacement of [125]oCRF from rat cortex CRF1 receptor
ChEMBL 355 8 0 3 6.6 CCCc1cc(C)c(Oc2nc(C)cc(OC(CC)CC)c2C)c(C)c1 10.1021/jm070578k
24768334 151356 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 386 8 1 8 3.4 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(OC)nc1OC 10.1021/jm0611410
CHEMBL390763 151356 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 386 8 1 8 3.4 CCCCN(CC)c1nc(C)nc2c1NCCN2c1ccc(OC)nc1OC 10.1021/jm0611410
46891089 13592 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
CHEMBL1083946 13592 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 404 6 1 6 4.6 Cc1nc(Nc2c(Cl)cc(OC(F)F)cc2Cl)c(=O)n(C(C)C2CC2)n1 10.1016/j.bmcl.2010.04.121
70690481 82680 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 429 6 1 4 6.6 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
CHEMBL2049196 82680 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 429 6 1 4 6.6 Cc1cc(C)c(Nc2nc3cccc(N(CC4CC4)C4CCOCC4)c3cc2C)c(C)c1 10.1016/j.bmcl.2012.05.066
58801667 84339 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 481 11 0 7 5.4 CCCN(CC1CCOCC1)c1c(CC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
CHEMBL2087572 84339 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 481 11 0 7 5.4 CCCN(CC1CCOCC1)c1c(CC)nn2c(-c3c(OC)cc(COC)cc3OC)cccc12 10.1021/jm300259r
46881866 14784 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 395 8 1 9 2.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)nc(OC)nc2OC)c1=O 10.1016/j.bmcl.2010.01.129
CHEMBL1090740 14784 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 395 8 1 9 2.4 COC[C@H](C1CC1)n1cc(Cl)nc(Nc2c(C)nc(OC)nc2OC)c1=O 10.1016/j.bmcl.2010.01.129
58896512 179756 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 556 7 1 7 6.3 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(S(C)(=O)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
CHEMBL4517763 179756 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount methodDisplacement of ovine [125I-Tyr0]-CRF from human CRF1 receptor expressed in CHO cell membrane measured after 1.5 hrs by TopCount method
ChEMBL 556 7 1 7 6.3 COc1cc(Br)cc(C)c1Nc1nc2cccc(N(c3cccc(S(C)(=O)=O)c3)C(C)C)c2n1C 10.1016/j.bmc.2016.08.005
10205141 70239 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 464 4 0 4 6.1 CCc1nc2c(n1Cc1cccc3ccccc13)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
CHEMBL179826 70239 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptorInhibition of [125I]- Ovine CRF binding to rat frontal cortex corticotropin releasing factor 1 receptor
ChEMBL 464 4 0 4 6.1 CCc1nc2c(n1Cc1cccc3ccccc13)C(=O)N(C)CN2c1ccc(Cl)cc1Cl 10.1021/jm049787k
71453736 89387 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 10 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC(C)C)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
CHEMBL2179190 89387 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 489 10 0 9 4.9 COCc1cc(OC)c(-c2csc3c(N(CC(C)C)C4CCOCC4)c(OC)nn23)c(OC)c1 10.1021/jm300864p
42618215 190873 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 9 2.3 COCCN(CCOC)c1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
CHEMBL482544 190873 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma countingDisplacement of [125I]Tyro-rat/human CRF from CRF1 receptor in rat cortical membrane by gamma counting
ChEMBL 413 9 0 9 2.3 COCCN(CCOC)c1nc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm900025h
44190338 202902 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 453 9 1 6 5.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCc3ccccc3)cc2C)c1=O 10.1021/jm900301y
CHEMBL561034 202902 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Displacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma countingDisplacement of [125I]Tyr-ovine-CRF from CRF1 receptor in rat frontal cortex homogenate by gamma counting
ChEMBL 453 9 1 6 5.4 COC[C@@H](C1CC1)n1cc(Cl)nc(Nc2cc(C)c(OCc3ccccc3)cc2C)c1=O 10.1021/jm900301y
51352160 134613 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 10 4.1 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4COCOC4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664548 134613 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 503 11 0 10 4.1 COCc1cc(OC)c(-c2csc3c(N(CC4CC4)CC4COCOC4)c(OC)nn23)c(OC)c1 nan
10377 7962 27 None -1 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
9818802 7962 27 None -1 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
CHEMBL270738 7962 27 None -1 2 Human 7.0 pIC50 = 7.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2011.02.086
11280845 133614 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 393 7 1 6 3.9 CCN(CCCC#N)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm049737f
CHEMBL365511 133614 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 393 7 1 6 3.9 CCN(CCCC#N)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm049737f
58223470 134608 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 563 12 0 10 6.3 COCc1cc(OC)c(-c2c(SC)sc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 nan
CHEMBL3664543 134608 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 563 12 0 10 6.3 COCc1cc(OC)c(-c2c(SC)sc3c(N(CC4CCOCC4)CC4CC4)c(SC)nn23)c(OC)c1 nan
23567868 71522 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 366 5 1 4 5.2 CCC(CC)Nc1c2c(nc3c(-c4ccc(F)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
CHEMBL1819072 71522 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 366 5 1 4 5.2 CCC(CC)Nc1c2c(nc3c(-c4ccc(F)cc4C)c(C)nn13)CCC2 10.1016/j.bmc.2011.07.055
44589348 182805 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 432 3 0 6 4.9 N#Cc1ccc(N2CCc3c(-n4ccc(-c5ccccn5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
CHEMBL459006 182805 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPADisplacement of [125I]sauvagine from human recombinant CRF1 receptor expressed in CHO cells by SPA
ChEMBL 432 3 0 6 4.9 N#Cc1ccc(N2CCc3c(-n4ccc(-c5ccccn5)n4)ccnc32)c(C(F)(F)F)c1 10.1021/jm800743q
46891190 13198 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 339 5 1 7 2.9 COc1cc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)cc1C#N 10.1016/j.bmcl.2010.04.121
CHEMBL1082401 13198 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-ovine CRF from rat CRF1 receptorDisplacement of [125I]Tyr-ovine CRF from rat CRF1 receptor
ChEMBL 339 5 1 7 2.9 COc1cc(Nc2nc(C)nn(C(C)C3CC3)c2=O)c(C)cc1C#N 10.1016/j.bmcl.2010.04.121
67363460 137368 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 468 7 3 3 5.4 O=C(O)Cc1ccc(NC[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1 nan
CHEMBL3681373 137368 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 468 7 3 3 5.4 O=C(O)Cc1ccc(NC[C@H]2CC[C@@H](NC(=O)c3cc(C(F)(F)F)ccc3Cl)CC2)cc1 nan
58223507 134631 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 537 11 0 9 5.1 COCc1cc(OC)c(-c2csc3c(N(CC4CCOC4)CC4CC(F)(F)C4)c(OC)nn23)c(OC)c1 nan
CHEMBL3664566 134631 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 537 11 0 9 5.1 COCc1cc(OC)c(-c2csc3c(N(CC4CCOC4)CC4CC(F)(F)C4)c(OC)nn23)c(OC)c1 nan
24768330 92351 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 383 7 1 6 3.8 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm0611410
CHEMBL228110 92351 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 383 7 1 6 3.8 CCCCN(CC)c1nc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1021/jm0611410
53357797 137388 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 449 5 2 4 4.7 O=C(N[C@H]1CC[C@H](Cn2cc(Cl)c(CO)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
CHEMBL3681393 137388 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.Homogeneous Time-Resolved Fluorescence Assay: Chinese hamster ovary (CHO) cells expressing either the human or rat recombinant CRF-1 or human CRF-2alpha (Chen et al, Proc Natl Acad Sci USA 90, 8967-8971, 1993; Liaw et al, Endocrinology 137, 72-77, 1996) are propagated in Dulbecco's modified Eagle medium supplemented with 10% foetal calf serum, non-essential amino acids, 100 U/ml penicillin, 100 mg/l streptomycin and 1 g/l geneticin. CHO cells expressing the rat CRF-2beta receptor (Wu et al, Endocrinology 148, 1675-1687, 2007) are propagated in HAM's-F12 Glutamax supplemented with 10% foetal calf serum, 100 IU/ml penicillin, 100 mg/l streptomycin, 600 ug/ml hygromycin, 10 ug/ml blasticidin and induced with 1 ug/ml of tetracyclin for 24 hours prior to experimentation. For cyclic AMP determinations the Homogeneous Time-Resolved Fluoresce (HTRF) CAMP dynamic 2 kit (Cisbio International, France) was used as per manufacturers' instructions.
ChEMBL 449 5 2 4 4.7 O=C(N[C@H]1CC[C@H](Cn2cc(Cl)c(CO)n2)CC1)c1cc(C(F)(F)F)ccc1Cl nan
58896424 146192 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 392 8 1 4 6.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(C(C)C)c12 10.1021/acs.jmedchem.5b01715
CHEMBL3793781 146192 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 392 8 1 4 6.9 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)n(C(C)C)c12 10.1021/acs.jmedchem.5b01715
22178115 71517 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 7 1 5 5.4 CCc1nn2c(NC(CC)CC)c3c(nc2c1-c1ccc(OC)cc1C)CCC3 10.1016/j.bmc.2011.07.055
CHEMBL1819067 71517 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 392 7 1 5 5.4 CCc1nn2c(NC(CC)CC)c3c(nc2c1-c1ccc(OC)cc1C)CCC3 10.1016/j.bmc.2011.07.055
54580961 67424 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 408 8 0 5 5.3 CCCCN(CCCC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
CHEMBL1760254 67424 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cellsDisplacement of ovine [125I]CRF from human CRF1 receptor expressed in CHO cells
ChEMBL 408 8 0 5 5.3 CCCCN(CCCC)c1nc2c(c(-c3c(C)cc(C)cc3C)cn2C)c(=O)n1C 10.1016/j.bmcl.2011.02.086
60155889 84350 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 527 11 1 9 4.6 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4(O)CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
CHEMBL2087797 84350 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counterDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by liquid scintillation counter
ChEMBL 527 11 1 9 4.6 COCc1cc(OC)c(-c2cccc3c(N(CC4CCOCC4)CC4(O)CC4)c(SC)nn23)c(OC)c1 10.1021/jm300259r
57912441 89383 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 475 10 0 9 4.6 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
CHEMBL2179186 89383 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assayDisplacement of [125I]CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation proximity assay
ChEMBL 475 10 0 9 4.6 CCCN(c1c(OC)nn2c(-c3c(OC)cc(COC)cc3OC)csc12)C1CCOCC1 10.1021/jm300864p
58223406 135587 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 9 0 9 4.1 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12 nan
CHEMBL3669428 135587 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.Binding Assay: A binding competition experiment with CRF was conducted by the SPA (GE Healthcare) method using a 96-well plate.
ChEMBL 468 9 0 9 4.1 CCCN(CC1C2COCC21)c1c(OC)nn2c(-c3c(OC)cc(C#N)cc3OC)csc12 nan
71456848 88285 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 394 7 0 5 5.4 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
CHEMBL2160159 88285 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation countingDisplacement of [125I]-CRF from human CRF1 receptor expressed in HEK293 cells after 2 hrs by scintillation counting
ChEMBL 394 7 0 5 5.4 CCN(CC)c1ccc(OC)c2nc(-c3c(OC)cc(C)cc3OC)c(C)cc12 10.1016/j.bmc.2012.09.028
58896475 146144 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 351 7 1 4 6.1 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)oc12 10.1021/acs.jmedchem.5b01715
CHEMBL3793059 146144 0 None - 0 Human 6.0 pIC50 = 6 Binding
Displacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting methodDisplacement of [125I]-CRF from human CRF1 receptor expressed in CHO cellular membrane fraction after 1.5 hrs by liquid scintillation counting method
ChEMBL 351 7 1 4 6.1 CCCN(CCC)c1cccc2nc(Nc3c(C)cc(C)cc3C)oc12 10.1021/acs.jmedchem.5b01715
9884878 179804 18 None - 1 Human 9.6 pKd = 9.6 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2011.08.040
CHEMBL45187 179804 18 None - 1 Human 9.6 pKd = 9.6 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2011.08.040
54591779 72804 0 None - 1 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 429 8 1 7 4.6 COc1cc(OC(F)F)ccc1-n1c(C)nc2c(NC(C3CC3)C3CC3)nc(C)nc21 10.1016/j.bmcl.2011.08.040
CHEMBL1836947 72804 0 None - 1 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 429 8 1 7 4.6 COc1cc(OC(F)F)ccc1-n1c(C)nc2c(NC(C3CC3)C3CC3)nc(C)nc21 10.1016/j.bmcl.2011.08.040
3520 10041 54 None 1 2 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
9821250 10041 54 None 1 2 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
CHEMBL309138 10041 54 None 1 2 Human 9.5 pKd = 9.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2011.08.040
44545165 72802 0 None - 1 Human 9.4 pKd = 9.4 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 433 7 1 6 5.3 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3Cl)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836945 72802 0 None - 1 Human 9.4 pKd = 9.4 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 433 7 1 6 5.3 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3Cl)c2n1 10.1016/j.bmcl.2011.08.040
54591854 72789 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
CHEMBL1836932 72789 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 363 6 1 6 4.0 COc1ccc(-n2c(C)nc3c(NC(C4CC4)C4CC4)nc(C)nc32)cc1 10.1016/j.bmcl.2011.08.040
45485040 204063 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2011.08.040
CHEMBL568606 204063 0 None - 1 Human 7.9 pKd = 7.9 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 383 8 0 7 3.6 CCCN(CCOC)c1nc(C)nc2c1c(C)nn2-c1ccc(OC)cc1C 10.1016/j.bmcl.2011.08.040
44545161 72801 0 None - 1 Human 8.5 pKd = 8.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 399 7 1 6 4.6 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL1836944 72801 0 None - 1 Human 8.5 pKd = 8.5 Binding
Binding affinity to recombinant human CRF1 receptor expressed in CHO cellsBinding affinity to recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 399 7 1 6 4.6 Cc1nc(NC(C2CC2)C2CC2)c2nc(C)n(-c3ccc(OC(F)F)cc3)c2n1 10.1016/j.bmcl.2011.08.040
CHEMBL4299295 220341 0 None 1 2 Human 9.8 pKi = 9.8 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127033542 145400 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775796 145400 0 None 2 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127032315 145206 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3774395 145206 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL4299341 220349 0 None -1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
11546255 194896 0 None 12022 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1016/j.bmcl.2008.07.063
CHEMBL498311 194896 0 None 12022 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1016/j.bmcl.2008.07.063
127031741 145274 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4028 129 57 50 -9.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774868 145274 0 None 1 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4028 129 57 50 -9.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127033842 145295 0 None 8 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4000 127 56 51 -10.2 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2cccs2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL3775030 145295 0 None 8 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4000 127 56 51 -10.2 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2cccs2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
127032010 145249 0 None 9 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4000 127 56 51 -10.2 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccsc2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL3774682 145249 0 None 9 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4000 127 56 51 -10.2 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccsc2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
127032315 145206 0 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3774395 145206 0 None 1 2 Human 9.6 pKi = 9.6 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 126 55 49 -10.4 CCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL4299349 220351 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)N[C@@](C)(CC(C)C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299348 220350 0 None 1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(CC(C)C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127033542 145400 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775796 145400 0 None 2 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3960 128 56 50 -10.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127031439 145377 0 None 5 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3994 127 56 50 -10.3 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL3775621 145377 0 None 5 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3994 127 56 50 -10.3 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc2ccccc2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL4299340 220348 0 None -1 2 Human 9.5 pKi = 9.5 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N1)C(=O)N[C@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC 10.1021/acs.jmedchem.5b00926
10111093 125529 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL341820 125529 0 None - 1 Human 9.4 pKi = 9.4 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
127031736 145384 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3876 124 56 50 -12.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775678 145384 0 None 1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3876 124 56 50 -12.4 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127032314 145398 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3902 125 55 49 -10.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](C)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775778 145398 0 None -1 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3902 125 55 49 -10.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](C)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299352 220352 0 None 2 2 Human 9.4 pKi = 9.4 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299286 220338 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299295 220341 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127031441 145354 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3900 124 55 49 -10.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775437 145354 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3900 124 55 49 -10.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127033544 145403 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4044 127 56 50 -9.1 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL3775812 145403 0 None 2 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4044 127 56 50 -9.1 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccc3ccccc3c2)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
9908879 16852 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 398 6 0 2 7.1 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115389 16852 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 398 6 0 2 7.1 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
127031132 145241 0 None 7 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4044 127 56 50 -9.1 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2cccc3ccccc23)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL3774594 145241 0 None 7 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4044 127 56 50 -9.1 CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2cccc3ccccc23)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
127031129 145395 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3936 130 55 49 -8.8 CCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3775761 145395 0 None -1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3936 130 55 49 -8.8 CCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL4299308 220343 0 None 1 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N1)C(=O)N[C@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC 10.1021/acs.jmedchem.5b00926
127029856 145318 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3866 125 55 49 -10.8 CCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3775192 145318 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3866 125 55 49 -10.8 CCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
10715520 126114 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL344223 126114 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
127030817 145285 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3824 122 55 49 -12.0 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774939 145285 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3824 122 55 49 -12.0 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
9909978 16810 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL115142 16810 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
9909978 16810 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL115142 16810 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
127031129 145395 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3936 130 55 49 -8.8 CCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3775761 145395 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3936 130 55 49 -8.8 CCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
127033847 145268 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 124 55 49 -10.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C(=O)N[C@H](C(N)=O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.5b00926
CHEMBL3774836 145268 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3880 124 55 49 -10.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C(=O)N[C@H](C(N)=O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.5b00926
127029856 145318 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3866 125 55 49 -10.8 CCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3775192 145318 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3866 125 55 49 -10.8 CCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
127031738 145224 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3903 125 55 49 -9.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774485 145224 0 None 1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3903 125 55 49 -9.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
127031126 145256 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3838 123 55 49 -11.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)CC)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774742 145256 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3838 123 55 49 -11.6 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)CC)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299297 220342 0 None -1 2 Human 9.2 pKi = 9.2 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C(=O)N[C@H](C(N)=O)[C@@H](C)CC)C(C)C 10.1021/acs.jmedchem.5b00926
10294626 38908 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 403 6 0 5 5.3 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL140894 38908 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 403 6 0 5 5.3 CCCN(CC1CC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
44347388 121329 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 434 7 0 5 6.4 CCCN(CC1CC1)c1cc(SC)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL333735 121329 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 434 7 0 5 6.4 CCCN(CC1CC1)c1cc(SC)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
127033848 145221 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3852 124 55 49 -11.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)CCC)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3774465 145221 0 None -2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3852 124 55 49 -11.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)CCC)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299286 220338 0 None 2 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(Cc2ccccc2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(Cc1ccccc1)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL4299340 220348 0 None -1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCCN)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N1)C(=O)N[C@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC 10.1021/acs.jmedchem.5b00926
44392711 130324 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 437 6 0 5 5.7 CCCN(CC1CC1)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL361782 130324 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 437 6 0 5 5.7 CCCN(CC1CC1)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
10552787 127513 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 480 7 1 6 5.4 CCCC(CCC)Nc1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
CHEMBL354886 127513 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 480 7 1 6 5.4 CCCC(CCC)Nc1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
CHEMBL439883 220628 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1016/j.bmcl.2015.10.010
CHEMBL439883 220628 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@@H]1CCC(=O)N1)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(=O)O 10.1016/j.bmcl.2015.10.010
127033261 145252 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3992 134 55 49 -7.3 CCCCCCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3774713 145252 0 None 1 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3992 134 55 49 -7.3 CCCCCCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
177990 7214 23 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm980224g
3489 7214 23 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm980224g
CHEMBL296641 7214 23 None -1 2 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm980224g
10694584 65506 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 7 0 5 5.9 CCCCN(CC)c1nc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168554 65506 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 7 0 5 5.9 CCCCN(CC)c1nc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10388138 16771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 432 9 0 4 7.0 CCCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL114912 16771 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 432 9 0 4 7.0 CCCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9821586 174882 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human CRF1 receptor expressed in CHO cells using [125I]-o-CRF as the radioligandBinding affinity towards cloned human CRF1 receptor expressed in CHO cells using [125I]-o-CRF as the radioligand
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL432800 174882 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards cloned human CRF1 receptor expressed in CHO cells using [125I]-o-CRF as the radioligandBinding affinity towards cloned human CRF1 receptor expressed in CHO cells using [125I]-o-CRF as the radioligand
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
9821586 174882 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/j.bmcl.2007.12.050
CHEMBL432800 174882 0 None - 1 Human 9.1 pKi = 9.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/j.bmcl.2007.12.050
10251024 175195 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 410 8 0 4 6.2 CCCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL434882 175195 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 410 8 0 4 6.2 CCCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL4299335 220347 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(Cc1ccccc1)C(=O)N[C@@H](C(N)=O)[C@H](C)CC 10.1021/acs.jmedchem.5b00926
177990 7214 23 None 1 2 Rat 9.0 pKi = 9 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm034077k
3489 7214 23 None 1 2 Rat 9.0 pKi = 9 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm034077k
CHEMBL296641 7214 23 None 1 2 Rat 9.0 pKi = 9 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm034077k
44341921 17066 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 444 9 0 4 7.0 CCCCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL116171 17066 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 444 9 0 4 7.0 CCCCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9998661 64722 0 None - 1 Rat 9.0 pKi = 9 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 360 3 0 4 4.4 COc1cc(Br)c(-n2ccc3c(C)cc(C)nc32)c(OC)c1 10.1021/jm980223o
CHEMBL167241 64722 0 None - 1 Rat 9.0 pKi = 9 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 360 3 0 4 4.4 COc1cc(Br)c(-n2ccc3c(C)cc(C)nc32)c(OC)c1 10.1021/jm980223o
9884878 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm990590f
CHEMBL45187 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1021/jm990590f
9884878 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.ejmech.2016.11.019
CHEMBL45187 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.ejmech.2016.11.019
10428930 210466 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 365 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(C)c12 10.1016/s0960-894x(02)00358-x
CHEMBL67484 210466 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 365 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(C)c12 10.1016/s0960-894x(02)00358-x
9822241 70783 8 None 9 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
CHEMBL1807053 70783 8 None 9 2 Human 9.0 pKi = 9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
9884878 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL45187 179804 18 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma countingDisplacement of [125I]CRF from human corticotropin-releasing factor receptor 1 expressed in CHO-K1 cells after 2 hrs by gamma counting
ChEMBL 352 6 1 5 4.9 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmc.2011.07.055
CHEMBL2373995 217161 0 None 1 2 Human 9.0 pKi = 9.0 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)N[C@@H](CC(=O)O)C(=O)[C@H](CC(=O)O)NC(=O)[C@@H](N)CC(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/jm990590f
CHEMBL4299314 220345 0 None -1 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
9913240 74722 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 484 7 0 5 6.2 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(C)C)cc3Br)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL191090 74722 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 484 7 0 5 6.2 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(C)C)cc3Br)c3nc(C)cc1c32 10.1021/jm050384+
44392663 72295 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 453 8 0 5 6.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL183068 72295 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 453 8 0 5 6.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
44290322 107947 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL295563 107947 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
23595022 70788 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 363 8 1 5 5.0 CCc1nc(-c2ccc(OC)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807058 70788 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 363 8 1 5 5.0 CCc1nc(-c2ccc(OC)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
10667354 123378 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 377 5 1 5 5.3 CCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL336678 123378 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 377 5 1 5 5.3 CCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL4299294 220340 0 None -3 2 Human 9.0 pKi = 9.0 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc1cnc[nH]1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@H](C)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H](C(=O)N[C@H](CC(N)=O)C(=O)N[C@H](CCCNC(=N)N)C(=O)N[C@H](CCCCN)C(=O)N[C@H](CC(C)C)C(=O)NC(CC2CCCCC2)C(=O)N[C@H](CC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@@H](C(N)=O)[C@H](C)CC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](C)NC1=O 10.1021/acs.jmedchem.5b00926
CHEMBL4299355 220353 0 None -1 2 Human 8.9 pKi = 8.9 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
44392722 71340 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 439 7 0 5 6.1 CCCCN(CCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL181536 71340 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 439 7 0 5 6.1 CCCCN(CCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
44392695 130650 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 425 6 0 5 5.7 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL362697 130650 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 425 6 0 5 5.7 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
44341892 117097 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 418 8 0 4 6.7 CCCCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL323886 117097 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 418 8 0 4 6.7 CCCCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
10668220 38052 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 1 5 5.7 CCCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL140143 38052 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 391 6 1 5 5.7 CCCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
10832574 123567 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 363 4 0 5 4.6 CCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL337768 123567 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 363 4 0 5 4.6 CCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
44347200 168520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)c(OC)c3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL413756 168520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)c(OC)c3)c(C)nn12 10.1016/j.bmcl.2004.05.019
11774042 210131 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL65078 210131 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
44341936 16388 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 404 7 0 4 6.3 CCCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112626 16388 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 404 7 0 4 6.3 CCCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44341723 174912 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 416 7 0 4 6.3 CCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL432976 174912 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 416 7 0 4 6.3 CCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
18629227 108264 0 None - 1 Human 8.9 pKi = 8.9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 389 4 0 5 5.5 CCC(CC)n1nnc2c(N3CCc4cc(Cl)cc(Cl)c43)nc(C)cc21 10.1021/jm990590f
CHEMBL297868 108264 0 None - 1 Human 8.9 pKi = 8.9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 389 4 0 5 5.5 CCC(CC)n1nnc2c(N3CCc4cc(Cl)cc(Cl)c43)nc(C)cc21 10.1021/jm990590f
90231873 130728 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 494 6 1 4 5.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628728 130728 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 494 6 1 4 5.6 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1Br 10.1016/j.bmcl.2015.10.010
23595046 70784 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 383 7 1 5 5.1 CCC(CC)Nc1nc(C)c(-c2ccc(C(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
CHEMBL1807054 70784 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 383 7 1 5 5.1 CCC(CC)Nc1nc(C)c(-c2ccc(C(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
11236249 132977 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 448 6 0 6 5.5 CCN(Cc1ccc(Cl)cc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL364987 132977 0 None - 1 Human 8.9 pKi = 8.9 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 448 6 0 6 5.5 CCN(Cc1ccc(Cl)cc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10648981 127520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 497 7 0 5 6.7 CCCCN(CC)c1nc(C)nc2c1nc(C(F)(F)F)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL354982 127520 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 497 7 0 5 6.7 CCCCN(CC)c1nc(C)nc2c1nc(C(F)(F)F)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341845 16270 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 436 8 0 5 6.2 CCCCN(CCSC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112057 16270 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 436 8 0 5 6.2 CCCCN(CCSC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
22248935 70782 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 1 5 5.6 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(OC(F)F)cc1Cl 10.1021/jm200365y
CHEMBL1807052 70782 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 1 5 5.6 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(OC(F)F)cc1Cl 10.1021/jm200365y
10479355 136257 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 8 0 6 5.6 CCCCN(CC)c1nc(C)nc2c1nc(OC)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL367253 136257 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 8 0 6 5.6 CCCCN(CC)c1nc(C)nc2c1nc(OC)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
44386320 138122 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 463 7 0 5 6.3 CCCCN(CC)c1nc(C)nc2c1nc(Cl)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL368772 138122 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 463 7 0 5 6.3 CCCCN(CC)c1nc(C)nc2c1nc(Cl)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10813254 127539 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 445 8 0 6 5.8 CCCCC(CC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL355214 127539 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 445 8 0 6 5.8 CCCCC(CC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341735 117698 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 430 8 0 4 6.7 CCCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL326156 117698 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 430 8 0 4 6.7 CCCCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
15486940 166580 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 356 5 1 4 5.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(C)cc3Cl)c(C)nn12 10.1016/j.ejmech.2016.11.019
CHEMBL4105538 166580 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 356 5 1 4 5.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(C)cc3Cl)c(C)nn12 10.1016/j.ejmech.2016.11.019
9952997 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1021/jm049085v
CHEMBL445075 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1021/jm049085v
11462455 121550 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 356 6 0 4 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL333903 121550 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 356 6 0 4 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
3495 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm9904351
5311055 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm9904351
CHEMBL9946 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm9904351
10136000 35912 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 405 7 1 5 6.1 CCCC(CCC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL138154 35912 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 405 7 1 5 6.1 CCCC(CCC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
10692703 39147 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 405 7 1 5 6.1 CCCCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL141085 39147 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 405 7 1 5 6.1 CCCCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
11774042 210131 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm040058e
CHEMBL65078 210131 0 None - 1 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm040058e
3495 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm980224g
5311055 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm980224g
CHEMBL9946 7958 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm980224g
44392653 130009 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 473 6 0 5 6.5 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL361314 130009 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 473 6 0 5 6.5 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
9951076 74185 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL188844 74185 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL2165204 74185 2 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1016/j.bmcl.2012.08.112
10291750 91388 26 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 355 7 1 7 3.8 CCC(COC)n1nnc2c(Nc3ccc(OC)cc3C)nc(C)cc21 10.1016/j.bmcl.2012.08.112
CHEMBL2165203 91388 26 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 355 7 1 7 3.8 CCC(COC)n1nnc2c(Nc3ccc(OC)cc3C)nc(C)cc21 10.1016/j.bmcl.2012.08.112
CHEMBL2221285 91388 26 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 355 7 1 7 3.8 CCC(COC)n1nnc2c(Nc3ccc(OC)cc3C)nc(C)cc21 10.1016/j.bmcl.2012.08.112
78075688 91389 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 436 9 0 6 4.4 COCCN(CCOC)Cc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL2165205 91389 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 436 9 0 6 4.4 COCCN(CCOC)Cc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL2221286 91389 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 436 9 0 6 4.4 COCCN(CCOC)Cc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
3499 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CRF1 receptor assessed as inhibition constantBinding affinity to human CRF1 receptor assessed as inhibition constant
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.ejmech.2021.113537
9909468 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CRF1 receptor assessed as inhibition constantBinding affinity to human CRF1 receptor assessed as inhibition constant
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.ejmech.2021.113537
CHEMBL44698 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to human CRF1 receptor assessed as inhibition constantBinding affinity to human CRF1 receptor assessed as inhibition constant
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1016/j.ejmech.2021.113537
9931767 16288 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 416 7 0 4 6.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
CHEMBL112152 16288 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 416 7 0 4 6.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
9952997 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL445075 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
9952997 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL445075 177382 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
3499 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
9909468 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
CHEMBL44698 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
137645497 164413 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 356 5 1 4 5.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(Cl)cc3C)c(C)nn12 10.1016/j.ejmech.2016.11.019
CHEMBL4081285 164413 0 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptorDisplacement of [125I-Tyr0]-CRF from recombinant human CRF1 receptor
ChEMBL 356 5 1 4 5.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(Cl)cc3C)c(C)nn12 10.1016/j.ejmech.2016.11.019
3499 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9904351
9909468 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9904351
CHEMBL44698 8230 28 None - 1 Human 8.8 pKi = 8.8 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm9904351
176157 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm960149e
3512 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm960149e
CHEMBL45281 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm960149e
176157 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm9900117
3512 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm9900117
CHEMBL45281 9515 28 None 9 2 Human 8.8 pKi = 8.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm9900117
3499 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
9909468 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
CHEMBL44698 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10.1021/jm990590f
10224173 39145 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 423 8 0 7 3.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL141084 39145 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 423 8 0 7 3.8 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
10344587 174623 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1021/jm034077k
CHEMBL1762817 174623 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1021/jm034077k
CHEMBL430892 174623 0 None 1 2 Rat 8.7 pKi = 8.7 Binding
Affinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brainAffinity for the Corticotropin releasing factor receptor 1 (CRHR1) was determined in rat brain
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1021/jm034077k
9824227 65725 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 433 7 0 7 4.2 CCC(COC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168936 65725 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 433 7 0 7 4.2 CCC(COC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9931814 65792 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 417 6 0 6 5.0 CCC(CC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169248 65792 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 417 6 0 6 5.0 CCC(CC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44347138 22043 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCCN(CC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121286 22043 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 382 8 0 6 4.7 CCCCN(CC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
23595043 70779 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 357 9 1 5 4.9 CCc1cc(OC)ccc1-c1nc(OC)c(NC(CC)CC)nc1CC 10.1021/jm200365y
CHEMBL1807049 70779 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 357 9 1 5 4.9 CCc1cc(OC)ccc1-c1nc(OC)c(NC(CC)CC)nc1CC 10.1021/jm200365y
10786785 35913 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 393 6 1 6 4.6 CCC(COC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL138155 35913 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 393 6 1 6 4.6 CCC(COC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
11639435 78346 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 376 5 0 5 4.7 CC[C@H]1Cn2nc(-c3ccc(OC)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL196312 78346 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 376 5 0 5 4.7 CC[C@H]1Cn2nc(-c3ccc(OC)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11575986 131146 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 448 4 0 4 6.7 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](c1ccccc1)N2CC1CC1 10.1021/jm049085v
CHEMBL363779 131146 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 448 4 0 4 6.7 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](c1ccccc1)N2CC1CC1 10.1021/jm049085v
10740981 64610 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 423 8 0 7 4.0 CCN(CC)c1nc(C)nc(N(CC)c2c(Br)cc(OC)cc2OC)n1 10.1021/jm980222w
CHEMBL167122 64610 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 423 8 0 7 4.0 CCN(CC)c1nc(C)nc(N(CC)c2c(Br)cc(OC)cc2OC)n1 10.1021/jm980222w
10595854 127037 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 378 8 0 6 4.5 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(OC)cc2OC)n1 10.1021/jm980222w
CHEMBL352378 127037 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 378 8 0 6 4.5 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(OC)cc2OC)n1 10.1021/jm980222w
44392741 72014 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL182700 72014 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
11164902 73076 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL184850 73076 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44375351 63292 0 None - 1 Rat 8.0 pKi = 8 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 424 9 0 4 6.6 CCCCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL163618 63292 0 None - 1 Rat 8.0 pKi = 8 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 424 9 0 4 6.6 CCCCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
44307737 107629 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 383 8 0 7 4.0 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)cc3OC)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL293469 107629 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 383 8 0 7 4.0 CCCN(CCC)c1nc(C)nc2c(-c3ccc(OC)cc3OC)n(C)nc12 10.1016/s0960-894x(02)00358-x
11164902 73076 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL184850 73076 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44337527 14220 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 402 7 0 4 5.0 CCCN(c1nc(-c2ccc(Br)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL108673 14220 0 None - 1 Human 8.0 pKi = 8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 402 7 0 4 5.0 CCCN(c1nc(-c2ccc(Br)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
44266482 11271 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.8 CCN(c1nc(C)cc(-c2c(Cl)cccc2Cl)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10208 11271 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.8 CCN(c1nc(C)cc(-c2c(Cl)cccc2Cl)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10813394 65945 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 1 8 3.5 COCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169998 65945 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 1 8 3.5 COCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341818 117272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 8 0 5 5.5 CCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL324889 117272 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 8 0 5 5.5 CCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9867507 65841 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 0 7 3.9 CCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169539 65841 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 0 7 3.9 CCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10576086 65875 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 463 9 0 9 2.4 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1Br 10.1021/jm980224g
CHEMBL169711 65875 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 463 9 0 9 2.4 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1Br 10.1021/jm980224g
44341817 179354 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 7 0 5 5.4 COCCN(CC(C)C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL448788 179354 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 7 0 5 5.4 COCCN(CC(C)C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
10574875 127522 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 434 7 0 7 4.6 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(SC)cc1Br 10.1021/jm980224g
CHEMBL355006 127522 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 434 7 0 7 4.6 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(SC)cc1Br 10.1021/jm980224g
12967651 26691 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 445 8 0 4 6.8 CCCN(Cc1sc(N(C)c2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL130264 26691 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 445 8 0 4 6.8 CCCN(Cc1sc(N(C)c2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44392710 71374 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 0 7 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N=O)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL181684 71374 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 0 7 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N=O)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
10671924 66150 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 466 7 0 8 3.3 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(S(C)(=O)=O)cc1Br 10.1021/jm980224g
CHEMBL170844 66150 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 466 7 0 8 3.3 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(S(C)(=O)=O)cc1Br 10.1021/jm980224g
44347108 22018 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 370 7 0 4 5.5 CCCN(CCC)c1cc(CC)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121116 22018 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 370 7 0 4 5.5 CCCN(CCC)c1cc(CC)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
44305971 107380 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 10 0 6 4.4 C=CCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL291828 107380 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 10 0 6 4.4 C=CCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
20780034 137246 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 382 7 0 4 4.8 CCCN(CCC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL368041 137246 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 382 7 0 4 4.8 CCCN(CCC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
10298157 130011 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 457 8 1 4 7.3 C=CCN(CCC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL361323 130011 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 457 8 1 4 7.3 C=CCN(CCC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10207702 138769 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1ccncc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL369531 138769 0 None - 1 Human 7.0 pKi = 7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1ccncc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11246476 130833 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 396 6 0 7 3.4 CCCC(OC)N1CCn2c(=O)n(-c3ccc(OC)cc3C)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL363152 130833 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 396 6 0 7 3.4 CCCC(OC)N1CCn2c(=O)n(-c3ccc(OC)cc3C)c3nc(C)cc1c32 10.1021/jm050384+
44389125 71391 0 None - 1 Human 5.0 pKi = 5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 429 4 1 4 6.5 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CCCC1 10.1016/j.bmcl.2004.10.055
CHEMBL181765 71391 0 None - 1 Human 5.0 pKi = 5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 429 4 1 4 6.5 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CCCC1 10.1016/j.bmcl.2004.10.055
44460545 212346 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 452 7 1 3 6.8 O=C(CCc1ccncc1)C(Nc1ccc(Cl)cc1Cl)c1ccccc1C(F)(F)F 10.1021/jm049974i
CHEMBL81262 212346 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 452 7 1 3 6.8 O=C(CCc1ccncc1)C(Nc1ccc(Cl)cc1Cl)c1ccccc1C(F)(F)F 10.1021/jm049974i
10790231 65812 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 10 0 10 2.1 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
CHEMBL169365 65812 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 10 0 10 2.1 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
44446715 101516 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2Cl)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253084 101516 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 386 6 0 2 7.1 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2Cl)c2ccccc12 10.1016/j.bmcl.2007.12.050
44460553 212675 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity of compound towards human Corticotropin releasing factor receptor 1Binding affinity of compound towards human Corticotropin releasing factor receptor 1
ChEMBL 442 7 1 3 6.2 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2Br)c(Cl)c1 10.1021/jm049974i
CHEMBL83914 212675 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity of compound towards human Corticotropin releasing factor receptor 1Binding affinity of compound towards human Corticotropin releasing factor receptor 1
ChEMBL 442 7 1 3 6.2 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2Br)c(Cl)c1 10.1021/jm049974i
10548395 109637 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 389 8 1 5 5.7 CCCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL305671 109637 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 389 8 1 5 5.7 CCCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10542924 211917 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 309 3 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nc(N3CC=CCC3)n2)c(C)c1 10.1021/jm960148m
CHEMBL78035 211917 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 309 3 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nc(N3CC=CCC3)n2)c(C)c1 10.1021/jm960148m
10548395 109637 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 389 8 1 5 5.7 CCCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL305671 109637 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 389 8 1 5 5.7 CCCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
10542924 211917 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 309 3 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nc(N3CC=CCC3)n2)c(C)c1 10.1021/jm9900117
CHEMBL78035 211917 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 309 3 1 5 3.6 Cc1cc(C)c(Nc2nc(C)nc(N3CC=CCC3)n2)c(C)c1 10.1021/jm9900117
44446735 101404 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 428 8 0 5 5.9 CCCN(CCn1ccnc1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252301 101404 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 428 8 0 5 5.9 CCCN(CCn1ccnc1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
44460602 212525 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 459 6 2 4 6.2 COc1ccc(C(=O)C(Nc2ccc(C)cc2Cl)c2ccccc2Br)cc1O 10.1021/jm049974i
CHEMBL82707 212525 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 459 6 2 4 6.2 COc1ccc(C(=O)C(Nc2ccc(C)cc2Cl)c2ccccc2Br)cc1O 10.1021/jm049974i
44317955 110697 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 470 6 2 3 5.8 CNC(=O)c1cccc(C(=O)C(Nc2ccc(C)cc2Cl)c2ccccc2Br)c1 10.1021/jm049974i
CHEMBL309244 110697 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 470 6 2 3 5.8 CNC(=O)c1cccc(C(=O)C(Nc2ccc(C)cc2Cl)c2ccccc2Br)c1 10.1021/jm049974i
11395370 80953 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 2 5 4.4 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(CO)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL202299 80953 0 None - 1 Rat 6.0 pKi = 6.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 2 5 4.4 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(CO)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
11065773 209774 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 278 4 2 4 2.8 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C#N 10.1021/jm025512y
CHEMBL63140 209774 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 278 4 2 4 2.8 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C#N 10.1021/jm025512y
44266473 11190 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 409 5 0 3 6.5 CCN(c1nc(C)cc(-c2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10150 11190 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 409 5 0 3 6.5 CCN(c1nc(C)cc(-c2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10494830 127126 1 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 305 2 0 3 3.9 Cc1ccc(N(C)c2nc(C)cc(C)n2)c(Br)c1 10.1021/jm980222w
CHEMBL353075 127126 1 None - 1 Rat 6.0 pKi = 6.0 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 305 2 0 3 3.9 Cc1ccc(N(C)c2nc(C)cc(C)n2)c(Br)c1 10.1021/jm980222w
20780064 131107 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 480 7 0 4 6.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL363592 131107 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 480 7 0 4 6.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
11797750 64870 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 448 10 0 5 5.7 CCCN(CCOC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL167444 64870 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 448 10 0 5 5.7 CCCN(CCOC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10739468 65779 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 395 7 0 5 4.9 CCN(CC)c1cc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL169094 65779 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 395 7 0 5 4.9 CCN(CC)c1cc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
44347356 119646 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 372 7 1 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(CO)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL330954 119646 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 372 7 1 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(CO)nn12 10.1016/j.bmcl.2004.05.019
44341712 121738 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL334262 121738 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
10024020 209881 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63989 209881 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 401 9 0 5 5.2 CCCN(c1nccc(-c2c(Cl)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
44307806 210551 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 393 8 0 5 5.8 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(CCC)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL68076 210551 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 393 8 0 5 5.8 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(CCC)nc12 10.1016/s0960-894x(02)00358-x
44305523 108945 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 392 6 0 5 4.8 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL302645 108945 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 392 6 0 5 4.8 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
20780164 100496 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 421 7 0 5 5.7 C=CCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247151 100496 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 421 7 0 5 5.7 C=CCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
20780148 157902 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 7 0 5 5.9 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
CHEMBL395929 157902 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 7 0 5 5.9 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
9980466 160907 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 436 9 1 6 5.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
CHEMBL398531 160907 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 436 9 1 6 5.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
10302495 130067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 541 8 1 4 8.9 CCCN(Cc1ccc(Cl)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL361438 130067 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 541 8 1 4 8.9 CCCN(Cc1ccc(Cl)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11189570 134261 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.2 Cc1cc(N(Cc2ccccc2)C(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
CHEMBL366096 134261 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.2 Cc1cc(N(Cc2ccccc2)C(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
9803645 65497 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 446 7 0 7 4.3 CCC(COC)N(C)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168519 65497 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 446 7 0 7 4.3 CCC(COC)N(C)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341858 117911 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 446 7 0 5 6.0 CCCCN(CC1CCCO1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL326355 117911 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 446 7 0 5 6.0 CCCCN(CC1CCCO1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
18691306 105352 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 451 5 0 3 7.4 CCN(c1nc(C)cc(-c2c(C)cc(C)cc2C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL276716 105352 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 451 5 0 3 7.4 CCN(c1nc(C)cc(-c2c(C)cc(C)cc2C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
22249041 70751 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 358 9 1 6 4.3 CCc1nc(-c2ccc(OC)nc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806958 70751 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 358 9 1 6 4.3 CCc1nc(-c2ccc(OC)nc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
11155051 113127 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 446 8 0 5 6.2 CCCN(c1nc(-c2ccc(OC)cc2C)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL3085415 113127 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 446 8 0 5 6.2 CCCN(c1nc(-c2ccc(OC)cc2C)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL3139200 113127 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 446 8 0 5 6.2 CCCN(c1nc(-c2ccc(OC)cc2C)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
136216703 85680 0 None -5 5 Rat 7.0 pKi = 7.0 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 482 2 4 7 4.0 N[C@H]1CCCC[C@@H]1NC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL2112936 85680 0 None -5 5 Rat 7.0 pKi = 7.0 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 482 2 4 7 4.0 N[C@H]1CCCC[C@@H]1NC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
44392740 130604 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 337 6 0 5 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncccc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL362437 130604 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 337 6 0 5 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncccc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
10142769 13274 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 520 8 0 4 7.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC4CC4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082720 13274 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 520 8 0 4 7.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC4CC4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
44392771 73445 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 7 3.7 CCCN(CC1CC1)c1cc(C(=O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL185400 73445 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 7 3.7 CCCN(CC1CC1)c1cc(C(=O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
44389050 69276 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 505 6 2 8 7.1 CSc1snnc1NCc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL178131 69276 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 505 6 2 8 7.1 CSc1snnc1NCc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10140223 130033 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 471 8 1 4 7.5 CCN(CCC1CC1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL361394 130033 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 471 8 1 4 7.5 CCN(CCC1CC1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10160871 26584 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 445 8 1 4 6.7 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1CC 10.1016/j.bmcl.2003.08.055
CHEMBL130180 26584 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 445 8 1 4 6.7 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1CC 10.1016/j.bmcl.2003.08.055
10551027 64363 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 438 3 0 5 4.9 Cc1cc(N2CCOCC2)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL166760 64363 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 438 3 0 5 4.9 Cc1cc(N2CCOCC2)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
44307652 210577 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 7 1 5 5.6 CCCCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL68303 210577 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 7 1 5 5.6 CCCCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44385525 66814 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 394 6 0 7 3.4 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
CHEMBL173624 66814 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 394 6 0 7 3.4 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
10902707 210377 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1Cl 10.1021/jm025512y
CHEMBL66950 210377 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1Cl 10.1021/jm025512y
44308155 210494 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 446 7 0 6 5.0 CCCN(CCN1CCCC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL67646 210494 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 446 7 0 6 5.0 CCCN(CCN1CCCC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44443574 101106 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 381 8 2 5 5.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1ncc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
CHEMBL250616 101106 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 381 8 2 5 5.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1ncc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
10567951 211857 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 323 7 1 5 4.0 C=CCN(CC=C)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL77391 211857 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 323 7 1 5 4.0 C=CCN(CC=C)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10567951 211857 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 323 7 1 5 4.0 C=CCN(CC=C)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL77391 211857 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 323 7 1 5 4.0 C=CCN(CC=C)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
10222698 194629 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 401 10 1 6 4.3 CCCN(CCC)c1c(CC(C)O)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL496269 194629 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 401 10 1 6 4.3 CCCN(CCC)c1c(CC(C)O)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
44385545 67051 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 499 9 0 6 5.8 CCCCN(CC)c1nc(C)nc2c1n(CC1CC1)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL174213 67051 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 499 9 0 6 5.8 CCCCN(CC)c1nc(C)nc2c1n(CC1CC1)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
44385463 68153 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 433 6 1 7 3.4 COCCNc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL176937 68153 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 433 6 1 7 3.4 COCCNc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
20780127 142020 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 446 6 0 4 5.9 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL372499 142020 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 446 6 0 4 5.9 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12 10.1016/j.bmcl.2005.06.028
135593026 70721 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 343 8 2 5 4.6 CCc1nc(-c2ccc(OC)cc2O)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806735 70721 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 343 8 2 5 4.6 CCc1nc(-c2ccc(OC)cc2O)c(CC)nc1NC(CC)CC 10.1021/jm200365y
44443571 101105 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 314 7 0 5 4.2 CCCN(CCC)c1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
CHEMBL250615 101105 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 314 7 0 5 4.2 CCCN(CCC)c1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
11475729 82151 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 422 7 1 5 5.5 C=CCOc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL203807 82151 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 422 7 1 5 5.5 C=CCOc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
9887145 133429 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 398 6 0 5 4.9 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL365260 133429 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 398 6 0 5 4.9 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
9907170 184878 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980222w
CHEMBL46479 184878 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980222w
44392687 73442 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 457 8 0 7 4.2 COCCN(CCOC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL185393 73442 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 457 8 0 7 4.2 COCCN(CCOC)c1cc(C)nc2c(-c3ncc(C(F)(F)F)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
21916254 13177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 576 7 0 4 8.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccc(Cl)cc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082338 13177 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 576 7 0 4 8.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccc(Cl)cc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
10300313 13591 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 494 7 0 4 6.9 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083935 13591 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 494 7 0 4 6.9 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
22248932 70768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 463 6 1 3 6.2 CCc1nc(NC(CC)CC)c(I)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807034 70768 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 463 6 1 3 6.2 CCc1nc(NC(CC)CC)c(I)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
44388407 69785 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL178735 69785 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
9907170 184878 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneInhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm990590f
CHEMBL46479 184878 0 None -2 2 Human 7.9 pKi = 7.9 Binding
Inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneInhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm990590f
44341663 117651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 432 8 0 4 5.9 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
CHEMBL326107 117651 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 432 8 0 4 5.9 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
44384779 66485 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 487 8 0 7 4.2 COCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL172358 66485 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 487 8 0 7 4.2 COCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10739849 65277 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 401 5 0 5 4.9 CCN(CC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168353 65277 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 401 5 0 5 4.9 CCN(CC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341762 16927 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 7 0 5 5.1 CCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL115820 16927 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 7 0 5 5.1 CCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
11625175 78687 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 384 4 0 4 5.2 CC[C@H]1Cn2nc(-c3ccc(F)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL197187 78687 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 384 4 0 4 5.2 CC[C@H]1Cn2nc(-c3ccc(F)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11530590 147554 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 4 0 4 5.0 CC[C@H]1Cn2nc(-c3ccc(C)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL381850 147554 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 4 0 4 5.0 CC[C@H]1Cn2nc(-c3ccc(C)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
9957261 72050 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 490 7 0 6 7.0 CCCN(CC1CC1)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL18285 72050 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 490 7 0 6 7.0 CCCN(CC1CC1)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
10669526 172193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 414 4 1 6 4.8 Cc1nc(NC2CCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
CHEMBL423833 172193 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 414 4 1 6 4.8 Cc1nc(NC2CCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
44446738 101423 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 473 10 0 4 7.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252492 101423 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 473 10 0 4 7.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
10117501 70959 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 493 7 1 4 7.9 CCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL180880 70959 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 493 7 1 4 7.9 CCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11441193 70190 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 408 10 0 6 5.3 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL179647 70190 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 408 10 0 6 5.3 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
44337549 15946 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 352 7 0 4 4.8 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL110222 15946 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 352 7 0 4 4.8 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
11223627 75446 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 410 6 0 6 3.9 COCC(COC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL192082 75446 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 410 6 0 6 3.9 COCC(COC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
44392731 130530 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 385 9 0 6 3.3 COCCN(CCOC)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL362226 130530 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 385 9 0 6 3.3 COCCN(CCOC)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
46891008 13206 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 424 3 0 4 5.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082441 13206 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 424 3 0 4 5.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780056 153019 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 444 5 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)Cc4ccncc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL392044 153019 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 444 5 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)Cc4ccncc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
20780286 14101 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 448 6 0 4 5.6 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1086164 14101 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 448 6 0 4 5.6 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
44389097 69789 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 441 4 1 4 6.6 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CC=CCC1 10.1016/j.bmcl.2004.10.055
CHEMBL178751 69789 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 441 4 1 4 6.6 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CC=CCC1 10.1016/j.bmcl.2004.10.055
10853581 127042 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 326 5 1 7 2.5 COCCNc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL352436 127042 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 326 5 1 7 2.5 COCCNc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44443572 161553 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 326 7 0 5 4.2 CCCN(CC1CC1)c1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
CHEMBL400155 161553 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 326 7 0 5 4.2 CCCN(CC1CC1)c1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
44443661 100894 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 503 9 1 6 6.1 CCc1nc(N(C)c2ncc(Cl)cc2Cl)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
CHEMBL249212 100894 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 503 9 1 6 6.1 CCc1nc(N(C)c2ncc(Cl)cc2Cl)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
44443636 101189 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 390 6 1 6 4.7 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
CHEMBL251006 101189 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 390 6 1 6 4.7 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
9890659 105838 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 464 3 0 7 5.2 Cc1nc(N2CCOCC2)c2sc(=S)n(-c3ccc(C(C)C)cc3Br)c2n1 10.1016/s0960-894x(99)00159-6
CHEMBL280449 105838 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 464 3 0 7 5.2 Cc1nc(N2CCOCC2)c2sc(=S)n(-c3ccc(C(C)C)cc3Br)c2n1 10.1016/s0960-894x(99)00159-6
10552595 65775 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 476 9 0 8 3.9 CCN(c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(COC)COC 10.1021/jm980224g
CHEMBL169070 65775 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 476 9 0 8 3.9 CCN(c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(COC)COC 10.1021/jm980224g
44384893 66681 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 382 6 0 7 3.4 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
CHEMBL173074 66681 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 382 6 0 7 3.4 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
11684703 78512 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 4 0 4 5.7 CC[C@@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL196604 78512 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 4 0 4 5.7 CC[C@@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
20780017 71718 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 458 7 0 4 5.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1Br 10.1016/j.bmcl.2005.05.117
CHEMBL182278 71718 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 458 7 0 4 5.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1Br 10.1016/j.bmcl.2005.05.117
44443634 100760 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 7 0 6 4.8 CCc1nc(N(C)[C@@H]2c3ccccc3C[C@@H]2OC)c(CC)nc1Oc1cc(C)ccn1 10.1016/j.bmcl.2007.09.008
CHEMBL248577 100760 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 7 0 6 4.8 CCc1nc(N(C)[C@@H]2c3ccccc3C[C@@H]2OC)c(CC)nc1Oc1cc(C)ccn1 10.1016/j.bmcl.2007.09.008
10641825 127244 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 353 2 0 3 5.1 Cc1ccc2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL354092 127244 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 353 2 0 3 5.1 Cc1ccc2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
53310410 70760 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 10 0 5 4.7 CCc1nc(N(CCOC)CCOC)c(CC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807026 70760 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 10 0 5 4.7 CCc1nc(N(CCOC)CCOC)c(CC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
20780074 74445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 7 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL190745 74445 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 7 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
10643831 64388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 385 10 0 6 4.5 CCCCN(CCOC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
CHEMBL166835 64388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 385 10 0 6 4.5 CCCCN(CCOC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
9866114 72024 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 407 10 0 4 5.6 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(CC)cc(CC)cc2CC)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182752 72024 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 407 10 0 4 5.6 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(CC)cc(CC)cc2CC)c1C 10.1016/j.bmcl.2004.05.072
44392693 73113 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 408 9 0 6 5.2 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(CC)CC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL185055 73113 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 408 9 0 6 5.2 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N(CC)CC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44392753 73429 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 1 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3NC)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL185292 73429 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 1 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3NC)c(C)nn12 10.1016/j.bmcl.2004.05.056
44342015 116994 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 467 8 0 5 6.5 CCCCN(CCc1ccccn1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL323756 116994 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 467 8 0 5 6.5 CCCCN(CCc1ccccn1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9846806 117388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 454 6 1 5 6.4 CCCN(Cc1ccc(O)cc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL325638 117388 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 454 6 1 5 6.4 CCCN(Cc1ccc(O)cc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
46891116 13583 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 454 8 0 5 5.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(OC)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
CHEMBL1083922 13583 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 454 8 0 5 5.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(OC)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
20780266 13658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 6 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CC4CCC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1084235 13658 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 6 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CC4CCC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
21916134 13899 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 436 7 0 4 5.9 C=CCN(CC=C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1085265 13899 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 436 7 0 4 5.9 C=CCN(CC=C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916107 14202 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 7 0 4 6.3 CCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1086594 14202 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 7 0 4 6.3 CCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
11280879 74321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 1 6 5.0 Cc1cc(NC(C)CCC(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
CHEMBL189754 74321 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 1 6 5.0 Cc1cc(NC(C)CCC(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
11306515 77227 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 459 7 0 5 5.7 CCCC(CCC)N1CCc2cn(-c3ccc(S(C)(=O)=O)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL194607 77227 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 459 7 0 5 5.7 CCCC(CCC)N1CCc2cn(-c3ccc(S(C)(=O)=O)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
11166658 140191 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 406 6 0 4 6.2 CCCC(CCC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL370501 140191 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 406 6 0 4 6.2 CCCC(CCC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
9844591 67587 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 412 6 0 6 6.1 CCCN(CC1CC1)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL17619 67587 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 412 6 0 6 6.1 CCCN(CC1CC1)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
44266463 11334 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 443 5 0 3 7.1 CCN(c1nc(C)cc(-c2ccccc2Cl)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10249 11334 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 443 5 0 3 7.1 CCN(c1nc(C)cc(-c2ccccc2Cl)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
44290640 108266 0 None - 1 Human 7.9 pKi = 7.9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)c(OC)c3)c(C)nn12 10.1021/jm990590f
CHEMBL297886 108266 0 None - 1 Human 7.9 pKi = 7.9 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)c(OC)c3)c(C)nn12 10.1021/jm990590f
44266481 12144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 427 6 0 5 5.4 CCN(c1nc(C)cc(-c2ccccc2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL10698 12144 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 427 6 0 5 5.4 CCN(c1nc(C)cc(-c2ccccc2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
122193806 130754 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 490 8 0 4 6.0 CCN(C)c1cc(C)nc2c1N(CCCCF)C(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628854 130754 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 490 8 0 4 6.0 CCN(C)c1cc(C)nc2c1N(CCCCF)C(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL2372939 217099 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)C(CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
9800789 129919 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3cccc(OC)c3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL361242 129919 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3cccc(OC)c3)c3nc(C)cc1c32 10.1021/jm050384+
44384828 66535 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 491 9 0 8 3.4 COCCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL172544 66535 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 491 9 0 8 3.4 COCCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
21916340 14152 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 502 8 0 4 7.5 CCCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1086380 14152 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 502 8 0 4 7.5 CCCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
10616216 110327 1 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 327 7 1 5 4.5 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL308544 110327 1 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 327 7 1 5 4.5 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10616216 110327 1 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 327 7 1 5 4.5 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL308544 110327 1 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 327 7 1 5 4.5 CCCN(CCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
10186078 71358 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 513 8 1 5 8.3 CCCN(Cc1cccs1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181625 71358 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 513 8 1 5 8.3 CCCN(Cc1cccs1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
18672249 71369 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 575 9 1 4 8.9 FC(F)(F)CCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181673 71369 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 575 9 1 4 8.9 FC(F)(F)CCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780053 175728 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 497 6 0 5 6.8 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4CCc4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL438847 175728 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 497 6 0 5 6.8 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4CCc4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
10229290 137198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1ccccn1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL368018 137198 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1ccccn1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44389082 69323 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 500 9 1 5 6.6 CN(C)CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL178246 69323 0 None - 1 Human 4.9 pKi = 4.9 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 500 9 1 5 6.6 CN(C)CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
11340431 80167 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 472 7 1 5 6.5 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2cccc(OCc3ccccc3)c2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL201518 80167 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 472 7 1 5 6.5 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2cccc(OCc3ccccc3)c2)c(C)c1 10.1016/j.bmcl.2005.10.097
11798911 127131 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 479 9 0 7 6.1 CCCCN(CC)c1nc(C)nc2c1nc(-c1ccccc1)n2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL353098 127131 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 479 9 0 7 6.1 CCCCN(CC)c1nc(C)nc2c1nc(-c1ccccc1)n2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
44318119 212679 0 None - 1 Human 6.9 pKi = 6.9 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 341 6 0 4 4.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)n(C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL83934 212679 0 None - 1 Human 6.9 pKi = 6.9 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 341 6 0 4 4.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)n(C)c1=O 10.1016/s0960-894x(03)00483-9
20780073 74059 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 452 7 0 4 6.4 C=CCN(CC=C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL188194 74059 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 452 7 0 4 6.4 C=CCN(CC=C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
10830877 212293 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 338 7 1 4 5.1 CCCN(CC1CC1)c1cc(Nc2c(C)cc(C)cc2C)nc(C)n1 10.1021/jm960149e
CHEMBL80806 212293 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 338 7 1 4 5.1 CCCN(CC1CC1)c1cc(Nc2c(C)cc(C)cc2C)nc(C)n1 10.1021/jm960149e
10830877 212293 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 338 7 1 4 5.1 CCCN(CC1CC1)c1cc(Nc2c(C)cc(C)cc2C)nc(C)n1 10.1021/jm9900117
CHEMBL80806 212293 0 None - 1 Human 5.9 pKi = 5.9 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 338 7 1 4 5.1 CCCN(CC1CC1)c1cc(Nc2c(C)cc(C)cc2C)nc(C)n1 10.1021/jm9900117
10506052 64220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 516 8 0 4 5.9 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(I)cc2Br)n1 10.1021/jm980222w
CHEMBL165531 64220 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 516 8 0 4 5.9 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(I)cc2Br)n1 10.1021/jm980222w
10529311 64302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 496 10 0 5 6.5 CCN(c1nc(C)cc(N(CCOC)Cc2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL166235 64302 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 496 10 0 5 6.5 CCN(c1nc(C)cc(N(CCOC)Cc2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
44392657 71986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3[N+](=O)[O-])c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL182567 71986 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3[N+](=O)[O-])c(C)nn12 10.1016/j.bmcl.2004.05.056
10346761 117380 1 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 524 7 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(I)cc2Cl)c1Cl 10.1016/s0960-894x(00)00661-2
CHEMBL325577 117380 1 None - 1 Rat 7.9 pKi = 7.9 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 524 7 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(I)cc2Cl)c1Cl 10.1016/s0960-894x(00)00661-2
21916292 14274 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 524 7 0 4 6.8 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CC2)CC(F)(F)C(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087166 14274 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 524 7 0 4 6.8 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CC2)CC(F)(F)C(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
11442212 69271 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 446 8 0 5 6.2 CCCN(c1nc(-c2ccc(OC)cc2C)n(C)n1)C(CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL178117 69271 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 446 8 0 5 6.2 CCCN(c1nc(-c2ccc(OC)cc2C)n(C)n1)C(CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
11212115 129105 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 412 9 0 5 5.9 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL359863 129105 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 412 9 0 5 5.9 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
44337106 13025 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 356 8 1 5 3.9 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(CCO)n1 10.1016/s0960-894x(01)00657-6
CHEMBL108158 13025 0 None - 1 Human 7.9 pKi = 7.9 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 356 8 1 5 3.9 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(CCO)n1 10.1016/s0960-894x(01)00657-6
122193726 130744 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 474 6 0 4 5.4 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2C/C=C/CF 10.1016/j.bmcl.2015.10.010
CHEMBL3628745 130744 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 474 6 0 4 5.4 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2C/C=C/CF 10.1016/j.bmcl.2015.10.010
9946605 70777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 353 6 1 4 5.4 CCC(CC)Nc1nc(OC)c(-c2ccc(Cl)cc2Cl)nc1C 10.1021/jm200365y
CHEMBL1807043 70777 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 353 6 1 4 5.4 CCC(CC)Nc1nc(OC)c(-c2ccc(Cl)cc2Cl)nc1C 10.1021/jm200365y
9957428 68053 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 494 9 0 8 4.1 COCCN(CCOC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL17666 68053 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 494 9 0 8 4.1 COCCN(CCOC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
9798798 69926 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 356 4 0 6 3.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL17897 69926 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 356 4 0 6 3.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
44341687 118093 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 378 8 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL326722 118093 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 378 8 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)cccc12 10.1016/s0960-894x(03)00684-x
11475328 132965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 408 8 0 6 4.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OCC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL364938 132965 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 408 8 0 6 4.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OCC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
44341634 17030 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 317 2 0 2 5.5 COc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL116106 17030 1 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 317 2 0 2 5.5 COc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
20780054 175909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 409 3 0 6 4.1 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCOCC4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL440232 175909 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 409 3 0 6 4.1 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCOCC4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
11109264 109336 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 297 5 2 4 3.4 COc1cccc(N/C(=N/Nc2ccccc2C)C(C)=O)c1 10.1021/jm025512y
CHEMBL304072 109336 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 297 5 2 4 3.4 COc1cccc(N/C(=N/Nc2ccccc2C)C(C)=O)c1 10.1021/jm025512y
20780180 73978 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 468 7 0 4 6.8 CCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL187815 73978 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 468 7 0 4 6.8 CCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
11782614 210738 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 335 4 2 3 4.3 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
CHEMBL69374 210738 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 335 4 2 3 4.3 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
44308156 109108 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 420 7 0 6 4.4 CCCN(CCN(C)C)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL303639 109108 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 420 7 0 6 4.4 CCCN(CCN(C)C)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
11245983 82688 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 380 4 1 4 5.2 Cc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL204967 82688 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 380 4 1 4 5.2 Cc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
1799083 210792 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 365 4 2 3 4.3 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccc(Br)cc1 10.1021/jm025512y
CHEMBL69686 210792 3 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 365 4 2 3 4.3 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccc(Br)cc1 10.1021/jm025512y
10594766 109913 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 361 6 1 5 4.9 CCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL307871 109913 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 361 6 1 5 4.9 CCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10594766 109913 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 361 6 1 5 4.9 CCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL307871 109913 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 361 6 1 5 4.9 CCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
22324320 212727 0 None - 1 Human 7.8 pKi = 7.8 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 381 7 0 4 5.2 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2Cl)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL84339 212727 0 None - 1 Human 7.8 pKi = 7.8 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 381 7 0 4 5.2 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2Cl)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
10596113 127364 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 382 7 0 5 5.1 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(OC)cc2Cl)n1 10.1021/jm980222w
CHEMBL354584 127364 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 382 7 0 5 5.1 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(OC)cc2Cl)n1 10.1021/jm980222w
10474043 71351 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 365 7 0 4 4.9 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL181593 71351 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 365 7 0 4 4.9 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
4183319 121527 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL333880 121527 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
44306488 209528 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 9 0 5 5.2 CCCN(c1ncc(C)c(-c2c(C)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL61954 209528 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 9 0 5 5.2 CCCN(c1ncc(C)c(-c2c(C)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
9865575 210176 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL65484 210176 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 397 10 0 6 4.6 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
44308017 109308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 379 7 0 5 5.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(CC)c12 10.1016/s0960-894x(02)00358-x
CHEMBL304059 109308 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 379 7 0 5 5.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(CC)c12 10.1016/s0960-894x(02)00358-x
44305208 107523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 356 6 0 4 5.3 CCCCN(CC)c1cc(C)nc2c(-c3ccccc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL292764 107523 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 356 6 0 4 5.3 CCCCN(CC)c1cc(C)nc2c(-c3ccccc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
20780153 100536 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 449 8 0 5 6.3 CCCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247359 100536 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 449 8 0 5 6.3 CCCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
20780142 151841 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 415 7 0 5 5.5 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
CHEMBL391141 151841 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 415 7 0 5 5.5 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
20780165 154538 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 423 7 0 5 5.9 CCCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL393250 154538 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 423 7 0 5 5.9 CCCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
10132995 194770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 357 8 0 5 4.7 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497301 194770 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 357 8 0 5 4.7 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
11375016 130856 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 478 7 0 6 6.4 CCCN(Cc1ccc2ccccc2c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL363269 130856 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 478 7 0 6 6.4 CCCN(Cc1ccc2ccccc2c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44337304 116660 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 396 7 0 4 5.3 CCCN(c1nc(-c2cc(F)c(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL323437 116660 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 396 7 0 4 5.3 CCCN(c1nc(-c2cc(F)c(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
44387103 68560 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 473 8 1 6 5.7 CCCCC(CC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL177310 68560 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 473 8 1 6 5.7 CCCCC(CC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10717531 65284 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 10 0 9 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
CHEMBL168388 65284 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 10 0 9 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
10812125 65909 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 421 7 0 7 4.2 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980224g
CHEMBL169862 65909 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 421 7 0 7 4.2 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980224g
11656502 77972 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 4 0 4 6.0 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC(C)C 10.1021/jm049085v
CHEMBL195636 77972 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 4 0 4 6.0 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC(C)C 10.1021/jm049085v
11361057 74446 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 382 6 0 7 3.1 CCCC(OC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190757 74446 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 382 6 0 7 3.1 CCCC(OC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
21916165 74005 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 446 8 0 4 6.5 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL187940 74005 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 446 8 0 4 6.5 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
44397642 74332 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 546 8 0 4 7.8 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(C(C)C)cc3Br)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL189809 74332 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 546 8 0 4 7.8 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(C(C)C)cc3Br)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
44347117 23219 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 466 7 0 6 5.0 CCCN(CC1CC1)c1cc(S(C)(=O)=O)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL123306 23219 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 466 7 0 6 5.0 CCCN(CC1CC1)c1cc(S(C)(=O)=O)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
21916109 13478 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 533 8 0 6 7.0 CCCN(Cc1ccc([N+](=O)[O-])cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083612 13478 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 533 8 0 6 7.0 CCCN(Cc1ccc([N+](=O)[O-])cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916289 13648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 474 6 0 4 6.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1084184 13648 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 474 6 0 4 6.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
10502620 126197 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 426 7 0 4 6.4 CCCN(CC1CC1)c1nc(C)nc(N(C)c2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
CHEMBL344805 126197 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 426 7 0 4 6.4 CCCN(CC1CC1)c1nc(C)nc(N(C)c2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
10275456 70151 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 445 7 1 4 7.1 CCCN(CC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL179576 70151 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 445 7 1 4 7.1 CCCN(CC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11429073 69392 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 384 7 0 5 5.1 CCC(c1ccccc1)N(CC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL178346 69392 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 384 7 0 5 5.1 CCC(c1ccccc1)N(CC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
44337446 11972 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 420 8 0 4 5.8 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(CC(F)(F)F)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL106093 11972 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 420 8 0 4 5.8 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(CC(F)(F)F)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
22248956 70770 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 381 8 1 4 6.0 CCOc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807036 70770 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 381 8 1 4 6.0 CCOc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
46881398 14277 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 3 0 5 4.2 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCOCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087173 14277 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 3 0 5 4.2 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCOCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
22249081 70761 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 408 9 0 4 5.4 CCCN(CCN(C)C)c1nc(CC)c(-c2ccc(Cl)cc2Cl)nc1CC 10.1021/jm200365y
CHEMBL1807027 70761 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 408 9 0 4 5.4 CCCN(CCN(C)C)c1nc(CC)c(-c2ccc(Cl)cc2Cl)nc1CC 10.1021/jm200365y
44460260 212117 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1[C@@H](Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL79587 212117 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1[C@@H](Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
44443575 100761 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 414 8 2 4 6.9 CCc1nc(NC(CC)CC)c(CC)nc1Nc1c(Cl)cc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
CHEMBL248585 100761 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 414 8 2 4 6.9 CCc1nc(NC(CC)CC)c(CC)nc1Nc1c(Cl)cc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
20780024 71999 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 472 8 0 4 5.7 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2005.05.117
CHEMBL182624 71999 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 472 8 0 4 5.7 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2005.05.117
11454794 82384 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 497 7 1 6 6.3 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccc(C#N)cc3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL204706 82384 0 None - 1 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 497 7 1 6 6.3 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccc(C#N)cc3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
11704536 78540 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 424 5 0 6 4.9 CC[C@H]1Cn2nc(-c3ccc(C(=O)OC)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL196682 78540 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 424 5 0 6 4.9 CC[C@H]1Cn2nc(-c3ccc(C(=O)OC)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
9843989 78694 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 2 0 4 5.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2C1CCCCC1 10.1021/jm049085v
CHEMBL197204 78694 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 2 0 4 5.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2C1CCCCC1 10.1021/jm049085v
11524923 131584 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 436 4 0 4 6.5 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1Cc1ccccc1 10.1021/jm049085v
CHEMBL364261 131584 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 436 4 0 4 6.5 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1Cc1ccccc1 10.1021/jm049085v
44352386 25734 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 451 8 1 4 7.1 CCCN(Cc1sc(Nc2c(C)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL128709 25734 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 451 8 1 4 7.1 CCCN(Cc1sc(Nc2c(C)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44341635 16773 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 333 2 0 2 6.2 CSc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL114914 16773 1 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 333 2 0 2 6.2 CSc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
46891210 13410 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083320 13410 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)CC4CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780253 13721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 6 0 4 6.3 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CCC1 10.1016/j.bmcl.2010.04.094
CHEMBL1084511 13721 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 6 0 4 6.3 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CCC1 10.1016/j.bmcl.2010.04.094
44307870 210322 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 5 1 5 5.2 CCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66492 210322 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 5 1 5 5.2 CCC(CC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44307654 210346 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 351 6 1 4 4.8 CCCN(CCC)c1[nH]c(C)nc2c(-c3c(C)cc(C)cc3C)nnc1-2 10.1016/s0960-894x(02)00358-x
CHEMBL66719 210346 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 351 6 1 4 4.8 CCCN(CCC)c1[nH]c(C)nc2c(-c3c(C)cc(C)cc3C)nnc1-2 10.1016/s0960-894x(02)00358-x
21916343 100155 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 7 0 5 6.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
CHEMBL245671 100155 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 7 0 5 6.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
44587491 194898 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 371 9 0 5 5.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OCC 10.1016/j.bmcl.2008.07.063
CHEMBL498318 194898 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 371 9 0 5 5.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OCC 10.1016/j.bmcl.2008.07.063
11235868 141962 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 397 5 0 4 5.4 CCC(COC)N1CCc2cn(-c3c(C)cc(Cl)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL372009 141962 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 397 5 0 4 5.4 CCC(COC)N1CCc2cn(-c3c(C)cc(Cl)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
44341452 16287 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 9 0 4 7.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C(C)C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL112151 16287 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 9 0 4 7.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C(C)C)c12 10.1016/s0960-894x(03)00621-8
9843717 73552 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 396 6 0 6 4.7 CCCN(CC1CC1)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL18590 73552 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 396 6 0 6 4.7 CCCN(CC1CC1)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
11166649 113202 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 442 10 0 6 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2cc(OC)c(OC)cc2Cl)n(C)n1 10.1021/jm049339c
CHEMBL3085418 113202 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 442 10 0 6 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2cc(OC)c(OC)cc2Cl)n(C)n1 10.1021/jm049339c
CHEMBL3139572 113202 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 442 10 0 6 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2cc(OC)c(OC)cc2Cl)n(C)n1 10.1021/jm049339c
122193722 130741 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 416 4 1 4 4.8 CCN(C)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628742 130741 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 416 4 1 4 4.8 CCN(C)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
135444727 127002 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.4 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL352154 127002 0 None -3 2 Rat 6.8 pKi = 6.8 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.4 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
21916299 13178 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 460 5 0 4 6.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082339 13178 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 460 5 0 4 6.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
21916288 13471 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 546 6 0 4 7.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(Cc4ccc(F)cc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083593 13471 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 546 6 0 4 7.4 Cc1cc(C)c(-n2c(Cl)cn3c(CN(Cc4ccc(F)cc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
10276375 70050 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 8 1 4 7.5 CCCN(CCC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL179225 70050 0 None - 1 Human 6.8 pKi = 6.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 8 1 4 7.5 CCCN(CCC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780156 130453 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 544 8 0 4 8.1 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL362124 130453 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 544 8 0 4 8.1 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
46891009 13207 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.1 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCCC4C)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082442 13207 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.1 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCCC4C)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
10273816 26150 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 421 7 1 5 5.3 CCN(CCOC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL129196 26150 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 421 7 1 5 5.3 CCN(CCOC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
44587372 194768 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 387 10 1 6 4.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OCCO 10.1016/j.bmcl.2008.07.063
CHEMBL497286 194768 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 387 10 1 6 4.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OCCO 10.1016/j.bmcl.2008.07.063
44462061 113368 0 None - 1 Human 5.8 pKi = 5.8 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 425 8 0 5 5.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CC(F)(F)F)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL314267 113368 0 None - 1 Human 5.8 pKi = 5.8 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 425 8 0 5 5.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CC(F)(F)F)c1=O 10.1016/s0960-894x(03)00483-9
44446732 101644 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 334 5 1 3 5.7 CCCNc1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253915 101644 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 334 5 1 3 5.7 CCCNc1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
22249005 70766 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 355 6 1 3 5.8 CCc1nc(NC(CC)CC)c(F)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807032 70766 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 355 6 1 3 5.8 CCc1nc(NC(CC)CC)c(F)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
44446717 162210 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1c(C)nc(-c2ccccc2Cl)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL403745 162210 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1c(C)nc(-c2ccccc2Cl)c2ccccc12 10.1016/j.bmcl.2007.12.050
10787219 211950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 401 5 2 5 5.5 Cc1cc(C)c(Nc2nc(C)nc(NCc3ccc(C(F)(F)F)cc3)n2)c(C)c1 10.1021/jm960148m
CHEMBL78271 211950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 401 5 2 5 5.5 Cc1cc(C)c(Nc2nc(C)nc(NCc3ccc(C(F)(F)F)cc3)n2)c(C)c1 10.1021/jm960148m
10787219 211950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 401 5 2 5 5.5 Cc1cc(C)c(Nc2nc(C)nc(NCc3ccc(C(F)(F)F)cc3)n2)c(C)c1 10.1021/jm9900117
CHEMBL78271 211950 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 401 5 2 5 5.5 Cc1cc(C)c(Nc2nc(C)nc(NCc3ccc(C(F)(F)F)cc3)n2)c(C)c1 10.1021/jm9900117
9954503 74326 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 432 6 0 5 5.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL189780 74326 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 432 6 0 5 5.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
10669045 64914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 6 4.1 CCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
CHEMBL167853 64914 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 6 4.1 CCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
10647940 127501 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 466 8 0 4 6.9 CCN(Cc1ccccc1)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL354791 127501 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 466 8 0 4 6.9 CCN(Cc1ccccc1)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
44392709 136674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 420 7 0 6 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N4CCCCC4)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL367583 136674 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 420 7 0 6 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N4CCCCC4)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44308187 210831 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 375 3 1 5 5.0 Cc1nc(NC2CCCC2)c2nn(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(02)00358-x
CHEMBL69968 210831 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 375 3 1 5 5.0 Cc1nc(NC2CCCC2)c2nn(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(02)00358-x
20780144 157768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 443 8 0 5 6.2 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
CHEMBL395833 157768 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 443 8 0 5 6.2 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
11454873 147533 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 502 8 1 6 6.5 COc1ccccc1COc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL381824 147533 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 502 8 1 6 6.5 COc1ccccc1COc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
44446724 101582 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 414 9 0 4 6.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253493 101582 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 414 9 0 4 6.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
11485413 172934 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 5 1 6 4.2 Cc1cc(NC(C)C(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
CHEMBL426260 172934 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 5 1 6 4.2 Cc1cc(NC(C)C(C)C)n2nc(C)c(-c3cnc(N(C)C)cc3C)c2n1 10.1021/jm040058e
22249061 70754 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 359 9 1 7 3.7 CCc1nc(-c2cnc(OC)nc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807020 70754 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 359 9 1 7 3.7 CCc1nc(-c2cnc(OC)nc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
44384750 138579 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 395 7 1 6 4.7 CCCCC(CC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
CHEMBL369371 138579 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 395 7 1 6 4.7 CCCCC(CC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
44266437 215187 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.5 CCN(c1nc(C)cc(-c2cccc(C(F)(F)F)c2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL9975 215187 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.5 CCN(c1nc(C)cc(-c2cccc(C(F)(F)F)c2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
11429605 131315 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 404 4 0 5 4.5 CCC(CC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL364037 131315 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 404 4 0 5 4.5 CCC(CC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
44341983 16311 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 362 5 1 4 5.5 CCCCNc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112266 16311 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 362 5 1 4 5.5 CCCCNc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
21916286 13475 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 7 0 4 7.1 CCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083608 13475 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 7 0 4 7.1 CCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
46891057 14055 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 426 3 0 5 4.6 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCOCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086016 14055 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 426 3 0 5 4.6 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCOCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780039 13462 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 444 7 0 4 5.8 CCCN(CCc1ccccc1)C(=O)c1c(C)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1083513 13462 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 444 7 0 4 5.8 CCCN(CCc1ccccc1)C(=O)c1c(C)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
10785716 35064 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 375 8 1 5 5.1 CCc1cccc(CC)c1Nc1nc(C)nc(N(CC)Cc2ccccc2)n1 10.1021/jm960148m
CHEMBL137434 35064 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 375 8 1 5 5.1 CCc1cccc(CC)c1Nc1nc(C)nc(N(CC)Cc2ccccc2)n1 10.1021/jm960148m
44446737 162387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 459 10 0 4 6.9 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL404559 162387 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 459 10 0 4 6.9 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
44443658 161698 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 489 9 2 6 6.1 CCc1nc(N[C@@H]2c3ccccc3C[C@@H]2OCCF)c(CC)nc1Nc1ncc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
CHEMBL400952 161698 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 489 9 2 6 6.1 CCc1nc(N[C@@H]2c3ccccc3C[C@@H]2OCCF)c(CC)nc1Nc1ncc(Cl)cc1Cl 10.1016/j.bmcl.2007.09.008
44307479 210334 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 389 3 1 5 5.4 Cc1nc(NC2CCCCC2)c2nn(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(02)00358-x
CHEMBL66631 210334 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 389 3 1 5 5.4 Cc1nc(NC2CCCCC2)c2nn(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(02)00358-x
44407869 81892 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 4 1 4 5.5 Cc1ccc(S(=O)(=O)c2c(C)cc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL203609 81892 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 4 1 4 5.5 Cc1ccc(S(=O)(=O)c2c(C)cc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
44379386 127531 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 465 11 0 7 4.3 CCN(c1nc(C)nc(N(CCOC)CCOC)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL355055 127531 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 465 11 0 7 4.3 CCN(c1nc(C)nc(N(CCOC)CCOC)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
44341823 16778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 434 9 0 5 5.9 CCCCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL114928 16778 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 434 9 0 5 5.9 CCCCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
20780123 202391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 451 9 0 5 6.7 CCCCN(CCCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL556060 202391 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 451 9 0 5 6.7 CCCCN(CCCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44379486 126810 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm049737f
CHEMBL350356 126810 0 None - 1 Human 7.8 pKi = 7.8 Binding
Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1Inhibition of [125I]ovine-CRF binding to corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm049737f
18691318 103935 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 423 5 0 3 6.8 CCN(c1nc(C)cc(-c2ccccc2C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL268043 103935 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 423 5 0 3 6.8 CCN(c1nc(C)cc(-c2ccccc2C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
135958362 64940 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 482 2 4 7 3.7 N[C@@H]1CCCC[C@H]1NC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@H]1CCCC[C@@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL168162 64940 0 None -2 2 Rat 6.8 pKi = 6.8 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 482 2 4 7 3.7 N[C@@H]1CCCC[C@H]1NC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@H]1CCCC[C@@H]1N2 10.1016/s0960-894x(99)00075-x
44392788 130529 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 387 6 0 4 5.8 CCCN(c1ccccc1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL362224 130529 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 387 6 0 4 5.8 CCCN(c1ccccc1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
44341612 117451 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 10 0 4 7.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CCC)c12 10.1016/s0960-894x(03)00621-8
CHEMBL325960 117451 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 10 0 4 7.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CCC)c12 10.1016/s0960-894x(03)00621-8
20779996 13362 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 450 5 0 5 5.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)Cc4ccco4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083101 13362 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 450 5 0 5 5.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)Cc4ccco4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
122193721 130740 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 402 3 1 4 4.4 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2 10.1016/j.bmcl.2015.10.010
CHEMBL3628741 130740 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 402 3 1 4 4.4 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2 10.1016/j.bmcl.2015.10.010
10204577 128805 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 454 5 1 5 6.7 CCc1nccn1Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL359494 128805 0 None - 1 Human 5.8 pKi = 5.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 454 5 1 5 6.7 CCc1nccn1Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44389071 70128 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 426 4 1 5 6.1 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1Cn1ccnc1 10.1016/j.bmcl.2004.10.055
CHEMBL179480 70128 0 None - 1 Human 4.8 pKi = 4.8 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 426 4 1 5 6.1 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1Cn1ccnc1 10.1016/j.bmcl.2004.10.055
11141163 170384 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1ccc(Cl)cc1)NNc1ccccc1C 10.1021/jm025512y
CHEMBL420361 170384 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1ccc(Cl)cc1)NNc1ccccc1C 10.1021/jm025512y
10663467 64283 1 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 319 3 0 3 4.2 CCc1ccc(N(C)c2nc(C)cc(C)n2)c(Br)c1 10.1021/jm980222w
CHEMBL166102 64283 1 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 319 3 0 3 4.2 CCc1ccc(N(C)c2nc(C)cc(C)n2)c(Br)c1 10.1021/jm980222w
44379486 126810 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL350356 126810 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
44392644 129799 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 355 6 0 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ncc(F)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL360905 129799 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 355 6 0 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ncc(F)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44306220 107646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 381 9 0 5 4.9 CCCN(c1ncc(C)c(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL293627 107646 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 381 9 0 5 4.9 CCCN(c1ncc(C)c(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
46881397 14275 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 432 6 0 4 5.2 C=CCN(CC=C)C(=O)c1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1087167 14275 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 432 6 0 4 5.2 C=CCN(CC=C)C(=O)c1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
10111096 70759 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 391 8 0 3 6.2 CCCN(CC1CC1)c1nc(CC)c(-c2ccc(Cl)cc2Cl)nc1CC 10.1021/jm200365y
CHEMBL1807025 70759 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 391 8 0 3 6.2 CCCN(CC1CC1)c1nc(CC)c(-c2ccc(Cl)cc2Cl)nc1CC 10.1021/jm200365y
10694719 65829 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 446 6 1 8 3.8 CCC(Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(=O)OC 10.1021/jm980224g
CHEMBL169460 65829 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 446 6 1 8 3.8 CCC(Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(=O)OC 10.1021/jm980224g
11568262 77060 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 434 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL194295 77060 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 434 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11713460 142350 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CCC1 10.1021/jm049085v
CHEMBL372905 142350 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CCC1 10.1021/jm049085v
44462060 212684 0 None - 1 Human 6.7 pKi = 6.7 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 9 0 5 4.9 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CCC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL83970 212684 0 None - 1 Human 6.7 pKi = 6.7 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 9 0 5 4.9 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CCC)c1=O 10.1016/s0960-894x(03)00483-9
11441545 74353 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 420 5 0 6 4.1 CCCC(OC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190037 74353 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 420 5 0 6 4.1 CCCC(OC)N1CCn2c(=O)n(-c3ccc(C(F)(F)F)cc3)c3nc(C)cc1c32 10.1021/jm050384+
21916311 14072 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 500 5 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCC4Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086061 14072 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 500 5 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCC4Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11188091 175202 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 377 7 0 4 5.7 CCCC(CCC)N1CCc2cn(-c3cccc(OC)c3)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL434910 175202 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 377 7 0 4 5.7 CCCC(CCC)N1CCc2cn(-c3cccc(OC)c3)c3nc(C)cc1c23 10.1021/jm050070m
44392777 72258 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 401 10 1 7 3.5 CCCN(CC1CC1)c1cc(C(O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL183037 72258 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 401 10 1 7 3.5 CCCN(CC1CC1)c1cc(C(O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
44392750 132296 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 415 10 1 7 3.7 CCCN(CC1CC1)c1cc(C(C)(O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL364640 132296 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 415 10 1 7 3.7 CCCN(CC1CC1)c1cc(C(C)(O)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
46890889 13369 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4cccnc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083119 13369 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4cccnc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
46890950 14071 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 556 8 0 4 7.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCc4ccccc4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086059 14071 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 556 8 0 4 7.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCc4ccccc4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11223591 75387 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 409 7 0 3 6.7 CCCC(CCC)N1CCc2cn(Cc3ccc(Cl)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL191780 75387 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 409 7 0 3 6.7 CCCC(CCC)N1CCc2cn(Cc3ccc(Cl)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
20780284 70277 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 8 0 4 5.1 CCCN(Cc1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2005.05.117
CHEMBL179985 70277 0 None - 1 Human 4.7 pKi = 4.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 8 0 4 5.1 CCCN(Cc1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2005.05.117
44389113 71386 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 474 8 1 5 6.2 CCN(CCN(C)C)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181732 71386 0 None - 1 Human 4.7 pKi = 4.7 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 474 8 1 5 6.2 CCN(CCN(C)C)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44307893 210254 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 335 3 1 5 4.1 CCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66052 210254 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 335 3 1 5 4.1 CCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
10501205 65860 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 400 3 0 6 4.0 Cc1nc(N2CCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
CHEMBL169629 65860 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 400 3 0 6 4.0 Cc1nc(N2CCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
10741433 127146 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 6 1 7 4.2 COCC(C)(C)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL353238 127146 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 6 1 7 4.2 COCC(C)(C)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11078292 174989 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 339 4 2 3 4.1 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
CHEMBL433505 174989 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 339 4 2 3 4.1 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
11474959 82073 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 1 5 4.9 COc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL203744 82073 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 1 5 4.9 COc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
10028059 109663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to inhibit [125I]CRH binding to human Corticotropin releasing factor receptor 1Ability to inhibit [125I]CRH binding to human Corticotropin releasing factor receptor 1
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1Br 10.1021/jm9900117
CHEMBL305900 109663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Ability to inhibit [125I]CRH binding to human Corticotropin releasing factor receptor 1Ability to inhibit [125I]CRH binding to human Corticotropin releasing factor receptor 1
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1Br 10.1021/jm9900117
CHEMBL2372950 217100 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CCCC)NC(=O)[C@H](CCCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(C)=O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N1)C(=O)CN[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
9843598 74550 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190845 74550 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
10835052 64864 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 403 7 0 3 6.7 CCC(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL167407 64864 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 403 7 0 3 6.7 CCC(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL263451 217351 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H](N)Cc2ccccc2)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](Cc2c[nH]cn2)C(=O)N1)[C@@H](C)CC)C(N)=O 10.1021/jm990590f
10344587 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2013.02.009
CHEMBL1762817 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2013.02.009
CHEMBL430892 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRF1 receptor (unknown origin)Binding affinity to CRF1 receptor (unknown origin)
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2013.02.009
10344587 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL1762817 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
CHEMBL430892 174623 0 None -1 2 Human 8.7 pKi = 8.7 Binding
Binding affinity to CRFR1 by autoradiographyBinding affinity to CRFR1 by autoradiography
ChEMBL 467 8 0 7 3.9 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Br)cc3Cl)c(C)nn12 10.1016/j.bmcl.2012.08.112
44341832 16190 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL111665 16190 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
44341832 16190 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL111665 16190 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44307738 107590 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
CHEMBL293228 107590 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
44307491 109069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
CHEMBL303380 109069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
176157 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
3512 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
CHEMBL45281 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
44307738 107590 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL293228 107590 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44307491 109069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL303380 109069 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
3533 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2008.07.063
5282340 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2008.07.063
CHEMBL291657 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2008.07.063
42618174 200113 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 8 1 8 2.8 COCC(COC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2008.07.063
CHEMBL524616 200113 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 8 1 8 2.8 COCC(COC)Nc1nc(C)nc2c(-c3ccc(OC)cc3C)c(C)nn12 10.1016/j.bmcl.2008.07.063
44587375 200179 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 393 9 0 6 4.8 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL525716 200179 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 393 9 0 6 4.8 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
10028059 109663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1Br 10.1021/jm960149e
CHEMBL305900 109663 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1Br 10.1021/jm960149e
176157 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm049339c
3512 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm049339c
CHEMBL45281 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1021/jm049339c
44341581 16763 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 432 9 0 4 7.1 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
CHEMBL114861 16763 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 432 9 0 4 7.1 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
44341877 117242 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 412 8 0 4 6.6 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL324728 117242 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 412 8 0 4 6.6 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
127033261 145252 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3992 134 55 49 -7.3 CCCCCCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
CHEMBL3774713 145252 0 None 1 2 Human 8.7 pKi = 8.7 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3992 134 55 49 -7.3 CCCCCCCCCCCCCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(CCCC)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)NC(C)(C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NC(CCCC)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)NC(=O)C(C)(C)NC(=O)[C@H](C)NC1=O)C(C)C)[C@@H](C)O 10.1021/acs.jmedchem.5b00926
10739593 65769 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 397 8 0 6 5.6 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
CHEMBL169010 65769 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 397 8 0 6 5.6 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
44342074 16712 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 372 6 0 2 6.8 CCCN(CC1CC1)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL114596 16712 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 372 6 0 2 6.8 CCCN(CC1CC1)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
22249054 70781 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 8 1 5 5.3 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(OC)cc1C(F)(F)F 10.1021/jm200365y
CHEMBL1807051 70781 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 8 1 5 5.3 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(OC)cc1C(F)(F)F 10.1021/jm200365y
11291949 134287 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
CHEMBL366155 134287 0 None - 1 Human 8.7 pKi = 8.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
44375151 63432 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 390 6 0 4 5.9 CCCN(CC1CC1)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL164206 63432 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 390 6 0 4 5.9 CCCN(CC1CC1)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
9801874 109749 1 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 412 7 1 4 6.4 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
CHEMBL306482 109749 1 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 412 7 1 4 6.4 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
9801874 109749 1 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 412 7 1 4 6.4 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm9900117
CHEMBL306482 109749 1 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 412 7 1 4 6.4 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm9900117
11247393 73587 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1ccc(C)cc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL186033 73587 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1ccc(C)cc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44347137 21707 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 394 8 0 6 4.7 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL120823 21707 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 394 8 0 6 4.7 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
44347202 120291 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 364 7 0 5 4.6 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL332101 120291 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 364 7 0 5 4.6 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
9950788 117293 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 360 6 0 2 6.8 CCCCN(CC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL325047 117293 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 360 6 0 2 6.8 CCCCN(CC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
10095518 11151 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 454 6 0 5 6.4 CCN(c1nc(C)cc(-c2ccccc2[N+](=O)[O-])n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10125 11151 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 454 6 0 5 6.4 CCN(c1nc(C)cc(-c2ccccc2[N+](=O)[O-])n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10027220 73639 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 458 7 1 4 6.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL186252 73639 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 458 7 1 4 6.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
122193720 130739 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 508 6 0 4 5.7 CCCCN(CC)c1cc(C)nc2c1N(C)C(=O)CN2c1ccc(Br)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628740 130739 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 508 6 0 4 5.7 CCCCN(CC)c1cc(C)nc2c1N(C)C(=O)CN2c1ccc(Br)cc1Br 10.1016/j.bmcl.2015.10.010
11430299 73506 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1cccc(C)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL185705 73506 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1cccc(C)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
11224120 130079 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1ccccc1C)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL361509 130079 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 6 0 6 5.1 CCN(Cc1ccccc1C)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44341874 16690 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 412 6 0 2 7.5 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
CHEMBL114422 16690 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 412 6 0 2 7.5 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
177990 7214 23 None 1 2 Rat 8.6 pKi = 8.6 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/s0960-894x(00)00071-8
3489 7214 23 None 1 2 Rat 8.6 pKi = 8.6 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/s0960-894x(00)00071-8
CHEMBL296641 7214 23 None 1 2 Rat 8.6 pKi = 8.6 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1016/s0960-894x(00)00071-8
15490822 105042 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 481 5 0 4 7.1 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(SC)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL274578 105042 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 481 5 0 4 7.1 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(SC)cc1Br 10.1016/s0960-894x(99)00132-8
90231885 130729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 444 7 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1CC 10.1016/j.bmcl.2015.10.010
CHEMBL3628729 130729 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 444 7 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1CC 10.1016/j.bmcl.2015.10.010
90231897 130730 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 450 6 1 4 5.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628730 130730 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 450 6 1 4 5.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Br 10.1016/j.bmcl.2015.10.010
22249128 70789 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 1 5 5.6 CCc1nc(-c2ccc(OC(F)F)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807059 70789 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 399 9 1 5 5.6 CCc1nc(-c2ccc(OC(F)F)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
10787254 211664 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 400 7 1 4 6.4 CCCN(CCC)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
CHEMBL75859 211664 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 400 7 1 4 6.4 CCCN(CCC)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm960149e
10787254 211664 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 400 7 1 4 6.4 CCCN(CCC)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm9900117
CHEMBL75859 211664 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 400 7 1 4 6.4 CCCN(CCC)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1C 10.1021/jm9900117
11465828 73536 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 482 6 0 6 6.1 CCN(Cc1ccc(Cl)c(Cl)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL185858 73536 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 482 6 0 6 6.1 CCN(Cc1ccc(Cl)c(Cl)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
177990 7214 23 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm049085v
3489 7214 23 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm049085v
CHEMBL296641 7214 23 None -1 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm049085v
44347046 121323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.056
CHEMBL333713 121323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.056
44347046 121323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.019
CHEMBL333713 121323 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 377 6 0 3 6.5 CCCCN(CC)c1cc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2004.05.019
3520 10041 54 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
9821250 10041 54 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
CHEMBL309138 10041 54 None 1 2 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
11773421 72862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCCN(CC)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL183845 72862 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCCN(CC)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
11326815 74335 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 392 7 0 6 4.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL189821 74335 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 392 7 0 6 4.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovineBinding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovine
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovineBinding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovine
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovineBinding affinity against [125I]-Try0-o-Corticotropin-releasing Factor to Corticotropin releasing hormone receptor 1 from ovine
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm960861b
176157 9515 28 None 9 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2004.05.072
3512 9515 28 None 9 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2004.05.072
CHEMBL45281 9515 28 None 9 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2004.05.072
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00132-8
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00132-8
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(99)00132-8
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
90231888 130731 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 450 6 1 4 5.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1Cl 10.1016/j.bmcl.2015.10.010
CHEMBL3628731 130731 0 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 450 6 1 4 5.5 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1Cl 10.1016/j.bmcl.2015.10.010
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(02)00358-x
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(02)00358-x
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(02)00358-x
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.12.050
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.12.050
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2007.12.050
11306178 85101 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
11306179 85101 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL2094063 85101 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL2109725 85101 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
3495 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
binding affinity for human CRF1 receptor in IMR32 neuroblastoma cellsbinding affinity for human CRF1 receptor in IMR32 neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm990590f
5311055 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
binding affinity for human CRF1 receptor in IMR32 neuroblastoma cellsbinding affinity for human CRF1 receptor in IMR32 neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm990590f
CHEMBL9946 7958 28 None - 1 Human 8.6 pKi = 8.6 Binding
binding affinity for human CRF1 receptor in IMR32 neuroblastoma cellsbinding affinity for human CRF1 receptor in IMR32 neuroblastoma cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1021/jm990590f
10788803 64351 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 1 6 5.4 CCCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL166669 64351 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 1 6 5.4 CCCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341879 16658 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 398 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(C)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL114273 16658 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 398 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(C)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44290322 107947 0 None - 1 Human 8.6 pKi = 8.6 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm990590f
CHEMBL295563 107947 0 None - 1 Human 8.6 pKi = 8.6 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 382 8 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm990590f
10646985 64601 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 0 5 6.4 CCCCC(CC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL167017 64601 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 0 5 6.4 CCCCC(CC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11282181 74125 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 442 8 0 6 5.6 CCCCN(Cc1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL188566 74125 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 442 8 0 6 5.6 CCCCN(Cc1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
9802053 130972 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 416 6 0 4 6.4 CCCC(CCC)N1CCc2nn(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL363414 130972 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 416 6 0 4 6.4 CCCC(CCC)N1CCc2nn(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
176157 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2003.08.055
3512 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL45281 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2003.08.055
11326483 74553 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 380 5 0 6 3.8 CCC(CC)N1CCn2c(=O)n(-c3ccc(OC)cc3C)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190881 74553 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 380 5 0 6 3.8 CCC(CC)N1CCn2c(=O)n(-c3ccc(OC)cc3C)c3nc(C)cc1c32 10.1021/jm050384+
21916279 172582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 414 7 0 4 6.1 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL424812 172582 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 414 7 0 4 6.1 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
10810752 64273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 396 7 0 6 4.3 CCN(CC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL165991 64273 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 396 7 0 6 4.3 CCN(CC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
10710543 65280 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 316 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1SC 10.1021/jm980222w
CHEMBL168360 65280 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 316 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1SC 10.1021/jm980222w
176157 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
3512 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
CHEMBL45281 9515 28 None 9 2 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/j.bmcl.2005.05.117
44307747 210364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3c(Cl)cccc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66831 210364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1nc(C)nc2c(-c3c(Cl)cccc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
20780178 100574 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 6 0 5 5.9 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
CHEMBL247558 100574 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 6 0 5 5.9 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
11153216 132612 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)cnn12 10.1021/jm040058e
CHEMBL364828 132612 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)cnn12 10.1021/jm040058e
10504455 65498 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 466 6 0 6 4.7 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
CHEMBL168531 65498 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 466 6 0 6 4.7 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
15490823 105225 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 513 5 0 5 5.8 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(S(C)(=O)=O)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL275738 105225 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 513 5 0 5 5.8 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(S(C)(=O)=O)cc1Br 10.1016/s0960-894x(99)00132-8
10500190 65561 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 383 8 0 7 3.1 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL168788 65561 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 383 8 0 7 3.1 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
10736859 127109 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 354 6 0 7 2.9 CCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL352916 127109 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 354 6 0 7 2.9 CCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
136216702 85396 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.7 NCCNC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@H]1CCCC[C@@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL2112326 85396 0 None -2 2 Rat 6.7 pKi = 6.7 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.7 NCCNC(=O)c1c2c(c3c4c(ncnc14)-c1ccccc1C3=O)N[C@H]1CCCC[C@@H]1N2 10.1016/s0960-894x(99)00075-x
11222924 74375 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 386 5 0 6 3.7 CCCC(OC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190262 74375 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 386 5 0 6 3.7 CCCC(OC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
44392772 129757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 351 7 0 4 4.6 CCCN(CC1CC1)c1cc(C(=O)c2c(C)cc(C)cc2C)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL360845 129757 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 351 7 0 4 4.6 CCCN(CC1CC1)c1cc(C(=O)c2c(C)cc(C)cc2C)nc(C)n1 10.1016/j.bmcl.2004.05.072
44305974 109622 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 425 9 0 7 5.1 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2ccsc2)CC1 10.1016/j.bmcl.2004.02.053
CHEMBL305583 109622 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 425 9 0 7 5.1 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2ccsc2)CC1 10.1016/j.bmcl.2004.02.053
10761294 127173 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 364 2 0 5 4.1 Cc1cc(C)c(-n2c(C)c(C)c3c(N4CCOCC4)nc(C)nc32)c(C)c1 10.1021/jm980224g
CHEMBL353425 127173 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 364 2 0 5 4.1 Cc1cc(C)c(-n2c(C)c(C)c3c(N4CCOCC4)nc(C)nc32)c(C)c1 10.1021/jm980224g
9980256 101192 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 7 1 7 4.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC(C)=O 10.1016/j.bmcl.2007.09.008
CHEMBL251034 101192 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 7 1 7 4.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC(C)=O 10.1016/j.bmcl.2007.09.008
10551475 127556 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 9 0 8 3.2 COCCN(CCOC)c1ncnc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL355394 127556 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 9 0 8 3.2 COCCN(CCOC)c1ncnc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44317962 212406 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 462 7 1 3 6.5 O=C(CCc1ccncc1)C(Nc1ccc(Cl)cc1Cl)c1ccccc1Br 10.1021/jm049974i
CHEMBL81726 212406 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 462 7 1 3 6.5 O=C(CCc1ccncc1)C(Nc1ccc(Cl)cc1Cl)c1ccccc1Br 10.1021/jm049974i
135884427 63949 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 374 3 4 7 1.1 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=NCCN2 10.1016/s0960-894x(99)00075-x
CHEMBL164829 63949 0 None -3 2 Rat 5.7 pKi = 5.7 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 374 3 4 7 1.1 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=NCCN2 10.1016/s0960-894x(99)00075-x
44318122 212607 0 None - 1 Human 7.7 pKi = 7.7 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 371 8 0 5 4.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL83385 212607 0 None - 1 Human 7.7 pKi = 7.7 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 371 8 0 5 4.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
44352382 123506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 475 8 1 4 6.9 CCCN(Cc1sc(Nc2c(C)cc(C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL337409 123506 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 475 8 1 4 6.9 CCCN(Cc1sc(Nc2c(C)cc(C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
21916208 74113 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 428 8 0 4 6.4 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL188523 74113 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 428 8 0 4 6.4 CCCN(Cc1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
10717814 127125 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 436 10 0 10 2.3 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL353050 127125 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 436 10 0 10 2.3 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
10254503 16504 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Br)cc2Cl)c1Cl 10.1016/s0960-894x(00)00661-2
CHEMBL113333 16504 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 476 7 1 4 6.9 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Br)cc2Cl)c1Cl 10.1016/s0960-894x(00)00661-2
21916260 13363 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 502 8 0 4 7.2 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083102 13363 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 502 8 0 4 7.2 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916302 14436 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 448 7 0 4 6.4 CCCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CCC1 10.1016/j.bmcl.2010.01.127
CHEMBL1088478 14436 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 448 7 0 4 6.4 CCCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CCC1 10.1016/j.bmcl.2010.01.127
44446720 101554 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 366 6 0 2 6.8 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253287 101554 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 366 6 0 2 6.8 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
11393576 130572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 337 6 0 5 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C)nc3)c(C)nn12 10.1021/jm040058e
CHEMBL362305 130572 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 337 6 0 5 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C)nc3)c(C)nn12 10.1021/jm040058e
10552046 127569 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 8 0 8 3.5 COCC(COC)N(C)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL355494 127569 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 8 0 8 3.5 COCC(COC)N(C)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
122193727 130745 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 476 7 0 4 5.6 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2CCCCF 10.1016/j.bmcl.2015.10.010
CHEMBL3628746 130745 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 476 7 0 4 5.6 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2CCCCF 10.1016/j.bmcl.2015.10.010
11795486 127191 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 403 6 1 6 4.1 COCCNc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL353662 127191 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 403 6 1 6 4.1 COCCNc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44315264 211869 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 361 6 1 5 4.5 Cc1cc(C)c(Nc2nc(C)nc(N(C)CCc3ccccc3)n2)c(C)c1 10.1021/jm960148m
CHEMBL77527 211869 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 361 6 1 5 4.5 Cc1cc(C)c(Nc2nc(C)nc(N(C)CCc3ccccc3)n2)c(C)c1 10.1021/jm960148m
44315264 211869 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 361 6 1 5 4.5 Cc1cc(C)c(Nc2nc(C)nc(N(C)CCc3ccccc3)n2)c(C)c1 10.1021/jm9900117
CHEMBL77527 211869 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 361 6 1 5 4.5 Cc1cc(C)c(Nc2nc(C)nc(N(C)CCc3ccccc3)n2)c(C)c1 10.1021/jm9900117
44443597 100766 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 348 6 1 5 5.2 CCC(Nc1nc(C)c(Oc2cc(C)ccn2)nc1C)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL248623 100766 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 348 6 1 5 5.2 CCC(Nc1nc(C)c(Oc2cc(C)ccn2)nc1C)c1ccccc1 10.1016/j.bmcl.2007.09.008
44443649 161186 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 430 8 1 6 5.4 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC1CC1 10.1016/j.bmcl.2007.09.008
CHEMBL398843 161186 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 430 8 1 6 5.4 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC1CC1 10.1016/j.bmcl.2007.09.008
44446734 162386 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 431 8 0 4 6.1 CCCN(CCN1CCCC1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL404558 162386 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 431 8 0 4 6.1 CCCN(CCN1CCCC1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
1799074 210556 3 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 4.1 CC(=O)/C(=N\Nc1ccccc1C)Nc1cccc(Cl)c1 10.1021/jm025512y
CHEMBL68118 210556 3 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 4.1 CC(=O)/C(=N\Nc1ccccc1C)Nc1cccc(Cl)c1 10.1021/jm025512y
44305524 210190 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 392 6 0 5 5.5 CCCCN(OC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL65574 210190 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 392 6 0 5 5.5 CCCCN(OC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
11795560 64462 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 4 5.7 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL166890 64462 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 4 5.7 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10741540 64902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 434 9 0 5 5.3 CCN(CCOC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL167737 64902 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 434 9 0 5 5.3 CCN(CCOC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10549990 174849 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL432496 174849 0 None -1 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
10766371 66136 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 459 11 0 7 5.8 CCCCc1nc2c(N(CC)CCCC)nc(C)nc2n1-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL170791 66136 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 459 11 0 7 5.8 CCCCc1nc2c(N(CC)CCCC)nc(C)nc2n1-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
10549990 174849 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980223o
CHEMBL432496 174849 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980223o
10048452 100804 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 8 1 6 5.5 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)cc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL248785 100804 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 8 1 6 5.5 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)cc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
9980267 101218 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 8 1 6 5.6 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC(C)C 10.1016/j.bmcl.2007.09.008
CHEMBL251200 101218 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 8 1 6 5.6 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC(C)C 10.1016/j.bmcl.2007.09.008
10133826 200114 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 371 9 0 5 5.0 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL524617 200114 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 371 9 0 5 5.0 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
11178282 113201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 408 10 0 6 5.3 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3085417 113201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 408 10 0 6 5.3 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3139571 113201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 408 10 0 6 5.3 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
44337305 12079 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 358 7 0 4 4.8 CCCN(c1nc(-c2ccc(Cl)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL106675 12079 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 358 7 0 4 4.8 CCCN(c1nc(-c2ccc(Cl)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
44392681 71299 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 339 6 1 4 4.9 CCC(CC)Nc1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL181439 71299 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 339 6 1 4 4.9 CCC(CC)Nc1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
20780282 70557 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 6 0 4 4.5 CCCN(CC1CC1)C(=O)c1c(C)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL180178 70557 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 6 0 4 4.5 CCCN(CC1CC1)C(=O)c1c(C)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780038 72383 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 436 7 0 4 5.3 CCCN(CCC(F)(F)F)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL183348 72383 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 436 7 0 4 5.3 CCCN(CCC(F)(F)F)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780036 72760 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 444 8 0 4 5.6 CCCN(CCc1ccccc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL183639 72760 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 444 8 0 4 5.6 CCCN(CCc1ccccc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
44306534 210247 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 371 8 0 6 4.3 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1CCCC1 10.1016/j.bmcl.2004.02.053
CHEMBL65979 210247 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 371 8 0 6 4.3 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1CCCC1 10.1016/j.bmcl.2004.02.053
44337502 12161 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 378 9 0 4 5.5 C=CCn1nc(N(CCC)C(C2CC2)C2CC2)nc1-c1c(C)cc(C)cc1C 10.1016/s0960-894x(01)00657-6
CHEMBL107091 12161 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 378 9 0 4 5.5 C=CCn1nc(N(CCC)C(C2CC2)C2CC2)nc1-c1c(C)cc(C)cc1C 10.1016/s0960-894x(01)00657-6
44307772 176212 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 313 4 1 5 3.6 CC(=O)/C(=N\Nc1ccccc1C#N)Oc1ccc(Cl)cc1 10.1021/jm025512y
CHEMBL442559 176212 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 313 4 1 5 3.6 CC(=O)/C(=N\Nc1ccccc1C#N)Oc1ccc(Cl)cc1 10.1021/jm025512y
10782556 66061 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 328 2 0 2 5.2 Cc1ccc2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL170487 66061 0 None - 1 Rat 6.7 pKi = 6.7 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 328 2 0 2 5.2 Cc1ccc2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
44266524 169362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 428 6 0 6 4.8 CCN(c1nc(C)cc(-c2ccccn2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL416882 169362 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 428 6 0 6 4.8 CCN(c1nc(C)cc(-c2ccccn2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
44443632 101256 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 404 7 1 6 4.8 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC 10.1016/j.bmcl.2007.09.008
CHEMBL251397 101256 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 404 7 1 6 4.8 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC 10.1016/j.bmcl.2007.09.008
18449326 70756 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 9 1 5 4.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(COC)COC 10.1021/jm200365y
CHEMBL1807022 70756 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 9 1 5 4.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(COC)COC 10.1021/jm200365y
10892583 210209 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 3.9 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
CHEMBL65721 210209 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 3.9 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C(F)(F)F 10.1021/jm025512y
3623188 210750 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccc(C)cc1 10.1021/jm025512y
CHEMBL69431 210750 1 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 301 4 2 3 3.9 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccc(C)cc1 10.1021/jm025512y
44266453 105043 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 428 6 0 6 4.8 CCN(c1nc(C)cc(-c2cccnc2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL274579 105043 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 428 6 0 6 4.8 CCN(c1nc(C)cc(-c2cccnc2)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
12967650 26695 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 8 1 4 6.8 CCCN(Cc1sc(Nc2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL130265 26695 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 8 1 4 6.8 CCCN(Cc1sc(Nc2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
11246568 140390 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 399 6 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cn3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL371348 140390 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 399 6 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cn3)c3nc(C)cc1c32 10.1021/jm050384+
15965420 73709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 468 7 0 4 6.8 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL186628 73709 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 468 7 0 4 6.8 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
10808132 64210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 355 8 0 5 4.9 CCCCN(CC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
CHEMBL165473 64210 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 355 8 0 5 4.9 CCCCN(CC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
44392766 72105 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3N(C)C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL182915 72105 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3N(C)C)c(C)nn12 10.1016/j.bmcl.2004.05.056
20780080 151876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 427 7 0 5 5.5 Cc1cc(C)c(-n2c3ncccc3n3c(CN(CC4CC4)CC4CC4)c(C)nc23)c(C)c1 10.1016/j.bmcl.2007.01.008
CHEMBL391169 151876 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 427 7 0 5 5.5 Cc1cc(C)c(-n2c3ncccc3n3c(CN(CC4CC4)CC4CC4)c(C)nc23)c(C)c1 10.1016/j.bmcl.2007.01.008
10298158 71382 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 457 7 1 4 7.1 CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL181718 71382 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 457 7 1 4 7.1 CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
18691327 104967 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 427 5 0 3 6.6 CCN(c1nc(C)cc(-c2ccccc2F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL274081 104967 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 427 5 0 3 6.6 CCN(c1nc(C)cc(-c2ccccc2F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10789842 64901 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 453 9 0 9 2.7 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980224g
CHEMBL167717 64901 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 453 9 0 9 2.7 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980224g
9945957 70719 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 341 8 1 4 5.2 CCc1nc(-c2ccc(C)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806733 70719 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 341 8 1 4 5.2 CCc1nc(-c2ccc(C)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
11797773 65436 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 449 11 0 9 3.3 COCCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL168459 65436 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 449 11 0 9 3.3 COCCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
9805117 71762 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 478 7 0 6 7.0 CCCCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL18230 71762 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 478 7 0 6 7.0 CCCCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
44341455 171919 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 322 6 0 4 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL422784 171919 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 322 6 0 4 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)n(C)nc12 10.1016/s0960-894x(03)00621-8
20780283 14100 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 7 0 4 5.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1086163 14100 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 7 0 4 5.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
10528499 127168 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 473 7 1 7 4.1 CCCC(Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(=O)N(C)C 10.1021/jm980224g
CHEMBL353393 127168 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 473 7 1 7 4.1 CCCC(Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br)C(=O)N(C)C 10.1021/jm980224g
18691332 214894 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 424 5 1 4 6.1 CCN(c1nc(C)cc(-c2ccccc2N)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL9795 214894 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 424 5 1 4 6.1 CCN(c1nc(C)cc(-c2ccccc2N)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
44443599 160659 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 362 6 1 5 5.4 Cc1ccnc(Oc2nc(C)c(NC(c3ccccc3)C(C)C)nc2C)c1 10.1016/j.bmcl.2007.09.008
CHEMBL398300 160659 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 362 6 1 5 5.4 Cc1ccnc(Oc2nc(C)c(NC(c3ccccc3)C(C)C)nc2C)c1 10.1016/j.bmcl.2007.09.008
10646364 64303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 6 0 4 5.9 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(Br)cc2Cl)n1 10.1021/jm980222w
CHEMBL166238 64303 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 6 0 4 5.9 CCN(CC)c1cc(C)nc(N(CC)c2c(Cl)cc(Br)cc2Cl)n1 10.1021/jm980222w
11797409 64613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 440 7 0 6 4.0 CCN(CC)c1cc(C)nc(N(CC)c2ccc(S(C)(=O)=O)cc2Br)n1 10.1021/jm980222w
CHEMBL167171 64613 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 440 7 0 6 4.0 CCN(CC)c1cc(C)nc(N(CC)c2ccc(S(C)(=O)=O)cc2Br)n1 10.1021/jm980222w
10501643 64640 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 408 7 0 5 5.3 CCN(CC)c1cc(C)nc(N(CC)c2ccc(SC)cc2Br)n1 10.1021/jm980222w
CHEMBL167195 64640 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 408 7 0 5 5.3 CCN(CC)c1cc(C)nc(N(CC)c2ccc(SC)cc2Br)n1 10.1021/jm980222w
44347223 22027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3cccc(OC)c3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121183 22027 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3cccc(OC)c3)c(C)nn12 10.1016/j.bmcl.2004.05.019
44341736 16985 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 362 4 0 4 5.1 CCCN(C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL116003 16985 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 362 4 0 4 5.1 CCCN(C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
15490815 11314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 487 5 0 3 7.3 CCN(c1nc(C)cc(-c2ccccc2Br)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10237 11314 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 487 5 0 3 7.3 CCN(c1nc(C)cc(-c2ccccc2Br)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
20780276 130713 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 474 6 0 4 5.6 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(Cl)cc1Cl 10.1016/j.bmcl.2005.05.117
CHEMBL362815 130713 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 474 6 0 4 5.6 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(Cl)cc1Cl 10.1016/j.bmcl.2005.05.117
44307879 109048 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 349 4 1 5 4.5 CCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL303272 109048 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 349 4 1 5 4.5 CCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
11282946 70140 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 440 11 0 6 5.8 CCCCC(c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL179540 70140 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 440 11 0 6 5.8 CCCCC(c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(OC)cc2OC)n(C)n1 10.1021/jm049339c
11351594 131541 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 458 8 0 7 5.2 CCCN(Cc1cccc(OC)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL364214 131541 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 458 8 0 7 5.2 CCCN(Cc1cccc(OC)c1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10667729 65852 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 384 8 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169576 65852 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 384 8 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44266439 215159 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 466 5 0 4 7.1 CCN(c1nc(C)cc(-c2c(C)cc(C)nc2C)n1)c1c(C)cc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL9956 215159 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 466 5 0 4 7.1 CCN(c1nc(C)cc(-c2c(C)cc(C)nc2C)n1)c1c(C)cc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
20780041 132074 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 506 7 0 4 7.2 FC(F)(F)c1nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n2c1CN(CC1CC1)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL364537 132074 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 506 7 0 4 7.2 FC(F)(F)c1nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n2c1CN(CC1CC1)CC1CC1 10.1016/j.bmcl.2005.06.028
3533 7989 24 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2004.02.053
5282340 7989 24 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2004.02.053
CHEMBL291657 7989 24 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 10.1016/j.bmcl.2004.02.053
44305973 107325 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 433 10 0 6 5.5 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)[C@@H](c1ccccc1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL291419 107325 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 433 10 0 6 5.5 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)[C@@H](c1ccccc1)C1CC1 10.1016/j.bmcl.2004.02.053
18672262 69410 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 473 8 1 4 7.7 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC(C)C 10.1016/j.bmcl.2004.10.055
CHEMBL178375 69410 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 473 8 1 4 7.7 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC(C)C 10.1016/j.bmcl.2004.10.055
11751505 131436 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 458 7 0 6 5.2 CCCN(CCC)c1c(Br)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL364168 131436 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 458 7 0 6 5.2 CCCN(CCC)c1c(Br)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10316753 67265 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 364 7 1 3 5.2 CCCN(c1n[nH]c(-c2ccc(Cl)cc2Cl)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL175536 67265 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 364 7 1 3 5.2 CCCN(c1n[nH]c(-c2ccc(Cl)cc2Cl)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
10692645 65871 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 404 6 1 7 3.5 COCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169693 65871 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 404 6 1 7 3.5 COCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44443602 100812 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 376 8 1 5 5.7 CCc1nc(Oc2ncccc2C)c(CC)nc1NC(CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL248816 100812 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 376 8 1 5 5.7 CCc1nc(Oc2ncccc2C)c(CC)nc1NC(CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
44460263 212104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 378 7 1 3 5.7 Cc1ccc(N[C@@H](C(=O)CCc2ccncc2)c2ccccc2C)c(Cl)c1 10.1021/jm049974i
CHEMBL79502 212104 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 378 7 1 3 5.7 Cc1ccc(N[C@@H](C(=O)CCc2ccncc2)c2ccccc2C)c(Cl)c1 10.1021/jm049974i
21916075 14354 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 406 3 0 4 5.4 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCCCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087805 14354 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 406 3 0 4 5.4 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCCCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
10801589 168741 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 264 2 0 2 4.8 Cc1cc(C)c2ccn(-c3ccc(C(C)C)cc3)c2n1 10.1021/jm980223o
CHEMBL415752 168741 0 None - 1 Rat 5.6 pKi = 5.6 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 264 2 0 2 4.8 Cc1cc(C)c2ccn(-c3ccc(C(C)C)cc3)c2n1 10.1021/jm980223o
20780184 73871 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.3 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL187362 73871 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.3 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
11452262 80157 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 1 5 4.9 COc1cccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL201470 80157 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 396 5 1 5 4.9 COc1cccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)c1 10.1016/j.bmcl.2005.10.097
10596146 64382 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 383 9 0 6 4.1 CCN(c1nc(C)nc(N(CCOC)CC2CC2)n1)c1c(C)cc(C)cc1C 10.1021/jm980222w
CHEMBL166807 64382 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 383 9 0 6 4.1 CCN(c1nc(C)nc(N(CCOC)CC2CC2)n1)c1c(C)cc(C)cc1C 10.1021/jm980222w
10504356 127510 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 464 11 0 6 4.9 CCN(c1nc(C)cc(N(CCOC)CCOC)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL354859 127510 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 464 11 0 6 4.9 CCN(c1nc(C)cc(N(CCOC)CCOC)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
44392767 73048 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL184694 73048 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 7 0 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.056
10807869 65549 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 351 6 0 5 4.7 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL168731 65549 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 351 6 0 5 4.7 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44307653 108933 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 363 5 1 5 4.9 CCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL302589 108933 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 363 5 1 5 4.9 CCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
10119101 139186 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.4 CCCN(Cc1ccc(F)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL369734 139186 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.4 CCCN(Cc1ccc(F)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11639847 134291 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 396 5 0 5 5.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3OC)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL366179 134291 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 396 5 0 5 5.1 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3OC)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
10788201 65773 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 418 6 2 7 3.6 CCC(CO)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169035 65773 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 418 6 2 7 3.6 CCC(CO)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10573217 127273 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 402 5 0 6 4.3 CCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL354398 127273 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 402 5 0 6 4.3 CCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
20780155 74139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 518 8 0 4 7.7 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL188623 74139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 518 8 0 4 7.7 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
44305986 108902 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 425 9 0 7 5.1 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2cccs2)CC1 10.1016/j.bmcl.2004.02.053
CHEMBL302396 108902 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 425 9 0 7 5.1 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2cccs2)CC1 10.1016/j.bmcl.2004.02.053
11236826 147769 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 473 7 1 6 5.9 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccccn3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL382347 147769 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 473 7 1 6 5.9 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccccn3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
44443592 161771 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 362 7 1 5 5.3 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(C)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL401327 161771 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 362 7 1 5 5.3 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(C)c1ccccc1 10.1016/j.bmcl.2007.09.008
10668655 31578 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2cc(Cl)c(Cl)cc2Cl)nc(C)n1 10.1021/jm960149e
CHEMBL134475 31578 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2cc(Cl)c(Cl)cc2Cl)nc(C)n1 10.1021/jm960149e
10573027 211811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm9900117
CHEMBL77006 211811 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm9900117
44386385 66842 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 382 6 0 7 3.4 CCCN(CCC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
CHEMBL173780 66842 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 382 6 0 7 3.4 CCCN(CCC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)nc1C 10.1016/s0960-894x(99)00108-0
20780137 74174 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 7 0 4 7.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CCC1 10.1016/j.bmcl.2005.06.028
CHEMBL188813 74174 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 7 0 4 7.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CCC1 10.1016/j.bmcl.2005.06.028
10667355 64229 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 377 5 0 4 5.1 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(C(C)C)cc1OC 10.1021/jm980222w
CHEMBL165589 64229 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 377 5 0 4 5.1 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(C(C)C)cc1OC 10.1021/jm980222w
10813479 64259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 450 8 0 5 6.4 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(C(C)C)cc2SC)n1 10.1021/jm980222w
CHEMBL165873 64259 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 450 8 0 5 6.4 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(C(C)C)cc2SC)n1 10.1021/jm980222w
44392761 129122 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 385 10 0 6 4.0 CCCN(CC1CC1)c1cc(Cc2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL359925 129122 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 385 10 0 6 4.0 CCCN(CC1CC1)c1cc(Cc2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
9865133 170646 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 388 6 1 3 5.8 CCCN(CC1CC1)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
CHEMBL420681 170646 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 388 6 1 3 5.8 CCCN(CC1CC1)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
20780016 71950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 498 6 0 4 5.4 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1Br 10.1016/j.bmcl.2005.05.117
CHEMBL182482 71950 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 498 6 0 4 5.4 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1Br 10.1016/j.bmcl.2005.05.117
53310277 70758 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 403 8 0 3 6.2 CCc1nc(N(CC2CC2)CC2CC2)c(CC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807024 70758 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 403 8 0 3 6.2 CCc1nc(N(CC2CC2)CC2CC2)c(CC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
20780089 174552 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 399 7 0 5 5.1 C=CCN(CC=C)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL430391 174552 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 399 7 0 5 5.1 C=CCN(CC=C)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44446727 101610 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(OC)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253700 101610 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(OC)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
10163122 71607 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 483 8 1 4 7.5 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN(CC1CC1)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL181980 71607 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 483 8 1 4 7.5 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN(CC1CC1)CC1CC1 10.1016/j.bmcl.2004.10.055
11350066 175052 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 398 8 0 5 5.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(CC)c1ccccc1 10.1021/jm049339c
CHEMBL433940 175052 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 398 8 0 5 5.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(CC)c1ccccc1 10.1021/jm049339c
11394728 12446 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 374 8 0 5 4.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL107786 12446 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 374 8 0 5 4.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
44385520 136984 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 523 8 0 7 5.0 COCCN(Cc1ccccc1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL367920 136984 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 523 8 0 7 5.0 COCCN(Cc1ccccc1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
44318102 212836 0 None - 1 Human 6.6 pKi = 6.6 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 399 10 0 6 4.3 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CC2CC2)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL85363 212836 0 None - 1 Human 6.6 pKi = 6.6 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 399 10 0 6 4.3 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CC2CC2)c1=O 10.1016/s0960-894x(03)00483-9
21916125 13479 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 7.3 CCCN(Cc1cccc(F)c1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083613 13479 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 7.3 CCCN(Cc1cccc(F)c1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
11211248 72943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 1 7 3.6 CCC(COC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL184284 72943 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 1 7 3.6 CCC(COC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10292638 124844 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 371 7 1 4 5.4 CCCN(CC1CC1)C(=O)c1sc(Nc2c(C)cc(C)cc2C)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL340469 124844 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 371 7 1 4 5.4 CCCN(CC1CC1)C(=O)c1sc(Nc2c(C)cc(C)cc2C)nc1C 10.1016/j.bmcl.2003.08.055
11427630 69784 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 334 7 0 5 3.8 CCCN(CC1CC1)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL178725 69784 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 334 7 0 5 3.8 CCCN(CC1CC1)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
44337533 174648 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 326 6 0 4 4.4 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(C)n1 10.1016/s0960-894x(01)00657-6
CHEMBL431067 174648 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 326 6 0 4 4.4 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(C)n1 10.1016/s0960-894x(01)00657-6
44446736 101405 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 433 10 0 4 6.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN(C)C)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252302 101405 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 433 10 0 4 6.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN(C)C)c2ccccc12 10.1016/j.bmcl.2007.12.050
44443627 160806 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 422 9 1 6 4.9 CCc1nc(Oc2ccccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
CHEMBL398425 160806 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 422 9 1 6 4.9 CCc1nc(Oc2ccccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
10599448 65609 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 7 0 6 4.4 CCN(CCN(C)C)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168846 65609 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 7 0 6 4.4 CCN(CCN(C)C)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11351416 80689 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 450 5 1 5 5.8 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OC(F)(F)F)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL201966 80689 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 450 5 1 5 5.8 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OC(F)(F)F)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
10835160 64211 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 5 4.6 CCN(CC)c1cc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL165475 64211 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 5 4.6 CCN(CC)c1cc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
10621342 127219 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 5 5.1 CCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL353890 127219 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 405 7 0 5 5.1 CCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
53309695 70774 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 337 5 1 3 5.7 CCC(CC)Nc1nc(C)c(-c2ccc(Cl)cc2Cl)nc1C 10.1021/jm200365y
CHEMBL1807040 70774 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 337 5 1 3 5.7 CCC(CC)Nc1nc(C)c(-c2ccc(Cl)cc2Cl)nc1C 10.1021/jm200365y
21916306 14449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 488 6 0 4 6.5 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CCC2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1088624 14449 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 488 6 0 4 6.5 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CCC2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
10618927 65820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 5 2 5 4.5 CCC(CO)Nc1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169418 65820 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 5 2 5 4.5 CCC(CO)Nc1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
10784215 66546 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 352 6 0 6 4.1 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL172571 66546 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 352 6 0 6 4.1 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44341476 16841 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 392 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL115313 16841 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 392 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12 10.1016/s0960-894x(03)00621-8
10764399 65840 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 7 1 7 4.1 COCC(Cc1ccccc1)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169538 65840 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 7 1 7 4.1 COCC(Cc1ccccc1)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
135958361 63962 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.4 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
CHEMBL164931 63962 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1Antagonistic activity against [125I]-Tyr-ovine CRF binding to Corticotropin releasing factor receptor 1
ChEMBL 428 3 4 7 2.4 NCCNC(=O)c1c2c(c3c(O)c4ccccc4c4ncnc1c34)=N[C@H]1CCCC[C@H]1N2 10.1016/s0960-894x(99)00075-x
20780021 70696 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 512 7 0 4 5.9 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2005.05.117
CHEMBL180613 70696 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 512 7 0 4 5.9 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2005.05.117
20780256 71073 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 518 7 0 4 6.8 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)Cc1ccc(Cl)cc1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181053 71073 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 518 7 0 4 6.8 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)Cc1ccc(Cl)cc1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780055 100727 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 444 5 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)Cc4cccnc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL248367 100727 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 444 5 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)Cc4cccnc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
44443577 100762 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 346 8 2 4 5.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.008
CHEMBL248588 100762 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 346 8 2 4 5.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1ccc(Cl)cc1 10.1016/j.bmcl.2007.09.008
3568686 209844 8 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 287 4 2 3 3.8 CC(=O)/C(=N\Nc1ccccc1)Nc1cccc(Cl)c1 10.1021/jm025512y
CHEMBL63664 209844 8 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 287 4 2 3 3.8 CC(=O)/C(=N\Nc1ccccc1)Nc1cccc(Cl)c1 10.1021/jm025512y
44587453 195886 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 359 9 0 6 4.1 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL510224 195886 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 359 9 0 6 4.1 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
20780170 130630 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 490 6 0 4 7.2 CCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL362567 130630 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 490 6 0 4 7.2 CCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
44352478 27643 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 505 8 1 4 7.9 CCCN(Cc1sc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL131046 27643 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 505 8 1 4 7.9 CCCN(Cc1sc(Nc2c(Cl)cc(C(F)(F)F)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44352464 28216 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 539 8 1 4 7.4 CCCN(Cc1sc(Nc2c(Br)cc(C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL131533 28216 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 539 8 1 4 7.4 CCCN(Cc1sc(Nc2c(Br)cc(C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
20780173 133949 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 454 6 0 4 6.5 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL365715 133949 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 454 6 0 4 6.5 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
10526864 64336 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 434 8 0 6 4.8 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(C(C)=O)cc2OC)n1 10.1021/jm980222w
CHEMBL166504 64336 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 434 8 0 6 4.8 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(C(C)=O)cc2OC)n1 10.1021/jm980222w
10740490 185462 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 413 3 0 4 5.1 Cc1cc(N2CCOCC2)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL46798 185462 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 413 3 0 4 5.1 Cc1cc(N2CCOCC2)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
21916258 13477 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 522 7 0 4 7.8 CCCN(Cc1ccc(Cl)cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083611 13477 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 522 7 0 4 7.8 CCCN(Cc1ccc(Cl)cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
20780133 100462 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 471 7 0 5 6.7 CCCN(Cc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL246944 100462 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 471 7 0 5 6.7 CCCN(Cc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
20780060 100535 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 419 7 0 5 5.4 C=CCN(CC=C)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247358 100535 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 419 7 0 5 5.4 C=CCN(CC=C)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44446721 162286 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 362 7 0 3 6.2 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL404171 162286 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 362 7 0 3 6.2 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2C)c2ccccc12 10.1016/j.bmcl.2007.12.050
12967653 71503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 521 9 1 4 8.3 CCCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181884 71503 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 521 9 1 4 8.3 CCCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11394728 12446 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 374 8 0 5 4.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C1CC1)C1CC1 10.1021/jm049339c
CHEMBL107786 12446 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 374 8 0 5 4.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C1CC1)C1CC1 10.1021/jm049339c
11798947 65908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 480 10 0 10 2.4 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL169861 65908 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 480 10 0 10 2.4 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
44388401 69771 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 394 11 0 6 5.3 CCCCC(CC)N(OCCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL178667 69771 0 None - 1 Human 6.6 pKi = 6.6 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 394 11 0 6 5.3 CCCCC(CC)N(OCCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
10180472 28716 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 419 7 1 4 6.4 CCCCN(CC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL132055 28716 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 419 7 1 4 6.4 CCCCN(CC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
20780057 158941 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4ccccn4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL396821 158941 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4ccccn4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
10598041 127090 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 7 0 6 4.7 CCCCN(CC)c1ncnc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL352784 127090 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 7 0 6 4.7 CCCCN(CC)c1ncnc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10811877 172487 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 416 5 0 4 5.8 CCN(c1nc(C)cc(N2CCCCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL424562 172487 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 416 5 0 4 5.8 CCN(c1nc(C)cc(N2CCCCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
10665582 127187 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 350 5 1 4 5.5 CCCCNc1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL353638 127187 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 350 5 1 4 5.5 CCCCNc1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44347190 22054 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 384 8 1 7 3.2 CCCN(CCO)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121301 22054 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 384 8 1 7 3.2 CCCN(CCO)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
10548172 65902 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 385 3 0 5 4.3 COc1cc(Br)c(-n2cc(C#N)c3c(C)cc(C)nc32)c(OC)c1 10.1021/jm980223o
CHEMBL169838 65902 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 385 3 0 5 4.3 COc1cc(Br)c(-n2cc(C#N)c3c(C)cc(C)nc32)c(OC)c1 10.1021/jm980223o
44308157 210641 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 419 8 0 5 6.1 CCCCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL68697 210641 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 419 8 0 5 6.1 CCCCCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
20780274 69767 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 382 7 0 4 4.8 CCCCN(CC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL178617 69767 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 382 7 0 4 4.8 CCCCN(CC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
10164483 129530 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1cccnc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL360458 129530 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 508 8 1 5 7.7 CCCN(Cc1cccnc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10183075 138228 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 8 1 4 7.5 CCCCN(CC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL369109 138228 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 8 1 4 7.5 CCCCN(CC)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44352437 28134 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 489 9 1 4 7.4 CCCN(Cc1sc(Nc2ccc(C(C)C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL131422 28134 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 489 9 1 4 7.4 CCCN(Cc1sc(Nc2ccc(C(C)C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44441102 158944 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 409 6 1 5 5.5 CCCC(C)NCc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL396822 158944 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 409 6 1 5 5.5 CCCC(C)NCc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44389083 69409 0 None - 1 Human 4.5 pKi = 4.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 429 6 2 4 6.4 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CNCC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL178374 69409 0 None - 1 Human 4.5 pKi = 4.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 429 6 2 4 6.4 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CNCC1CC1 10.1016/j.bmcl.2004.10.055
10914632 169465 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 335 4 2 3 4.3 CC(=O)/C(=N\c1cccc(C(F)(F)F)c1)NNc1ccccc1C 10.1021/jm025512y
CHEMBL417037 169465 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 335 4 2 3 4.3 CC(=O)/C(=N\c1cccc(C(F)(F)F)c1)NNc1ccccc1C 10.1021/jm025512y
44397564 74427 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 550 6 0 4 7.5 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL190638 74427 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 550 6 0 4 7.5 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
10549983 65648 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 418 7 1 7 3.9 COCCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168883 65648 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 418 7 1 7 3.9 COCCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11022531 210567 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 287 4 2 3 3.6 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1Cl 10.1021/jm025512y
CHEMBL68238 210567 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 287 4 2 3 3.6 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1Cl 10.1021/jm025512y
CHEMBL413591 219855 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
10765122 64936 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 9 0 6 4.3 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL168131 64936 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 9 0 6 4.3 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
44386432 66363 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 458 7 0 5 5.5 CCCCN(CC)c1cc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL171893 66363 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 458 7 0 5 5.5 CCCCN(CC)c1cc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
9955329 214609 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 0 8 3.9 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL9633 214609 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 0 8 3.9 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
44340885 16931 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL None None None None 10.1016/s0960-894x(00)00661-2
CHEMBL115836 16931 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL None None None None 10.1016/s0960-894x(00)00661-2
44341765 16563 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 374 7 0 2 7.2 CCCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL113653 16563 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 374 7 0 2 7.2 CCCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
44342075 174652 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 360 6 0 2 6.8 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL431076 174652 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 360 6 0 2 6.8 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
44307478 109407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 423 8 0 7 3.7 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
CHEMBL304272 109407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 423 8 0 7 3.7 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
44307474 109415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 377 5 0 5 4.9 CCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
CHEMBL304335 109415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cellsDisplacement of 125I-sauvagine from CRF1 receptor in human IMR-32 cells
ChEMBL 377 5 0 5 4.9 CCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/j.bmc.2017.10.012
CHEMBL4299313 220344 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCN)[C@@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
3520 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
9821250 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
CHEMBL309138 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2015.10.010
44307478 109407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 423 8 0 7 3.7 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL304272 109407 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 423 8 0 7 3.7 COCCN(CCOC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44307474 109415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 5 0 5 4.9 CCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL304335 109415 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 5 0 5 4.9 CCCN(CC)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44307892 210256 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 379 7 0 5 5.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(CC)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66054 210256 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 379 7 0 5 5.4 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(CC)nc12 10.1016/s0960-894x(02)00358-x
9885480 210291 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 365 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66275 210291 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 365 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)n(C)nc12 10.1016/s0960-894x(02)00358-x
3495 7958 28 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2008.07.063
5311055 7958 28 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2008.07.063
CHEMBL9946 7958 28 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2008.07.063
3520 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2008.07.063
9821250 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2008.07.063
CHEMBL309138 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/j.bmcl.2008.07.063
CHEMBL407570 219447 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
177990 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050384+
3489 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050384+
CHEMBL296641 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050384+
10694630 65935 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 1 6 5.8 CCCCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169952 65935 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 1 6 5.8 CCCCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9912938 11235 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.5 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10175 11235 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 3 7.5 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
122193723 130742 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 458 7 1 4 6.0 CCCN(CCC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628743 130742 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 458 7 1 4 6.0 CCCN(CCC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
177990 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050070m
3489 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050070m
CHEMBL296641 7214 23 None -1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 10.1021/jm050070m
11025 9517 7 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
11713007 9517 7 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
CHEMBL380800 9517 7 None 1 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 10.1021/jm049085v
44392707 70532 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 407 7 0 6 4.6 CCCN(CCOC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL180142 70532 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 407 7 0 6 4.6 CCCN(CCOC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
44392688 73089 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL184930 73089 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 391 6 0 5 5.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
10622522 66223 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 0 5 5.6 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL171202 66223 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 0 5 5.6 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44342014 16315 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 0 5 4.7 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112290 16315 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 0 5 4.7 CCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44341754 16806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 408 6 0 2 7.6 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115099 16806 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 408 6 0 2 7.6 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
11774042 210131 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL65078 210131 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 402 6 0 4 5.9 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
9960282 71098 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 595 8 1 4 9.5 FC(F)(F)CCN(Cc1ccc(Cl)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181134 71098 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 595 8 1 4 9.5 FC(F)(F)CCN(Cc1ccc(Cl)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
9952376 16645 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
CHEMBL114193 16645 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00621-8
9952376 16645 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL114193 16645 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9843355 18002 2 None - 1 Human 8.5 pKi = 8.5 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL1178813 18002 2 None - 1 Human 8.5 pKi = 8.5 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
CHEMBL44169 18002 2 None - 1 Human 8.5 pKi = 8.5 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor receptorCompound was tested for the binding affinity to human corticotropin releasing factor receptor
ChEMBL 389 7 1 7 4.0 COCC(COC)n1nnc2c(Nc3c(C)cc(C)cc3Cl)nc(C)cc21 10.1021/jm990590f
9865624 22316 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121896 22316 12 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
11384238 73624 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 406 6 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2015.10.010
CHEMBL186203 73624 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 406 6 1 4 5.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1Cl 10.1016/j.bmcl.2015.10.010
122193716 130732 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 478 6 1 4 5.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(I)cc1C 10.1016/j.bmcl.2015.10.010
CHEMBL3628732 130732 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 478 6 1 4 5.0 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(I)cc1C 10.1016/j.bmcl.2015.10.010
9865624 22316 12 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm040058e
CHEMBL121896 22316 12 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 9 0 7 3.9 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1021/jm040058e
11305029 73703 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 432 6 0 6 4.9 CCN(Cc1ccccc1F)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL186592 73703 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 432 6 0 6 4.9 CCN(Cc1ccccc1F)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10789622 127517 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 447 8 0 7 4.5 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL354940 127517 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 447 8 0 7 4.5 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
10835789 172101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 417 8 0 7 4.7 CCCCN(CC)c1nc(C)nc2c1nc(C)n2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL423444 172101 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 417 8 0 7 4.7 CCCCN(CC)c1nc(C)nc2c1nc(C)n2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
10835759 175309 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 6 0 5 5.6 CCC(CC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL435468 175309 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 6 0 5 5.6 CCC(CC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44347236 120087 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 347 6 0 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C#N)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL331539 120087 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 347 6 0 5 4.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C#N)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
10363370 126653 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 396 7 0 4 5.8 CCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL348967 126653 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 396 7 0 4 5.8 CCN(CCCCF)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(00)00071-8
CHEMBL4299313 220344 0 None -2 2 Human 8.5 pKi = 8.5 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(=O)CCOCCOCCOCCOCCOCCOCCN)[C@@H](C)O)C(C)C)C(=O)N[C@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
3520 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
9821250 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
CHEMBL309138 10041 54 None 1 2 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm040058e
11189666 77970 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 395 6 0 3 6.6 CCCC(CCC)N1CCc2cn(-c3ccc(C)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL195631 77970 0 None - 1 Human 8.5 pKi = 8.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 395 6 0 3 6.6 CCCC(CCC)N1CCc2cn(-c3ccc(C)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
44381516 65823 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 8 1 5 6.4 CCCC(CCC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169430 65823 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 8 1 5 6.4 CCCC(CCC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44347217 103405 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL263492 103405 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 352 7 0 5 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
3495 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2003.08.055
5311055 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2003.08.055
CHEMBL9946 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2003.08.055
9934089 11779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL10504 11779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341813 16375 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 416 6 0 4 6.1 Cc1cc(N(CC(C)C)CC2CC2)c2c(n1)c(-c1ccc(Cl)cc1Cl)nn2C 10.1016/s0960-894x(03)00622-x
CHEMBL112560 16375 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 416 6 0 4 6.1 Cc1cc(N(CC(C)C)CC2CC2)c2c(n1)c(-c1ccc(Cl)cc1Cl)nn2C 10.1016/s0960-894x(03)00622-x
9934089 11779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Compound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneCompound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
CHEMBL10504 11779 0 None - 1 Human 8.4 pKi = 8.4 Binding
Compound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneCompound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 462 9 0 8 3.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
3495 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
5311055 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
CHEMBL9946 7958 28 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/j.bmcl.2005.05.117
18449330 70755 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 389 7 1 3 6.2 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(C1CC1)C1CC1 10.1021/jm200365y
CHEMBL1807021 70755 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 389 7 1 3 6.2 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(C1CC1)C1CC1 10.1021/jm200365y
10188470 138227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 579 8 1 4 9.0 Fc1cccc(CN(CCC(F)(F)F)Cc2sc(Nc3c(Cl)cc(Cl)cc3Cl)nc2C(F)(F)F)c1 10.1016/j.bmcl.2004.10.055
CHEMBL369107 138227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 579 8 1 4 9.0 Fc1cccc(CN(CCC(F)(F)F)Cc2sc(Nc3c(Cl)cc(Cl)cc3Cl)nc2C(F)(F)F)c1 10.1016/j.bmcl.2004.10.055
CHEMBL427807 220164 0 None -1 2 Human 8.4 pKi = 8.4 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CO)C(=O)N[C@H](C(N)=O)C(C)C)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O 10.1021/jm990590f
44341664 16797 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 434 6 0 2 7.9 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115030 16797 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 434 6 0 2 7.9 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
3520 10041 54 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
9821250 10041 54 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
CHEMBL309138 10041 54 None -1 2 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm200365y
10550438 211885 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 426 8 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1CC 10.1021/jm960149e
CHEMBL77716 211885 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 426 8 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1CC 10.1021/jm960149e
10550438 211885 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 426 8 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1CC 10.1021/jm9900117
CHEMBL77716 211885 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 426 8 1 4 6.7 CCCN(CC1CC1)c1nc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)c1CC 10.1021/jm9900117
44392702 163639 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 403 6 0 5 5.3 CCCN(CC1CC1)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL407168 163639 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 403 6 0 5 5.3 CCCN(CC1CC1)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
10670904 127528 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 442 7 0 4 6.6 CCCCN(CC)c1cc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL355049 127528 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 442 7 0 4 6.6 CCCCN(CC)c1cc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44347139 121726 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 368 7 1 6 4.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL334237 121726 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 368 7 1 6 4.6 CCC(CC)Nc1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
46872036 130733 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 366 6 1 4 4.7 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1C 10.1016/j.bmcl.2015.10.010
CHEMBL3628733 130733 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 366 6 1 4 4.7 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1C 10.1016/j.bmcl.2015.10.010
11628147 77335 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 434 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(C(F)(F)F)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL194836 77335 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 434 4 0 4 6.1 CC[C@H]1Cn2nc(-c3ccc(C(F)(F)F)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11605928 78671 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 396 5 0 5 5.1 CC[C@H]1Cn2nc(-c3ccc(OC)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL197134 78671 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 396 5 0 5 5.1 CC[C@H]1Cn2nc(-c3ccc(OC)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11560698 142058 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 5 0 4 6.1 CCC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL372653 142058 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 5 0 4 6.1 CCC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11598576 148126 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 4 0 4 5.7 CCC(CC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
CHEMBL383602 148126 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 4 0 4 5.7 CCC(CC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
11795560 64462 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 4 5.7 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL166890 64462 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 4 5.7 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
44375438 63334 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 408 7 0 4 5.8 Cc1cc(C)c(-n2c(C)c(C)c3c(N(CCCF)CC4CC4)nc(C)nc32)c(C)c1 10.1016/s0960-894x(00)00071-8
CHEMBL164042 63334 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Compound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellumCompound was tested in vitro for its ability to displace [125 I]Tyr-sauvagine from corticotropin-releasing hormone type 1 receptor in rat cerebellum
ChEMBL 408 7 0 4 5.8 Cc1cc(C)c(-n2c(C)c(C)c3c(N(CCCF)CC4CC4)nc(C)nc32)c(C)c1 10.1016/s0960-894x(00)00071-8
10048451 160611 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 9 1 6 5.6 CCCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL398258 160611 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 9 1 6 5.6 CCCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
44446740 162388 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 475 10 0 5 6.2 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCOCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL404560 162388 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 475 10 0 5 6.2 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCOCC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
10573027 211811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm960149e
CHEMBL77006 211811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm960149e
10573027 211811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm9900117
CHEMBL77006 211811 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(Nc2c(Cl)cc(Cl)cc2Cl)nc(C)n1 10.1021/jm9900117
11152649 75296 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 361 6 0 3 6.0 CCCC(CCC)N1CCc2cn(-c3ccc(C)cc3)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL191755 75296 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 361 6 0 3 6.0 CCCC(CCC)N1CCc2cn(-c3ccc(C)cc3)c3nc(C)cc1c23 10.1021/jm050070m
20780290 70695 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 378 7 0 4 4.3 C=CCN(CC=C)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL180610 70695 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 378 7 0 4 4.3 C=CCN(CC=C)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780257 71061 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 464 7 0 4 6.2 CCCN(Cc1ccc(Cl)cc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181002 71061 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 464 7 0 4 6.2 CCCN(Cc1ccc(Cl)cc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
11798634 64368 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 470 7 0 5 5.3 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(Br)cc2OC)n1 10.1021/jm980222w
CHEMBL166776 64368 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 470 7 0 5 5.3 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(Br)cc2OC)n1 10.1021/jm980222w
11792683 64873 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 357 8 0 6 3.7 CCN(CCOC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
CHEMBL167464 64873 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 357 8 0 6 3.7 CCN(CCOC)c1nc(C)nc(N(CC)c2c(C)cc(C)cc2C)n1 10.1021/jm980222w
44392760 72016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 391 9 0 4 5.3 C=CCc1c(C(=O)c2c(C)cc(C)cc2C)nc(C)nc1N(CCC)CC1CC1 10.1016/j.bmcl.2004.05.072
CHEMBL182706 72016 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 391 9 0 4 5.3 C=CCc1c(C(=O)c2c(C)cc(C)cc2C)nc(C)nc1N(CCC)CC1CC1 10.1016/j.bmcl.2004.05.072
176157 9515 28 None -9 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/s0960-894x(00)00661-2
3512 9515 28 None -9 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/s0960-894x(00)00661-2
CHEMBL45281 9515 28 None -9 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.Binding affinity towards Corticotropin releasing hormone receptor type 1 of rat cerebellum using [125I]Tyr-sauvagine as radioligand.
ChEMBL 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 10.1016/s0960-894x(00)00661-2
21916078 14450 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 420 6 0 4 5.6 CCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2010.01.127
CHEMBL1088625 14450 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 420 6 0 4 5.6 CCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2010.01.127
44386496 69352 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 499 10 0 6 6.4 CCCCN(CC)c1nc(C)nc2c1nc(OCC1CC1)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL178272 69352 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 499 10 0 6 6.4 CCCCN(CC)c1nc(C)nc2c1nc(OCC1CC1)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10648379 65851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 479 10 0 9 3.0 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL169571 65851 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 479 10 0 9 3.0 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1c(Br)cc(OC)cc1OC 10.1021/jm980224g
11501973 103621 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 4 0 4 5.7 CCCN1c2cc(C)nc3c(-c4ccc(Cl)cc4Cl)nn(c23)C[C@@H]1CC 10.1021/jm049085v
CHEMBL265282 103621 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 4 0 4 5.7 CCCN1c2cc(C)nc3c(-c4ccc(Cl)cc4Cl)nn(c23)C[C@@H]1CC 10.1021/jm049085v
22324325 212652 0 None - 1 Human 6.5 pKi = 6.5 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 373 9 0 6 3.9 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL83789 212652 0 None - 1 Human 6.5 pKi = 6.5 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 373 9 0 6 3.9 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
21916104 13190 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 426 6 0 4 6.0 CCCCN(C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1082368 13190 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 426 6 0 4 6.0 CCCCN(C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
16416344 210157 14 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 376 2 0 5 4.2 Cc1cc(N2CCOCC2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(98)00372-2
CHEMBL65308 210157 14 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 376 2 0 5 4.2 Cc1cc(N2CCOCC2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(98)00372-2
44337472 115728 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 366 8 0 4 5.3 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(CC)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL321155 115728 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 366 8 0 4 5.3 CCCN(c1nc(-c2c(C)cc(C)cc2C)n(CC)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
10228046 28211 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 485 7 1 4 7.1 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2003.08.055
CHEMBL131530 28211 0 None - 1 Human 4.5 pKi = 4.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 485 7 1 4 7.1 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2003.08.055
44460259 212414 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1[C@H](Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL81760 212414 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1[C@H](Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
9828535 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980222w
CHEMBL424204 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980222w
CHEMBL43216 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980222w
44341728 16755 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 396 7 0 4 6.0 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(C)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL114821 16755 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 396 7 0 4 6.0 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(C)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
44341763 170213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 7 0 4 6.4 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL419761 170213 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 7 0 4 6.4 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
9821153 16248 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 378 5 0 5 4.3 COCCN(C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL111960 16248 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 378 5 0 5 4.3 COCCN(C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
21916241 13261 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 456 8 0 5 5.6 CCCN(CCOC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1082685 13261 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 456 8 0 5 5.6 CCCN(CCOC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
11225236 148148 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 472 7 1 5 6.5 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccccc3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL383773 148148 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 472 7 1 5 6.5 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3ccccc3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
21916145 14272 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 434 7 0 4 6.0 CCCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2010.01.127
CHEMBL1087164 14272 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 434 7 0 4 6.0 CCCN(Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2010.01.127
44446742 101454 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 489 10 1 5 6.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCC(O)C2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252688 101454 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 489 10 1 5 6.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCCC(O)C2)c2ccccc12 10.1016/j.bmcl.2007.12.050
9828535 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneInhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm990590f
CHEMBL424204 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneInhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm990590f
CHEMBL43216 172340 0 None 1 2 Human 7.5 pKi = 7.5 Binding
Inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneInhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm990590f
10671608 65531 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 458 9 0 6 5.8 CCCCN(CCCC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168646 65531 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 458 9 0 6 5.8 CCCCN(CCCC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11247120 17063 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL116167 17063 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 418 8 0 4 6.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
44341738 16813 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 332 6 0 2 6.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C)cc3)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115154 16813 1 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 332 6 0 2 6.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(C)cc3)cccc12 10.1016/s0960-894x(03)00684-x
44341729 17178 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 432 9 0 4 7.1 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL116280 17178 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 432 9 0 4 7.1 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
46891011 13209 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.0 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCC(C)CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082444 13209 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.0 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCC(C)CC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780059 173381 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4ccncc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL428044 173381 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4ccncc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
44337516 14359 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 338 7 1 3 4.8 CCCN(c1n[nH]c(-c2c(C)cc(C)cc2C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL108784 14359 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 338 7 1 3 4.8 CCCN(c1n[nH]c(-c2c(C)cc(C)cc2C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
44317667 111190 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 406 8 1 3 6.5 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C(C)C)c(Cl)c1 10.1021/jm049974i
CHEMBL310343 111190 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 406 8 1 3 6.5 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C(C)C)c(Cl)c1 10.1021/jm049974i
10572455 64464 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 389 7 1 5 4.8 C=CCNc1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL166897 64464 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 389 7 1 5 4.8 C=CCNc1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
20780009 13398 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 6 0 4 6.0 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083299 13398 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 6 0 4 6.0 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
44587490 194899 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 361 7 0 4 5.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1Cl 10.1016/j.bmcl.2008.07.063
CHEMBL498319 194899 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 361 7 0 4 5.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1Cl 10.1016/j.bmcl.2008.07.063
44337293 12083 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 344 7 0 4 4.5 CCCN(c1nc(-c2ccc(Cl)cc2)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL106728 12083 0 None - 1 Human 7.5 pKi = 7.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 344 7 0 4 4.5 CCCN(c1nc(-c2ccc(Cl)cc2)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
10791657 65499 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 504 9 0 9 3.3 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(OC(F)(F)F)cc1Br 10.1021/jm980224g
CHEMBL168536 65499 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 504 9 0 9 3.3 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(OC(F)(F)F)cc1Br 10.1021/jm980224g
10765120 65037 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 0 7 4.1 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)=O)cc1Br 10.1021/jm980224g
CHEMBL168252 65037 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 0 7 4.1 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)=O)cc1Br 10.1021/jm980224g
44460600 111904 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 8 1 3 6.3 CCc1ccccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL311431 111904 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 8 1 3 6.3 CCc1ccccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
46881383 13936 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 6 0 4 5.3 CCCN(CC1CCC1)C(=O)c1c(C)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1085431 13936 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 408 6 0 4 5.3 CCCN(CC1CCC1)C(=O)c1c(C)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
10640801 65556 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 339 2 0 3 3.5 Cc1cc(C)nc(N(C)c2ccc(I)cc2)n1 10.1021/jm980222w
CHEMBL168764 65556 1 None - 1 Rat 5.5 pKi = 5.5 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 339 2 0 3 3.5 Cc1cc(C)nc(N(C)c2ccc(I)cc2)n1 10.1021/jm980222w
44397565 129414 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 580 9 0 4 8.5 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CCc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL360389 129414 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 580 9 0 4 8.5 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CCc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
44318056 212029 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity of compound towards human Corticotropin releasing factor receptor 1Binding affinity of compound towards human Corticotropin releasing factor receptor 1
ChEMBL 398 7 1 3 6.1 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2Cl)c(Cl)c1 10.1021/jm049974i
CHEMBL78884 212029 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity of compound towards human Corticotropin releasing factor receptor 1Binding affinity of compound towards human Corticotropin releasing factor receptor 1
ChEMBL 398 7 1 3 6.1 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2Cl)c(Cl)c1 10.1021/jm049974i
44443609 100930 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 420 10 1 6 5.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(COC(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL249430 100930 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 420 10 1 6 5.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(COC(C)C)c1ccccc1 10.1016/j.bmcl.2007.09.008
44460599 174901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 7 1 3 6.4 Cc1cccc(C)c1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL432928 174901 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 7 1 3 6.4 Cc1cccc(C)c1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
44443578 161628 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 327 8 2 5 4.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1cccc(C)n1 10.1016/j.bmcl.2007.09.008
CHEMBL400531 161628 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 327 8 2 5 4.6 CCc1nc(NC(CC)CC)c(CC)nc1Nc1cccc(C)n1 10.1016/j.bmcl.2007.09.008
20780184 73871 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.3 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL187362 73871 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.3 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
20780065 173154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 7.6 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC(F)(F)C(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL427527 173154 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 7.6 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC(F)(F)C(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
44341855 121586 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 467 8 0 5 6.5 CCCCN(CCc1ccncc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL334061 121586 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 467 8 0 5 6.5 CCCCN(CCc1ccncc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
10502734 127224 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 429 3 0 3 6.8 Cc1cc(-c2ccccc2)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL353916 127224 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 429 3 0 3 6.8 Cc1cc(-c2ccccc2)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
20780265 13321 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 560 7 0 4 7.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccc(F)cc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082963 13321 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 560 7 0 4 7.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccc(F)cc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11307122 80432 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 532 9 1 7 6.5 COc1cc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)cc(OC)c1 10.1016/j.bmcl.2005.10.097
CHEMBL201798 80432 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 532 9 1 7 6.5 COc1cc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)cc(OC)c1 10.1016/j.bmcl.2005.10.097
44341861 16372 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 384 8 0 4 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112549 16372 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 384 8 0 4 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)nn(C)c12 10.1016/s0960-894x(03)00622-x
20780288 12361 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 406 6 0 4 4.9 Cc1cc(C)c(N2CCCn3c2nc(C)c3C(=O)N(CC2CC2)CC2CC2)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1077158 12361 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 406 6 0 4 4.9 Cc1cc(C)c(N2CCCn3c2nc(C)c3C(=O)N(CC2CC2)CC2CC2)c(C)c1 10.1016/j.bmcl.2010.01.127
44337533 174648 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 326 6 0 4 4.4 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(C)n1 10.1021/jm049339c
CHEMBL431067 174648 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 326 6 0 4 4.4 CCCN(CCC)c1nc(-c2ccc(Cl)cc2Cl)n(C)n1 10.1021/jm049339c
44337577 12116 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 390 6 0 5 5.3 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)c1ccccc1OC 10.1016/s0960-894x(01)00657-6
CHEMBL106874 12116 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 390 6 0 5 5.3 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)c1ccccc1OC 10.1016/s0960-894x(01)00657-6
44386313 127604 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 514 8 0 7 5.5 CCCCN(CC)c1nc(C)nc2c1nc(N1CCOCC1)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL355803 127604 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 514 8 0 7 5.5 CCCCN(CC)c1nc(C)nc2c1nc(N1CCOCC1)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10550837 64602 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 434 7 2 8 2.2 Cc1nc(N(CCO)CCO)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
CHEMBL167024 64602 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 434 7 2 8 2.2 Cc1nc(N(CCO)CCO)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
10041172 169242 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 311 4 2 3 3.6 C#Cc1cccc(/N=C(/NNc2ccccc2Cl)C(C)=O)c1 10.1021/jm025512y
CHEMBL416693 169242 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 311 4 2 3 3.6 C#Cc1cccc(/N=C(/NNc2ccccc2Cl)C(C)=O)c1 10.1021/jm025512y
10688248 65583 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 335 4 0 4 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(OC)cc1Br 10.1021/jm980222w
CHEMBL168824 65583 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 335 4 0 4 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(OC)cc1Br 10.1021/jm980222w
44341697 16718 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL114649 16718 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
10319873 101040 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL250282 101040 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
21916156 13667 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 7.3 CCCN(Cc1ccc(F)cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1084297 13667 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 7.3 CCCN(Cc1ccc(F)cc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916243 13738 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 474 6 0 4 6.7 CCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1084564 13738 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 474 6 0 4 6.7 CCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916231 14183 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 7 0 4 7.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCc4ccccc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086522 14183 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 7 0 4 7.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCc4ccccc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11395654 85102 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2094064 85102 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2109726 85102 0 None - 1 Human 6.5 pKi = 6.5 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
44352370 25655 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 455 8 1 4 7.0 CCCN(Cc1oc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL128310 25655 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 455 8 1 4 7.0 CCCN(Cc1oc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
18691315 105019 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 453 6 1 4 6.2 CCN(c1nc(C)cc(-c2ccccc2C(=O)O)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL274439 105019 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 453 6 1 4 6.2 CCN(c1nc(C)cc(-c2ccccc2C(=O)O)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10268909 200335 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 341 7 0 4 5.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL526829 200335 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 341 7 0 4 5.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)nc1OC 10.1016/j.bmcl.2008.07.063
20780126 175030 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 6 0 4 6.5 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL433763 175030 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 6 0 4 6.5 CCCN(CC1CC1)C(=O)c1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
10686839 64918 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 315 5 0 4 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1SC 10.1021/jm980222w
CHEMBL167871 64918 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 315 5 0 4 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1SC 10.1021/jm980222w
10787443 65809 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 404 3 0 2 6.9 Cc1cc(-c2ccccc2)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL169359 65809 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 404 3 0 2 6.9 Cc1cc(-c2ccccc2)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
20780122 100615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 423 7 0 5 5.9 CCCCN(CC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247755 100615 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 423 7 0 5 5.9 CCCCN(CC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
20780177 153782 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 421 6 0 5 5.5 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
CHEMBL392654 153782 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 421 6 0 5 5.5 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
44446722 101580 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 8 0 3 6.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2CC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253491 101580 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 8 0 3 6.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2CC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL2372911 217091 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
10838946 65838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 494 8 1 7 5.1 COCC(Cc1ccccc1)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169528 65838 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 494 8 1 7 5.1 COCC(Cc1ccccc1)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
12967647 25713 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 7 1 4 6.4 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL128625 25713 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 7 1 4 6.4 CCCN(CC1CC1)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
20780124 74187 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 428 6 0 4 5.8 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL188849 74187 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 428 6 0 4 5.8 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
44392802 128957 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 395 10 1 4 5.2 CCCN(CC1CC1)c1cc(C(O)c2c(CC)cc(CC)cc2CC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL359745 128957 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 395 10 1 4 5.2 CCCN(CC1CC1)c1cc(C(O)c2c(CC)cc(CC)cc2CC)nc(C)n1 10.1016/j.bmcl.2004.05.072
20780186 100647 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 395 5 0 5 5.1 CCN(CC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247957 100647 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 395 5 0 5 5.1 CCN(CC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
20780149 74080 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 8 0 4 7.2 CCCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL188358 74080 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 482 8 0 4 7.2 CCCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
10737736 65519 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 367 2 0 3 5.4 Cc1cc(C)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL168590 65519 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 367 2 0 3 5.4 Cc1cc(C)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
21916261 14276 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 404 3 0 4 5.1 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CC=CCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087172 14276 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 404 3 0 4 5.1 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CC=CCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
10545026 64664 1 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 339 2 0 3 3.5 Cc1cc(C)nc(N(C)c2ccccc2I)n1 10.1021/jm980222w
CHEMBL167217 64664 1 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 339 2 0 3 3.5 Cc1cc(C)nc(N(C)c2ccccc2I)n1 10.1021/jm980222w
53309547 70771 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 393 9 1 3 7.0 CCCCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807037 70771 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 393 9 1 3 7.0 CCCCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
15490819 104925 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 438 6 1 4 6.5 CCN(c1nc(C)cc(-c2ccccc2NC)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL273745 104925 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 438 6 1 4 6.5 CCN(c1nc(C)cc(-c2ccccc2NC)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
44341718 104159 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 9 0 4 7.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C(C)C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL269690 104159 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 9 0 4 7.7 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C(C)C)nc12 10.1016/s0960-894x(03)00621-8
10165732 71084 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 537 9 1 5 8.3 CCCN(Cc1ccc(OC)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181084 71084 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 537 9 1 5 8.3 CCCN(Cc1ccc(OC)cc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780140 130842 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 494 7 0 4 7.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL363218 130842 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 494 7 0 4 7.2 CCCN(Cc1c(C(F)(F)F)nc2n(-c3ccc(Cl)cc3Cl)c3ccccc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
44460572 111539 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL310773 111539 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 398 7 1 3 6.1 Cc1ccccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
22324329 110914 0 None - 1 Human 7.4 pKi = 7.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 373 9 0 6 3.9 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL309440 110914 0 None - 1 Human 7.4 pKi = 7.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 373 9 0 6 3.9 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
11122528 72002 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 413 10 0 7 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182643 72002 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 413 10 0 7 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
44392773 73431 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 349 7 0 4 4.4 C=CCN(CC=C)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL185329 73431 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 349 7 0 4 4.4 C=CCN(CC=C)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
10786842 64294 1 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 395 4 0 3 5.0 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1I 10.1021/jm980223o
CHEMBL166162 64294 1 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 395 4 0 3 5.0 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1I 10.1021/jm980223o
10786842 64294 1 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 395 4 0 3 5.0 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1I 10.1021/jm980222w
CHEMBL166162 64294 1 None - 1 Rat 7.4 pKi = 7.4 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 395 4 0 3 5.0 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1I 10.1021/jm980222w
44308172 169466 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 6 1 5 5.2 CCCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL417039 169466 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 377 6 1 5 5.2 CCCCCNc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
21916214 14352 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 524 7 0 4 7.0 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CCc2ccccc2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087803 14352 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 524 7 0 4 7.0 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CCc2ccccc2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
10301060 71639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 507 8 1 4 8.3 CCCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL182133 71639 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 507 8 1 4 8.3 CCCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10527943 65821 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 459 8 1 7 4.5 CCCC(CN(C)C)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169421 65821 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 459 8 1 7 4.5 CCCC(CN(C)C)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44392747 73095 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 5 0 5 3.9 COC[C@@H]1CCCN1c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL184963 73095 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 367 5 0 5 3.9 COC[C@@H]1CCCN1c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
44341857 117197 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 459 7 0 5 6.0 CCCCN(CC1CCCN1C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL324497 117197 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 459 7 0 5 6.0 CCCCN(CC1CCCN1C)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44443593 101108 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 406 10 1 6 5.3 CCOCC(Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL250618 101108 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 406 10 1 6 5.3 CCOCC(Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
11727011 210482 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 4.2 CC(=O)/C(=N\c1ccc(Cl)cc1)NNc1ccccc1Cl 10.1021/jm025512y
CHEMBL67570 210482 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 4.2 CC(=O)/C(=N\c1ccc(Cl)cc1)NNc1ccccc1Cl 10.1021/jm025512y
44317976 111541 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 415 6 2 4 6.1 COc1ccc(C(=O)C(Nc2ccc(Cl)cc2Cl)c2ccccc2C)cc1O 10.1021/jm049974i
CHEMBL310783 111541 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 415 6 2 4 6.1 COc1ccc(C(=O)C(Nc2ccc(Cl)cc2Cl)c2ccccc2C)cc1O 10.1021/jm049974i
44318168 212794 0 None - 1 Human 7.4 pKi = 7.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 389 9 0 5 4.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CCF)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL84974 212794 0 None - 1 Human 7.4 pKi = 7.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 389 9 0 5 4.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(CCF)c1=O 10.1016/s0960-894x(03)00483-9
11235365 73059 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 414 7 0 6 5.1 CCCN(CCC)c1c(Cl)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL184740 73059 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 414 7 0 6 5.1 CCCN(CCC)c1c(Cl)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10672294 65878 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 477 10 0 8 4.2 CCOCC(COCC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169751 65878 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 477 10 0 8 4.2 CCOCC(COCC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10166079 129891 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 547 7 1 4 8.4 FC(F)(F)CN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL361108 129891 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 547 7 1 4 8.4 FC(F)(F)CN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10833915 127523 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 384 9 0 8 2.7 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1 10.1021/jm980224g
CHEMBL355008 127523 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 384 9 0 8 2.7 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1 10.1021/jm980224g
11282674 80692 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 463 9 1 6 6.0 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCCCCC#N)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL201982 80692 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 463 9 1 6 6.0 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCCCCC#N)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
11677548 141956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 374 3 0 4 5.2 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2CC(C)C 10.1021/jm049085v
CHEMBL371981 141956 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 374 3 0 4 5.2 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2CC(C)C 10.1021/jm049085v
44443580 100886 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 353 6 2 5 5.1 CCC(CC)Nc1nc(C)c(Nc2ncc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2007.09.008
CHEMBL249191 100886 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 353 6 2 5 5.1 CCC(CC)Nc1nc(C)c(Nc2ncc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2007.09.008
44318106 112910 0 None - 1 Human 8.4 pKi = 8.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 9 0 5 4.7 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL313479 112910 0 None - 1 Human 8.4 pKi = 8.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 9 0 5 4.7 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
10790606 64872 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 471 9 0 6 5.2 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(OC(F)(F)F)cc2Br)n1 10.1021/jm980222w
CHEMBL167463 64872 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 471 9 0 6 5.2 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(OC(F)(F)F)cc2Br)n1 10.1021/jm980222w
10741479 65600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 433 9 0 5 5.9 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL168844 65600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 433 9 0 5 5.9 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10502738 172484 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 429 9 0 5 5.4 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL424555 172484 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 429 9 0 5 5.4 C=CCN(CC=C)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10808915 127591 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 7 1 6 4.8 CCCC(CCC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL355689 127591 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 7 1 6 4.8 CCCC(CCC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44341815 16230 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 448 10 0 5 6.3 CCCCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL111838 16230 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 448 10 0 5 6.3 CCCCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
11417694 74227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1016/j.bmcl.2015.10.010
CHEMBL189089 74227 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 382 7 1 5 4.4 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(OC)cc1C 10.1016/j.bmcl.2015.10.010
44307724 108956 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 371 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3C)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL302742 108956 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 371 6 0 5 4.9 CCCN(CCC)c1nc(C)nc2c(-c3ccc(Cl)cc3C)n(C)nc12 10.1016/s0960-894x(02)00358-x
11178741 113159 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 426 10 0 5 6.3 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3085414 113159 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 426 10 0 5 6.3 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3139324 113159 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 426 10 0 5 6.3 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
9868427 70614 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 450 5 0 6 6.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL18029 70614 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 450 5 0 6 6.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
9956594 104900 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 474 7 0 6 5.7 CCCN(CC1CC1)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL273559 104900 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 474 7 0 6 5.7 CCCN(CC1CC1)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
44341491 16262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 376 5 0 4 5.5 CCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112031 16262 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 376 5 0 4 5.5 CCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9868427 70614 0 None - 1 Human 8.4 pKi = 8.4 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 450 5 0 6 6.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
CHEMBL18029 70614 0 None - 1 Human 8.4 pKi = 8.4 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 450 5 0 6 6.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
22249094 70714 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 365 7 1 3 6.2 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806728 70714 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 365 7 1 3 6.2 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(CC)CC 10.1021/jm200365y
10223332 70722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 9 1 5 5.8 CCc1nc(-c2ccc(OC)cc2OC(F)(F)F)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806736 70722 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 9 1 5 5.8 CCc1nc(-c2ccc(OC)cc2OC(F)(F)F)c(CC)nc1NC(CC)CC 10.1021/jm200365y
9801390 116512 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 7 0 4 6.4 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
CHEMBL322969 116512 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 7 0 4 6.4 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(CC)c12 10.1016/s0960-894x(03)00621-8
46871760 13582 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 472 7 0 4 6.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3Cl)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
CHEMBL1083921 13582 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 472 7 0 4 6.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3Cl)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
122193717 130734 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 472 6 1 4 6.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628734 130734 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 472 6 1 4 6.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C(C)(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
53310133 70718 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 385 10 1 5 5.7 CCc1nc(-c2ccc(OC(C)C)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806732 70718 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 385 10 1 5 5.7 CCc1nc(-c2ccc(OC(C)C)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
9951076 74185 2 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
CHEMBL188844 74185 2 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
CHEMBL2165204 74185 2 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 7 0 6 4.1 CCCN(CCC)c1cc(C)nc2c(-c3ccc(N(C)C)nc3)c(C)nn12 10.1021/jm040058e
11177298 129760 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 408 9 0 6 5.2 CCCCN(CCCC)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL360851 129760 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 408 9 0 6 5.2 CCCCN(CCCC)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
11224781 131301 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 415 6 0 3 7.0 CCCC(CCC)N1CCc2cn(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL364016 131301 0 None - 1 Human 8.4 pKi = 8.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 415 6 0 3 7.0 CCCC(CCC)N1CCc2cn(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
10717500 127029 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 0 5 5.6 CCCCN(CC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL352340 127029 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 0 5 5.6 CCCCN(CC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10551312 127197 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 0 7 4.0 C=CCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL353732 127197 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 444 8 0 7 4.0 C=CCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
22249116 70775 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 353 6 1 4 5.4 CCC(CC)Nc1nc(C)c(-c2ccc(Cl)cc2Cl)nc1OC 10.1021/jm200365y
CHEMBL1807041 70775 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 353 6 1 4 5.4 CCC(CC)Nc1nc(C)c(-c2ccc(Cl)cc2Cl)nc1OC 10.1021/jm200365y
44384802 66709 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 381 6 0 6 4.0 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
CHEMBL173196 66709 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 381 6 0 6 4.0 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
9931098 65541 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 404 8 0 8 3.8 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL168676 65541 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 404 8 0 8 3.8 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
10717499 136177 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 1 5 6.0 CCCC(CC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL367110 136177 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 7 1 5 6.0 CCCC(CC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9908466 121582 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL334039 121582 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 390 6 0 4 5.9 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
44341739 120278 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 1 5 4.5 CCCN(CCO)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL332040 120278 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 1 5 4.5 CCCN(CCO)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44341737 120872 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 388 5 0 4 5.5 CCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL332721 120872 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 388 5 0 4 5.5 CCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
46872038 130735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 430 6 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1C 10.1016/j.bmcl.2015.10.010
CHEMBL3628735 130735 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 430 6 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Br)cc1C 10.1016/j.bmcl.2015.10.010
46872037 130736 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 430 6 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628736 130736 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 430 6 1 4 5.2 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1Br 10.1016/j.bmcl.2015.10.010
122193718 130737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 386 6 1 4 5.1 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1Cl 10.1016/j.bmcl.2015.10.010
CHEMBL3628737 130737 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 386 6 1 4 5.1 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(C)cc1Cl 10.1016/j.bmcl.2015.10.010
10200724 70749 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 395 8 1 4 5.9 CCc1nc(-c2ccc(OC)cc2C(F)(F)F)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806956 70749 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 395 8 1 4 5.9 CCc1nc(-c2ccc(OC)cc2C(F)(F)F)c(CC)nc1NC(CC)CC 10.1021/jm200365y
22248884 70780 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 8 1 5 5.3 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(C(F)(F)F)cc1OC 10.1021/jm200365y
CHEMBL1807050 70780 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 397 8 1 5 5.3 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(C(F)(F)F)cc1OC 10.1021/jm200365y
CHEMBL2372650 217058 0 None 2 2 Human 8.4 pKi = 8.4 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](C)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)[C@@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)CC)C(N)=O 10.1021/jm990590f
10375 9516 18 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm050384+
9888194 9516 18 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm050384+
CHEMBL188907 9516 18 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm050384+
10552437 65884 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 472 10 1 6 6.6 CCCCC(CCCC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169781 65884 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 472 10 1 6 6.6 CCCCC(CCCC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341875 174864 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 400 6 0 2 7.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
CHEMBL432607 174864 1 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 400 6 0 2 7.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)ccc12 10.1016/s0960-894x(03)00684-x
21916240 13843 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 7 0 4 6.1 C=CCN(CCC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1084999 13843 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 7 0 4 6.1 C=CCN(CCC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
9912040 127547 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 458 8 0 7 4.3 COCCN(CC1CC1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL355329 127547 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 458 8 0 7 4.3 COCCN(CC1CC1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
15490820 175505 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 4 6.6 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)=O)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL436978 175505 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 5 0 4 6.6 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(C(C)=O)cc1Br 10.1016/s0960-894x(99)00132-8
23595014 70785 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 385 8 1 5 5.3 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)F)cc2Cl)nc1OC 10.1021/jm200365y
CHEMBL1807055 70785 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 385 8 1 5 5.3 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)F)cc2Cl)nc1OC 10.1021/jm200365y
10695347 65844 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 9 0 7 4.1 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169561 65844 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 9 0 7 4.1 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10741252 127032 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 10 0 8 4.1 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
CHEMBL352353 127032 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 10 0 8 4.1 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1SC 10.1021/jm980224g
44341901 16843 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 414 9 0 5 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(OC)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL115349 16843 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 414 9 0 5 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(OC)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
10303689 130606 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 579 8 1 4 9.0 Fc1ccc(CN(CCC(F)(F)F)Cc2sc(Nc3c(Cl)cc(Cl)cc3Cl)nc2C(F)(F)F)cc1 10.1016/j.bmcl.2004.10.055
CHEMBL362448 130606 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 579 8 1 4 9.0 Fc1ccc(CN(CCC(F)(F)F)Cc2sc(Nc3c(Cl)cc(Cl)cc3Cl)nc2C(F)(F)F)cc1 10.1016/j.bmcl.2004.10.055
11429341 74136 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 8 1 6 5.2 CCCC(CCC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL188609 74136 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 8 1 6 5.2 CCCC(CCC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44392678 71420 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 1 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(NC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL181812 71420 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 366 7 1 6 4.4 CCCN(CCC)c1cc(C)nc2c(-c3ncc(NC)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44392749 73482 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3N)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL185570 73482 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3N)c(C)nn12 10.1016/j.bmcl.2004.05.056
11153953 16916 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 8 1 3 6.6 CCCCN(CCCC)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
CHEMBL115759 16916 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 404 8 1 3 6.6 CCCCN(CCCC)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
44305256 109134 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 376 6 0 4 5.6 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cnn12 10.1016/s0960-894x(98)00372-2
CHEMBL303789 109134 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 376 6 0 4 5.6 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cnn12 10.1016/s0960-894x(98)00372-2
11749772 75422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 394 5 0 5 4.6 CCC(COC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL191903 75422 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 394 5 0 5 4.6 CCC(COC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
44318123 212472 0 None - 1 Human 5.4 pKi = 5.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 403 11 0 7 3.5 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CCOC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL82275 212472 0 None - 1 Human 5.4 pKi = 5.4 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 403 11 0 7 3.5 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CCOC)c1=O 10.1016/s0960-894x(03)00483-9
22248970 70763 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 368 6 0 3 6.5 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1SC(C)CC 10.1021/jm200365y
CHEMBL1807029 70763 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 368 6 0 3 6.5 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1SC(C)CC 10.1021/jm200365y
44443567 161766 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 300 6 1 5 4.2 CCC(CC)Nc1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
CHEMBL401295 161766 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 300 6 1 5 4.2 CCC(CC)Nc1nc(C)c(Oc2cc(C)ccn2)nc1C 10.1016/j.bmcl.2007.09.008
20780131 74319 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.6 CCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL189714 74319 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 504 7 0 4 7.6 CCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
10645784 64255 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 419 8 1 5 5.8 CCC(CC)Nc1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL165824 64255 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 419 8 1 5 5.8 CCC(CC)Nc1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10553475 176274 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 500 10 0 8 5.2 CCCCN(Cc1nnnn1C)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL443235 176274 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 500 10 0 8 5.2 CCCCN(Cc1nnnn1C)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
20780279 129099 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 434 6 0 4 4.9 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL359832 129099 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 434 6 0 4 4.9 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780026 129125 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 454 6 0 4 5.3 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1Cl 10.1016/j.bmcl.2005.05.117
CHEMBL359936 129125 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 454 6 0 4 5.3 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)F)CCN2c1c(C)cc(C)cc1Cl 10.1016/j.bmcl.2005.05.117
44305246 109100 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 374 2 0 4 5.3 Cc1cc(N2CCCCC2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(98)00372-2
CHEMBL303593 109100 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 374 2 0 4 5.3 Cc1cc(N2CCCCC2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(98)00372-2
20780161 100497 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 401 7 0 5 5.3 C=CCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247152 100497 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 401 7 0 5 5.3 C=CCN(CCC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44446741 101425 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 489 10 1 5 6.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCC(O)CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252494 101425 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 489 10 1 5 6.3 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCC(O)CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
20780154 74328 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 596 9 0 4 8.6 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3ccc(C(C)C)cc3Br)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL189798 74328 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 596 9 0 4 8.6 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3ccc(C(C)C)cc3Br)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
20780272 70613 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 430 7 0 4 5.6 CCCN(Cc1ccccc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL180284 70613 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 430 7 0 4 5.6 CCCN(Cc1ccccc1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780061 100104 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 455 9 0 7 4.3 COCCN(CCOC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL245298 100104 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 455 9 0 7 4.3 COCCN(CCOC)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
11257259 75099 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 371 10 0 4 5.5 CCCC(CCC)N1CCc2cn(CCCOC(C)C)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL191650 75099 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 371 10 0 4 5.5 CCCC(CCC)N1CCc2cn(CCCOC(C)C)c3nc(C)cc1c23 10.1021/jm050070m
10946918 210457 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 312 4 2 4 3.6 CC(=O)/C(=N\Nc1ccccc1C#N)Nc1cccc(Cl)c1 10.1021/jm025512y
CHEMBL67448 210457 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 312 4 2 4 3.6 CC(=O)/C(=N\Nc1ccccc1C#N)Nc1cccc(Cl)c1 10.1021/jm025512y
10500311 66545 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 385 8 0 9 1.9 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)nc1C 10.1021/jm980224g
CHEMBL172570 66545 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 385 8 0 9 1.9 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)nc1C 10.1021/jm980224g
11045497 109168 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 4.4 CC(=O)/C(=N\Nc1ccccc1Cl)Nc1cccc(Cl)c1 10.1021/jm025512y
CHEMBL303931 109168 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 321 4 2 3 4.4 CC(=O)/C(=N\Nc1ccccc1Cl)Nc1cccc(Cl)c1 10.1021/jm025512y
11502109 129127 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 394 7 0 4 4.8 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL359956 129127 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 394 7 0 4 4.8 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
44446723 101581 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 378 8 0 4 5.9 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253492 101581 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 378 8 0 4 5.9 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
44389111 179216 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.4 CCCN(Cc1ccccc1F)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL447836 179216 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.4 CCCN(Cc1ccccc1F)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44385503 68108 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 461 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL176721 68108 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 461 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
44341949 117567 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 318 6 0 2 5.8 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL326074 117567 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 318 6 0 2 5.8 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)cccc12 10.1016/s0960-894x(03)00684-x
10206448 71344 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 485 9 1 4 7.9 CCCN(CCC1CC1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181566 71344 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 485 9 1 4 7.9 CCCN(CCC1CC1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780033 71609 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 448 7 0 4 5.7 CCCN(Cc1cccc(F)c1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181989 71609 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 448 7 0 4 5.7 CCCN(Cc1cccc(F)c1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780075 74014 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 8.2 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL187975 74014 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 8.2 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC(F)(F)F)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
11155555 85118 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL2093959 85118 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL2110007 85118 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
10402860 109902 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 305 4 2 3 3.7 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1Cl 10.1021/jm025512y
CHEMBL307795 109902 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 305 4 2 3 3.7 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1Cl 10.1021/jm025512y
11778680 210485 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 285 4 2 3 3.4 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1C 10.1021/jm025512y
CHEMBL67603 210485 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 285 4 2 3 3.4 CC(=O)/C(=N\c1cccc(F)c1)NNc1ccccc1C 10.1021/jm025512y
44347421 23202 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 414 10 0 8 3.1 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL123197 23202 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 414 10 0 8 3.1 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(OC)cc3OC)c(C)nn12 10.1016/j.bmcl.2004.05.019
9828535 172340 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980223o
CHEMBL424204 172340 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980223o
CHEMBL43216 172340 0 None -1 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 437 6 0 8 3.0 CCN(c1nc(C)nc(N2CCOCC2)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980223o
21916338 13343 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 7 0 4 7.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083035 13343 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 7 0 4 7.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780150 151878 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 429 8 0 5 5.9 CCCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL391170 151878 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 429 8 0 5 5.9 CCCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
10164617 71246 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 511 7 1 4 7.6 FC(F)(F)CN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL181381 71246 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 511 7 1 4 7.6 FC(F)(F)CN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
46890888 13298 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccccn4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082807 13298 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccccn4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
10477079 101216 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 417 8 1 5 5.8 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cccc(C)c2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL251199 101216 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 417 8 1 5 5.8 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cccc(C)c2)nc1CC 10.1016/j.bmcl.2007.09.008
44317800 211993 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 362 7 1 3 5.2 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(F)c1 10.1021/jm049974i
CHEMBL78608 211993 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 362 7 1 3 5.2 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(F)c1 10.1021/jm049974i
9865434 74804 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccccc3OC)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL191395 74804 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 394 7 0 6 4.3 CCCC(CCC)N1CCn2c(=O)n(-c3ccccc3OC)c3nc(C)cc1c32 10.1021/jm050384+
10526779 64903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 1 4 6.7 CCC(CC)CNc1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL167738 64903 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 1 4 6.7 CCC(CC)CNc1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10763375 122122 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 397 3 0 5 5.5 Cc1nc(N(C)c2ccccc2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1021/jm9904351
CHEMBL334935 122122 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 397 3 0 5 5.5 Cc1nc(N(C)c2ccccc2)n2nc(C)c(-c3ccc(Cl)cc3Cl)c2n1 10.1021/jm9904351
CHEMBL2372938 217098 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)C(CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
21916309 14045 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 530 7 0 4 7.1 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC(F)(F)C(F)(F)F 10.1016/j.bmcl.2010.04.094
CHEMBL1085989 14045 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 530 7 0 4 7.1 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC(F)(F)C(F)(F)F 10.1016/j.bmcl.2010.04.094
11486120 69768 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 390 10 0 5 5.3 CCCCC(CC)N(CC1CC1)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL178618 69768 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 390 10 0 5 5.3 CCCCC(CC)N(CC1CC1)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
21916155 14278 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 424 3 0 5 4.9 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCSCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087174 14278 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 424 3 0 5 4.9 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN2CCSCC2)c(C)c1 10.1016/j.bmcl.2010.01.127
10739049 64545 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 387 2 0 3 5.7 Cc1cc(Cl)nc2c1c(C#N)cn2-c1ccc(C(C)C)cc1Br 10.1021/jm980223o
CHEMBL166946 64545 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 387 2 0 3 5.7 Cc1cc(Cl)nc2c1c(C#N)cn2-c1ccc(C(C)C)cc1Br 10.1021/jm980223o
54586411 68426 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to CRHRBinding affinity to CRHR
ChEMBL 387 5 1 5 4.6 CCN(CCN)c1nc(C)nc2c1c1ccccc1n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.12.116
CHEMBL1771267 68426 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to CRHRBinding affinity to CRHR
ChEMBL 387 5 1 5 4.6 CCN(CCN)c1nc(C)nc2c1c1ccccc1n2-c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.12.116
CHEMBL2372900 217084 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
9870876 71385 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 506 7 0 6 7.8 CCC(C)N(c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br)C(C)CC 10.1016/s0960-894x(99)00159-6
CHEMBL18173 71385 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 506 7 0 6 7.8 CCC(C)N(c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br)C(C)CC 10.1016/s0960-894x(99)00159-6
10316753 67265 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 364 7 1 3 5.2 CCCN(c1n[nH]c(-c2ccc(Cl)cc2Cl)n1)C(C1CC1)C1CC1 10.1021/jm049339c
CHEMBL175536 67265 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 364 7 1 3 5.2 CCCN(c1n[nH]c(-c2ccc(Cl)cc2Cl)n1)C(C1CC1)C1CC1 10.1021/jm049339c
10025032 162017 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2ccc(C)cn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL402717 162017 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2ccc(C)cn2)nc1CC 10.1016/j.bmcl.2007.09.008
20780068 130864 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 536 8 0 4 7.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC4CC4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL363281 130864 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 536 8 0 4 7.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC4CC4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
10549751 127213 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 414 3 0 6 4.4 Cc1nc(N2CCCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
CHEMBL353856 127213 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 414 3 0 6 4.4 Cc1nc(N2CCCCC2)c2nnn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980224g
44341777 16980 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 416 7 0 4 6.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL115999 16980 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 416 7 0 4 6.4 CCCN(CC1CC1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
10831554 64809 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 347 4 0 3 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980223o
CHEMBL167264 64809 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 347 4 0 3 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980223o
10831554 64809 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 347 4 0 3 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
CHEMBL167264 64809 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 347 4 0 3 5.1 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)C)cc1Br 10.1021/jm980222w
10155816 70762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 366 7 0 3 6.1 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1OC(CC)CC 10.1021/jm200365y
CHEMBL1807028 70762 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 366 7 0 3 6.1 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1OC(CC)CC 10.1021/jm200365y
18672272 69267 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.0 FC(F)(F)CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL178081 69267 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 525 8 1 4 8.0 FC(F)(F)CCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
11247792 85119 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL2093960 85119 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL2110008 85119 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCC[C@H](c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
11383383 130719 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 10 0 5 5.3 CCCCC(CC)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL362847 130719 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 10 0 5 5.3 CCCCC(CC)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
11154954 74751 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 442 7 0 7 3.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(S(C)(=O)=O)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL191188 74751 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 442 7 0 7 3.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(S(C)(=O)=O)cc3)c3nc(C)cc1c32 10.1021/jm050384+
23000016 16338 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 301 1 0 1 5.8 Cc1cc(C)c2cccc(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(03)00684-x
CHEMBL112389 16338 1 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 301 1 0 1 5.8 Cc1cc(C)c2cccc(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(03)00684-x
44306185 109580 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 367 9 0 5 4.6 CCCN(c1nccc(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL305354 109580 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 367 9 0 5 4.6 CCCN(c1nccc(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
44352436 123772 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 437 8 1 4 6.8 CCCN(Cc1sc(Nc2ccc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL338780 123772 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 437 8 1 4 6.8 CCCN(Cc1sc(Nc2ccc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44387214 67580 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 458 7 0 5 5.5 CCCCN(CC)c1nc(C)cc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL176176 67580 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 458 7 0 5 5.5 CCCCN(CC)c1nc(C)cc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
44443605 100849 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 378 8 2 6 4.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(CO)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL249012 100849 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 378 8 2 6 4.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(CO)c1ccccc1 10.1016/j.bmcl.2007.09.008
44317728 112385 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 432 7 1 3 6.4 Cc1ccccc1C(Nc1ccc(Cl)cc1C(F)(F)F)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL312239 112385 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 432 7 1 3 6.4 Cc1ccccc1C(Nc1ccc(Cl)cc1C(F)(F)F)C(=O)CCc1ccncc1 10.1021/jm049974i
44318109 212783 0 None - 1 Human 7.3 pKi = 7.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 8 0 5 5.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(C(C)C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL84892 212783 0 None - 1 Human 7.3 pKi = 7.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 385 8 0 5 5.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(C(C)C)c1=O 10.1016/s0960-894x(03)00483-9
10497535 65886 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 342 2 0 2 5.5 Cc1cc(C)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL169784 65886 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 342 2 0 2 5.5 Cc1cc(C)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
44384780 66551 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 461 7 0 7 3.8 CCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL172606 66551 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 461 7 0 7 3.8 CCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
22324333 112397 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 359 8 0 6 3.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL312336 112397 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 359 8 0 6 3.4 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
44392776 72045 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 373 5 0 4 5.4 CCN(c1ccccc1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182825 72045 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 373 5 0 4 5.4 CCN(c1ccccc1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
46891115 13581 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 418 7 0 4 5.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)ccn12)CC1CC1 10.1016/j.bmcl.2010.04.094
CHEMBL1083920 13581 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 418 7 0 4 5.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)ccn12)CC1CC1 10.1016/j.bmcl.2010.04.094
11032842 210871 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 267 4 2 3 3.2 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1 10.1021/jm025512y
CHEMBL70195 210871 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 267 4 2 3 3.2 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1 10.1021/jm025512y
44443642 174315 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cccc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL430019 174315 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cccc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
10623894 65904 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 10 0 9 2.8 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
CHEMBL169841 65904 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 10 0 9 2.8 COCCN(CCOC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
11796523 127152 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 422 8 0 6 4.6 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(OC)cc2OC)n1 10.1021/jm980222w
CHEMBL353296 127152 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 422 8 0 6 4.6 CCN(CC)c1cc(C)nc(N(CC)c2c(Br)cc(OC)cc2OC)n1 10.1021/jm980222w
44380639 127585 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 381 3 0 3 4.6 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2I)n1 10.1021/jm980223o
CHEMBL355624 127585 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 381 3 0 3 4.6 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2I)n1 10.1021/jm980223o
20780051 100648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 483 5 0 5 6.5 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4Cc4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL247958 100648 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 483 5 0 5 6.5 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4Cc4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
21916263 12360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 420 7 0 4 5.8 C=CCN(CCC)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1077156 12360 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 420 7 0 4 5.8 C=CCN(CCC)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
44381252 127260 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 493 10 0 10 2.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1N(C)C 10.1021/jm980224g
CHEMBL354280 127260 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 493 10 0 10 2.5 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1c(Br)cc(OC)cc1N(C)C 10.1021/jm980224g
44381175 65645 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 495 8 0 8 4.5 COCCN(Cc1cccnc1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168858 65645 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 495 8 0 8 4.5 COCCN(Cc1cccnc1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
127033837 145406 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3901 126 54 50 -8.8 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)C1CCSSCCC(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775831 145406 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3901 126 54 50 -8.8 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)C1CCSSCCC(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)NC(C)(C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL2372937 217097 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)C(CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
127034112 145387 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4252 133 59 54 -8.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)C1CCSSCCC(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)NC(Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775707 145387 0 None -1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 4252 133 59 54 -8.7 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)C1CCSSCCC(NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)NC(Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
44392775 131425 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 6 4.6 CCCN(CC1CC1)c1cc(C(C)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL364117 131425 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 6 4.6 CCCN(CC1CC1)c1cc(C(C)c2c(OC)cc(OC)cc2OC)nc(C)n1 10.1016/j.bmcl.2004.05.072
46890768 13503 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 6 0 4 7.1 CCN(Cc1ccccc1C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1083720 13503 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 6 0 4 7.1 CCN(Cc1ccccc1C)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
53310276 70757 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 380 7 1 4 4.9 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(C)CN(C)C 10.1021/jm200365y
CHEMBL1807023 70757 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 380 7 1 4 4.9 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1NC(C)CN(C)C 10.1021/jm200365y
19063905 209748 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 399 7 0 3 5.6 CCCN(c1ncc(C)c(-c2ccc(Br)cc2)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63029 209748 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 399 7 0 3 5.6 CCCN(c1ncc(C)c(-c2ccc(Br)cc2)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
21916094 13344 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 560 7 0 4 7.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4cccc(F)c4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083036 13344 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 560 7 0 4 7.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC(F)(F)F)Cc4cccc(F)c4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11387007 175617 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 530 8 1 7 6.3 COC(=O)c1cccc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)c1 10.1016/j.bmcl.2005.10.097
CHEMBL437893 175617 1 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 530 8 1 7 6.3 COC(=O)c1cccc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)c1 10.1016/j.bmcl.2005.10.097
44446728 101611 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 362 7 0 3 6.2 CCCN(CCC)c1cnc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253701 101611 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 362 7 0 3 6.2 CCCN(CCC)c1cnc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
11175998 140396 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 364 4 0 4 5.0 CCCCN1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL371367 140396 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 364 4 0 4 5.0 CCCCN1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
10547488 109853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 375 7 1 5 5.3 CCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL307419 109853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 375 7 1 5 5.3 CCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10808133 170200 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 355 9 1 5 5.3 CCCCN(CCCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL419636 170200 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 355 9 1 5 5.3 CCCCN(CCCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
10547488 109853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 375 7 1 5 5.3 CCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL307419 109853 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 375 7 1 5 5.3 CCCN(Cc1ccccc1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
10808133 170200 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 355 9 1 5 5.3 CCCCN(CCCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL419636 170200 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 355 9 1 5 5.3 CCCCN(CCCC)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
9931738 67943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 416 8 0 8 3.2 COCCN(CCOC)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL17656 67943 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 416 8 0 8 3.2 COCCN(CCOC)c1nc(C)nc2c1sc(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
10646276 64316 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 429 8 0 5 5.4 C=CCN(c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1)C1CC1 10.1021/jm980222w
CHEMBL166345 64316 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 429 8 0 5 5.4 C=CCN(c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1)C1CC1 10.1021/jm980222w
10694122 64322 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 433 9 0 5 5.9 CCCCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL166388 64322 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 433 9 0 5 5.9 CCCCN(CC)c1nc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10809708 64463 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 378 5 0 5 4.1 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(N(C)C)cc1OC 10.1021/jm980222w
CHEMBL166895 64463 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 378 5 0 5 4.1 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(N(C)C)cc1OC 10.1021/jm980222w
11795557 64614 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 5 4.8 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
CHEMBL167177 64614 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 404 7 0 5 4.8 CCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
10503074 64868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 436 9 0 6 5.0 CCCN(CC1CC1)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL167428 64868 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 436 9 0 6 5.0 CCCN(CC1CC1)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
11796930 127218 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 8 0 4 6.2 CCCN(c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1)C1CC1 10.1021/jm980222w
CHEMBL353877 127218 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 430 8 0 4 6.2 CCCN(c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1)C1CC1 10.1021/jm980222w
10646531 127252 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 435 9 0 7 4.6 CCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL354178 127252 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 435 9 0 7 4.6 CCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
10838302 127269 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 475 9 0 6 5.6 CCCCN(CC)c1nc(C)nc(N(CC)c2ccc(OC(F)(F)F)cc2Br)n1 10.1021/jm980222w
CHEMBL354367 127269 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 475 9 0 6 5.6 CCCCN(CC)c1nc(C)nc(N(CC)c2ccc(OC(F)(F)F)cc2Br)n1 10.1021/jm980222w
10527467 127272 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 448 9 0 6 5.0 CCN(c1nc(C)nc(N(CC2CC2)CC2CC2)n1)c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980222w
CHEMBL354395 127272 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 448 9 0 6 5.0 CCN(c1nc(C)nc(N(CC2CC2)CC2CC2)n1)c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980222w
10366978 108162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 7 0 6 4.9 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL297170 108162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 7 0 6 4.9 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
9935525 65400 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 494 8 0 7 5.1 COCCN(Cc1ccccc1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168449 65400 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 494 8 0 7 5.1 COCCN(Cc1ccccc1)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11759092 16808 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 321 1 0 1 6.2 Cc1cc(Cl)c2cccc(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(03)00684-x
CHEMBL115119 16808 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 321 1 0 1 6.2 Cc1cc(Cl)c2cccc(-c3ccc(Cl)cc3Cl)c2n1 10.1016/s0960-894x(03)00684-x
9907170 184878 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980223o
CHEMBL46479 184878 0 None 2 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 365 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(OC)cc1OC 10.1021/jm980223o
10366978 108162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 459 7 0 6 4.9 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
CHEMBL297170 108162 0 None - 1 Human 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 459 7 0 6 4.9 CCCCN(CC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
9800614 107243 5 None - 1 Human 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm990590f
CHEMBL290762 107243 5 None - 1 Human 8.3 pKi = 8.3 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors.
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm990590f
3520 10041 54 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/s0960-894x(02)00358-x
9821250 10041 54 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/s0960-894x(02)00358-x
CHEMBL309138 10041 54 None 1 2 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1016/s0960-894x(02)00358-x
9800614 107243 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL290762 107243 5 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 390 6 0 4 5.9 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
137659453 165900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]o-CRF from recombinant human CRF1 receptor expressed in CHO cellsDisplacement of [125I]o-CRF from recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 432 9 0 4 7.0 CCCCc1nn2c(N(CC)CCCC)cc(C)nc2c1-c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2016.11.019
CHEMBL4097805 165900 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]o-CRF from recombinant human CRF1 receptor expressed in CHO cellsDisplacement of [125I]o-CRF from recombinant human CRF1 receptor expressed in CHO cells
ChEMBL 432 9 0 4 7.0 CCCCc1nn2c(N(CC)CCCC)cc(C)nc2c1-c1ccc(Cl)cc1Cl 10.1016/j.ejmech.2016.11.019
44446730 162339 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 388 7 0 3 6.5 CCCN(CC1CC1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL404351 162339 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 388 7 0 3 6.5 CCCN(CC1CC1)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
10375 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm049085v
9888194 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm049085v
CHEMBL188907 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 10.1021/jm049085v
9933199 78281 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 444 8 0 4 7.3 CCCCC(CCCC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
CHEMBL196270 78281 1 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 444 8 0 4 7.3 CCCCC(CCCC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
11718607 142000 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 4 0 4 6.0 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](C(C)C)N2CC1CC1 10.1021/jm049085v
CHEMBL372319 142000 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 414 4 0 4 6.0 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](C(C)C)N2CC1CC1 10.1021/jm049085v
9824168 74407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 432 6 0 5 5.6 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190488 74407 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 432 6 0 5 5.6 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm050384+
10837003 66572 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 8 1 5 6.4 CCCCC(CC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL172684 66572 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 443 8 1 5 6.4 CCCCC(CC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341862 16310 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112264 16310 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 8 0 4 6.3 CCCCN(CCCC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)nn(C)c12 10.1016/s0960-894x(03)00622-x
12086065 17607 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 7 0 5 5.1 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL117209 17607 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 7 0 5 5.1 CCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
10693263 65853 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 6 1 6 5.0 CCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169577 65853 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 416 6 1 6 5.0 CCC(CC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10549179 127594 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 403 8 0 7 4.4 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
CHEMBL355721 127594 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 403 8 0 7 4.4 CCCCN(CC)c1nc(C)nc2c1ncn2-c1c(Cl)cc(OC)cc1OC 10.1021/jm980224g
20780267 13590 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 492 6 0 4 6.5 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1083933 13590 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 492 6 0 4 6.5 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11386550 85105 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL2094043 85105 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
CHEMBL2109791 85105 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 466 8 0 5 6.5 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)[C@@H](CC)c1ccc(C(F)(F)F)cc1 10.1021/jm049339c
11383860 73797 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
CHEMBL187039 73797 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 394 7 0 6 4.7 CCCN(CCC)c1cc(C)nc2c(-c3c(C)cc(N(C)C)nc3C)c(C)nn12 10.1021/jm040058e
11201203 134057 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 7 0 6 5.2 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL365841 134057 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 428 7 0 6 5.2 CCCN(Cc1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
20780254 13598 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 7 0 4 6.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CCC1 10.1016/j.bmcl.2010.04.094
CHEMBL1083952 13598 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 7 0 4 6.7 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CCC1 10.1016/j.bmcl.2010.04.094
122193719 130738 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 386 6 1 4 5.1 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1C 10.1016/j.bmcl.2015.10.010
CHEMBL3628738 130738 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 386 6 1 4 5.1 CCCCN(CC)c1cc(C)nc2c1NC(=O)CN2c1ccc(Cl)cc1C 10.1016/j.bmcl.2015.10.010
11362799 78047 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 408 8 0 6 5.1 CCCC(CCC)N1CCc2cn(-c3ccc(OC)nc3OC)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL195699 78047 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 408 8 0 6 5.1 CCCC(CCC)N1CCc2cn(-c3ccc(OC)nc3OC)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL386892 219178 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC1CCCCC1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
10178818 70720 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 395 8 1 4 5.9 CCc1nc(-c2ccc(C(F)(F)F)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806734 70720 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 395 8 1 4 5.9 CCc1nc(-c2ccc(C(F)(F)F)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
11372928 177049 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 7 0 6 4.5 CCCN(CCC)c1c(F)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL444614 177049 0 None - 1 Human 8.3 pKi = 8.3 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 398 7 0 6 4.5 CCCN(CCC)c1c(F)c(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10205521 175283 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 471 7 0 6 4.9 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL435345 175283 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 471 7 0 6 4.9 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10593122 65537 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 338 5 1 6 4.0 CCC(CC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL168664 65537 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 338 5 1 6 4.0 CCC(CC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
44341636 16467 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 386 6 0 2 7.1 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL113097 16467 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 386 6 0 2 7.1 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
44341743 117360 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 418 8 0 4 5.6 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL325430 117360 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 418 8 0 4 5.6 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)cccc12 10.1016/s0960-894x(03)00684-x
11165678 85121 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2093962 85121 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2110010 85121 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
18691320 11511 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 513 4 0 3 7.2 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(Br)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10373 11511 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 513 4 0 3 7.2 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1ccc(Br)cc1Br 10.1016/s0960-894x(99)00132-8
18691324 103781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 434 5 0 4 6.4 CCN(c1nc(C)cc(-c2ccccc2C#N)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL266617 103781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 434 5 0 4 6.4 CCN(c1nc(C)cc(-c2ccccc2C#N)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10813902 64907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 9 0 7 4.1 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL167777 64907 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 461 9 0 7 4.1 COCCN(CCOC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
22249149 70769 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 367 7 1 4 5.6 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807035 70769 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 367 7 1 4 5.6 CCc1nc(NC(CC)CC)c(OC)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
9969024 70786 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 363 8 1 5 5.1 CCOc1ccc(-c2nc(OC)c(NC(CC)CC)nc2C)c(Cl)c1 10.1021/jm200365y
CHEMBL1807056 70786 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 363 8 1 5 5.1 CCOc1ccc(-c2nc(OC)c(NC(CC)CC)nc2C)c(Cl)c1 10.1021/jm200365y
21916308 100573 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 485 8 0 5 6.7 CCCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247557 100573 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 485 8 0 5 6.7 CCCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL4299287 220339 0 None -2 2 Human 8.2 pKi = 8.2 Binding
Displacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1]-PD-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL None None None CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H]1CCCCNC(=O)CC[C@@H](NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](C)NC(=O)C(C)(CC(C)C)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](C)NC(=O)C(CCCC)NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](NC(=O)[C@@H](CCC(=O)O)NC(=O)[C@@H](CCCNC(=N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(=O)O)NC(C)=O)[C@H](C)O)C(C)C)C(=O)N[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)C(=O)N[C@@H](Cc2ccc(NC(N)=O)cc2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)NC(C)(CC(C)C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL2372922 217092 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H](C(N)=O)[C@@H](C)CC)[C@@H](C)CC 10.1021/jm034180+
20780182 100614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 7 0 5 5.9 CCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL247753 100614 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 435 7 0 5 5.9 CCN(CCC1CC1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
10166565 71097 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 561 8 1 4 8.5 FC(F)(F)CN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181133 71097 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 561 8 1 4 8.5 FC(F)(F)CN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11598824 78559 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 404 5 0 5 5.0 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CCOC 10.1021/jm049085v
CHEMBL196740 78559 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 404 5 0 5 5.0 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CCOC 10.1021/jm049085v
11660986 147040 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 384 4 0 4 5.2 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL380563 147040 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 384 4 0 4 5.2 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
10157369 122035 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 391 5 1 4 5.6 CCN(CC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL334778 122035 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 391 5 1 4 5.6 CCN(CC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
11610200 78506 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 2 0 4 4.9 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1C 10.1021/jm049085v
CHEMBL196594 78506 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 2 0 4 4.9 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1C 10.1021/jm049085v
9928790 200334 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 359 9 0 6 4.1 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL526828 200334 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 359 9 0 6 4.1 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
11742775 161554 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2ncccc2C)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL400156 161554 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2ncccc2C)nc1CC 10.1016/j.bmcl.2007.09.008
11067569 210402 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 332 5 2 5 3.5 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccccc1[N+](=O)[O-] 10.1021/jm025512y
CHEMBL67121 210402 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 332 5 2 5 3.5 CC(=O)/C(=N\c1cccc(Cl)c1)NNc1ccccc1[N+](=O)[O-] 10.1021/jm025512y
10786789 65274 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 393 5 0 4 5.9 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(C(C)C)cc1SC 10.1021/jm980222w
CHEMBL168341 65274 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 393 5 0 4 5.9 CCN(c1nc(C)cc(C)n1)c1c(Br)cc(C(C)C)cc1SC 10.1021/jm980222w
44443654 100842 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 437 9 1 7 4.6 CCc1nc(Oc2cc(C)ncn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
CHEMBL248996 100842 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 437 9 1 7 4.6 CCc1nc(Oc2cc(C)ncn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCF 10.1016/j.bmcl.2007.09.008
11474841 85120 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2093961 85120 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2110009 85120 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
44352358 25518 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 429 10 1 6 5.5 CCCN(Cc1sc(Nc2ccc(OC)cc2OC)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL127783 25518 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 429 10 1 6 5.5 CCCN(Cc1sc(Nc2ccc(OC)cc2OC)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44392759 72015 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 393 7 0 4 5.5 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)c(C)c(C)c(C)c2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182705 72015 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 393 7 0 4 5.5 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)c(C)c(C)c(C)c2C)c1C 10.1016/j.bmcl.2004.05.072
10299169 139189 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 473 6 1 5 6.5 COC[C@@H]1CCCN1Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL369754 139189 0 None - 1 Human 5.3 pKi = 5.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 473 6 1 5 6.5 COC[C@@H]1CCCN1Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
10297799 25702 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 451 9 1 6 4.9 COCCN(CCOC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL128566 25702 0 None - 1 Human 4.3 pKi = 4.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 451 9 1 6 4.9 COCCN(CCOC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
44305179 210144 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 322 6 0 4 4.6 CCCCN(CC)c1cc(C)nc2c(-c3ccccc3)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL65195 210144 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 322 6 0 4 4.6 CCCCN(CC)c1cc(C)nc2c(-c3ccccc3)c(C)nn12 10.1016/s0960-894x(98)00372-2
44460546 212116 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 416 7 1 3 6.2 Cc1cc(F)ccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL79576 212116 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 416 7 1 3 6.2 Cc1cc(F)ccc1C(Nc1ccc(Cl)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
44460368 212430 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 490 6 2 3 6.8 CC(=O)Nc1cccc(C(=O)C(Nc2ccc(Cl)cc2Cl)c2ccccc2Br)c1 10.1021/jm049974i
CHEMBL81912 212430 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 490 6 2 3 6.8 CC(=O)Nc1cccc(C(=O)C(Nc2ccc(Cl)cc2Cl)c2ccccc2Br)c1 10.1021/jm049974i
44407864 82183 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 4 1 4 5.5 Cc1cccc(S(=O)(=O)c2c(C)cc(C)nc2Nc2c(C)cc(C)cc2C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL204014 82183 0 None - 1 Rat 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 4 1 4 5.5 Cc1cccc(S(=O)(=O)c2c(C)cc(C)nc2Nc2c(C)cc(C)cc2C)c1 10.1016/j.bmcl.2005.10.097
44341902 16940 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 348 7 0 3 5.8 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115928 16940 1 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 348 7 0 3 5.8 CCCN(CCC)c1cc(C)nc2c(-c3ccc(OC)cc3)cccc12 10.1016/s0960-894x(03)00684-x
11418006 82327 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 5 1 4 5.5 CCc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
CHEMBL204481 82327 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 394 5 1 4 5.5 CCc1ccc(S(=O)(=O)c2ccc(C)nc2Nc2c(C)cc(C)cc2C)cc1 10.1016/j.bmcl.2005.10.097
44446739 101424 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 488 10 0 5 6.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCN(C)CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL252493 101424 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 488 10 0 5 6.1 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OCCN2CCN(C)CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
11065415 210205 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 267 4 2 3 3.2 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C 10.1021/jm025512y
CHEMBL65708 210205 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 267 4 2 3 3.2 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1C 10.1021/jm025512y
11022343 210449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 281 4 2 3 3.5 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1C 10.1021/jm025512y
CHEMBL67394 210449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 281 4 2 3 3.5 CC(=O)/C(=N\c1cccc(C)c1)NNc1ccccc1C 10.1021/jm025512y
20780067 74663 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 6 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CCC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL191052 74663 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 6 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CCC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
21916146 13264 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 8 0 4 6.7 CCCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1082697 13264 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 466 8 0 4 6.7 CCCN(CCC1CC1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
10410573 101155 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 9 1 6 5.5 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(CC)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL250814 101155 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 432 9 1 6 5.5 CCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(CC)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
44587492 200408 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 10 0 5 5.5 CCCOc1nc(-c2c(C)cc(C)cc2OC)nc(C)c1N(CCC)CCC 10.1016/j.bmcl.2008.07.063
CHEMBL527030 200408 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 10 0 5 5.5 CCCOc1nc(-c2c(C)cc(C)cc2OC)nc(C)c1N(CCC)CCC 10.1016/j.bmcl.2008.07.063
22324332 113754 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 359 8 0 6 3.4 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL315112 113754 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 359 8 0 6 3.4 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
44392739 71465 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 6 1 6 4.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(O)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL181860 71465 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 6 1 6 4.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(O)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44443595 179429 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 390 8 1 5 5.9 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(c1ccccc1)C(C)C 10.1016/j.bmcl.2007.09.008
CHEMBL449657 179429 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 390 8 1 5 5.9 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(c1ccccc1)C(C)C 10.1016/j.bmcl.2007.09.008
11046479 109891 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 355 4 2 3 4.8 CC(=O)/C(=N\Nc1ccccc1C(F)(F)F)Nc1cccc(Cl)c1 10.1021/jm025512y
CHEMBL307751 109891 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 355 4 2 3 4.8 CC(=O)/C(=N\Nc1ccccc1C(F)(F)F)Nc1cccc(Cl)c1 10.1021/jm025512y
20780105 74798 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 8 0 4 7.8 CC(C)c1ccc(-n2c3ccccc3n3c(CN(CC4CC4)CC4CC4)c(C(F)(F)F)nc23)c(Br)c1 10.1016/j.bmcl.2005.06.028
CHEMBL191366 74798 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 8 0 4 7.8 CC(C)c1ccc(-n2c3ccccc3n3c(CN(CC4CC4)CC4CC4)c(C(F)(F)F)nc23)c(Br)c1 10.1016/j.bmcl.2005.06.028
10708209 64286 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 284 4 0 4 3.6 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1C 10.1021/jm980222w
CHEMBL166110 64286 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 284 4 0 4 3.6 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1C 10.1021/jm980222w
22249007 70772 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 351 6 1 3 5.9 CCc1nc(NC(CC)CC)c(C)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807038 70772 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 351 6 1 3 5.9 CCc1nc(NC(CC)CC)c(C)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
18691311 11818 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 457 7 0 6 5.4 CCN(c1nc(C)cc(-c2ccccc2OC)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL10526 11818 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 457 7 0 6 5.4 CCN(c1nc(C)cc(-c2ccccc2OC)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
44392800 139182 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 355 7 1 5 3.5 CCCN(CCO)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL369717 139182 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 355 7 1 5 3.5 CCCN(CCO)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
22249074 70765 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 337 6 1 3 5.6 CCc1nc(NC(CC)CC)cnc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807031 70765 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 337 6 1 3 5.6 CCc1nc(NC(CC)CC)cnc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
44460272 212476 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound towards human corticotropin releasing factor (h-CRF1) receptor showed a 2-fold activity in racemic mixtureBinding affinity of compound towards human corticotropin releasing factor (h-CRF1) receptor showed a 2-fold activity in racemic mixture
ChEMBL 442 7 1 3 6.2 Cc1ccc(N[C@@H](C(=O)CCc2ccncc2)c2ccccc2Br)c(Cl)c1 10.1021/jm049974i
CHEMBL82308 212476 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity of compound towards human corticotropin releasing factor (h-CRF1) receptor showed a 2-fold activity in racemic mixtureBinding affinity of compound towards human corticotropin releasing factor (h-CRF1) receptor showed a 2-fold activity in racemic mixture
ChEMBL 442 7 1 3 6.2 Cc1ccc(N[C@@H](C(=O)CCc2ccncc2)c2ccccc2Br)c(Cl)c1 10.1021/jm049974i
44443630 161507 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL399877 161507 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 418 8 1 6 5.2 CCO[C@H]1Cc2ccccc2[C@@H]1Nc1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
44392691 73077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 379 8 0 4 5.1 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1CC 10.1016/j.bmcl.2004.05.072
CHEMBL184851 73077 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 379 8 0 4 5.1 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1CC 10.1016/j.bmcl.2004.05.072
11156095 75749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 377 7 0 4 5.7 CCCC(CCC)N1CCc2cn(-c3ccccc3OC)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL192288 75749 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 377 7 0 4 5.7 CCCC(CCC)N1CCc2cn(-c3ccccc3OC)c3nc(C)cc1c23 10.1021/jm050070m
10835652 125955 0 None - 1 Human 4.3 pKi = 4.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 415 7 2 5 5.7 CCc1cccc(CC)c1Nc1nc(C)nc(NCc2ccc(C(F)(F)F)cc2)n1 10.1021/jm960148m
CHEMBL343073 125955 0 None - 1 Human 4.3 pKi = 4.3 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 415 7 2 5 5.7 CCc1cccc(CC)c1Nc1nc(C)nc(NCc2ccc(C(F)(F)F)cc2)n1 10.1021/jm960148m
44389084 129094 0 None - 1 Human 4.3 pKi = 4.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 443 4 1 4 6.9 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CCCCC1 10.1016/j.bmcl.2004.10.055
CHEMBL359828 129094 0 None - 1 Human 4.3 pKi = 4.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 443 4 1 4 6.9 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CCCCC1 10.1016/j.bmcl.2004.10.055
10164848 28250 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 517 10 0 4 7.8 CCCN(Cc1sc(N(CC)c2ccc(C(C)C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL131571 28250 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 517 10 0 4 7.8 CCCN(Cc1sc(N(CC)c2ccc(C(C)C)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
3495 7958 28 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(98)00372-2
5311055 7958 28 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(98)00372-2
CHEMBL9946 7958 28 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 364 6 0 4 5.6 CCCCN(c1nc(C)nc2c1c(C)cn2c1c(C)cc(cc1C)C)CC 10.1016/s0960-894x(98)00372-2
136029158 212449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 357 8 1 5 4.7 CCCN(CCC)c1c(O)nc(-c2c(C)cc(C)cc2OC)nc1CC 10.1016/s0960-894x(03)00483-9
CHEMBL82112 212449 0 None - 1 Human 6.3 pKi = 6.3 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 357 8 1 5 4.7 CCCN(CCC)c1c(O)nc(-c2c(C)cc(C)cc2OC)nc1CC 10.1016/s0960-894x(03)00483-9
44392751 128834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 397 10 0 6 4.5 C=C(c1cc(N(CCC)CC2CC2)nc(C)n1)c1c(OC)cc(OC)cc1OC 10.1016/j.bmcl.2004.05.072
CHEMBL359636 128834 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 397 10 0 6 4.5 C=C(c1cc(N(CCC)CC2CC2)nc(C)n1)c1c(OC)cc(OC)cc1OC 10.1016/j.bmcl.2004.05.072
10206904 129544 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 493 7 1 4 7.5 CN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL360471 129544 0 None - 1 Human 6.3 pKi = 6.3 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 493 7 1 4 7.5 CN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
21916237 100135 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 441 8 1 7 4.0 COCC(COC)NCc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL245506 100135 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 441 8 1 7 4.0 COCC(COC)NCc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44308134 210341 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 460 7 0 6 5.3 CCCN(CCN1CCCCC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL66671 210341 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 460 7 0 6 5.3 CCCN(CCN1CCCCC1)c1nc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44587452 194925 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 327 7 0 4 4.7 CCCN(CCC)c1cnc(-c2c(C)cc(C)cc2OC)nc1C 10.1016/j.bmcl.2008.07.063
CHEMBL498480 194925 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 327 7 0 4 4.7 CCCN(CCC)c1cnc(-c2c(C)cc(C)cc2OC)nc1C 10.1016/j.bmcl.2008.07.063
9797993 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960149e
CHEMBL306618 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960149e
9797993 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
CHEMBL306618 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm960148m
9797993 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
CHEMBL306618 109757 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 339 7 1 5 4.5 CCCN(CC1CC1)c1nc(C)nc(Nc2c(C)cc(C)cc2C)n1 10.1021/jm9900117
18672241 71140 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 455 8 1 4 7.0 C=CCN(CC=C)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181280 71140 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 455 8 1 4 7.0 C=CCN(CC=C)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780125 130652 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 442 7 0 4 6.0 CCCN(CC1CC1)C(=O)c1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL362706 130652 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 442 7 0 4 6.0 CCCN(CC1CC1)C(=O)c1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
20780058 100103 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4cccnc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL245297 100103 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 458 6 0 6 5.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN(C)CCc4cccnc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
10062901 177023 1 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 291 2 0 3 3.6 Cc1cc(C)nc(N(C)c2ccccc2Br)n1 10.1021/jm980222w
CHEMBL444577 177023 1 None - 1 Rat 5.2 pKi = 5.2 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 291 2 0 3 3.6 Cc1cc(C)nc(N(C)c2ccccc2Br)n1 10.1021/jm980222w
10783164 33831 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 337 9 1 5 4.2 C=CCN(CC=C)c1nc(C)nc(Nc2c(CC)cccc2CC)n1 10.1021/jm960148m
CHEMBL136519 33831 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 337 9 1 5 4.2 C=CCN(CC=C)c1nc(C)nc(Nc2c(CC)cccc2CC)n1 10.1021/jm960148m
20780072 74000 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 476 5 0 4 6.9 Cc1cc(C)c(-n2c3ccccc3n3c(CN(C)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL187924 74000 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 476 5 0 4 6.9 Cc1cc(C)c(-n2c3ccccc3n3c(CN(C)Cc4ccccc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
11268730 168623 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 370 4 0 5 4.2 CCC(CC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL414664 168623 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 370 4 0 5 4.2 CCC(CC)N1CCn2c(=O)n(-c3ccc(Cl)cc3)c3nc(C)cc1c32 10.1021/jm050384+
44392764 71973 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 7 0 4 4.9 CCCN(CCC)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182504 71973 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 7 0 4 4.9 CCCN(CCC)c1nc(C)nc(C(=O)c2c(C)cc(C)cc2C)c1C 10.1016/j.bmcl.2004.05.072
44443650 100806 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 446 9 1 6 5.9 CCCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)cc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL248803 100806 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 446 9 1 6 5.9 CCCO[C@H]1Cc2ccccc2[C@H]1Nc1nc(CC)c(Oc2cc(C)cc(C)n2)nc1CC 10.1016/j.bmcl.2007.09.008
11364104 82380 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 502 8 1 6 6.5 COc1cccc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)c1 10.1016/j.bmcl.2005.10.097
CHEMBL204690 82380 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 502 8 1 6 6.5 COc1cccc(COc2ccc(S(=O)(=O)c3ccc(C)nc3Nc3c(C)cc(C)cc3C)cc2)c1 10.1016/j.bmcl.2005.10.097
21916273 13739 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 6 0 4 8.1 CCN(Cc1ccc(Cl)c(Cl)c1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1084565 13739 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 542 6 0 4 8.1 CCN(Cc1ccc(Cl)c(Cl)c1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
20780049 155617 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 4 0 5 6.6 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4c4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL394112 155617 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 4 0 5 6.6 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCCC4c4ccccc4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
46891010 13208 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.0 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCC(C)C4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082443 13208 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 3 0 4 6.0 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCCC(C)C4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
21916154 129355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 432 7 0 4 6.3 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
CHEMBL360185 129355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 432 7 0 4 6.3 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12)CC1CC1 10.1016/j.bmcl.2005.06.028
44341755 16926 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 412 9 0 4 6.8 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(C)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL115818 16926 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 412 9 0 4 6.8 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(C)cc3Cl)n(CC)nc12 10.1016/s0960-894x(03)00621-8
122193724 130667 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 448 5 0 4 4.8 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2CCF 10.1016/j.bmcl.2015.10.010
CHEMBL3627731 130667 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 448 5 0 4 4.8 Cc1cc(N(C)C)c2c(n1)N(c1ccc(C(C)C)cc1Br)CC(=O)N2CCF 10.1016/j.bmcl.2015.10.010
44443591 101107 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 376 8 1 5 5.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
CHEMBL250617 101107 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 376 8 1 5 5.7 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1NC(CC)c1ccccc1 10.1016/j.bmcl.2007.09.008
10831985 127256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 354 6 1 7 3.3 CCC(COC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL354256 127256 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 354 6 1 7 3.3 CCC(COC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
10788999 64279 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 435 9 0 7 4.6 CCCCN(CC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL166056 64279 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 435 9 0 7 4.6 CCCCN(CC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
10764802 65491 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 424 9 0 6 5.0 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
CHEMBL168497 65491 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 424 9 0 6 5.0 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C(F)(F)F)n1 10.1021/jm980222w
10549365 172474 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 406 7 0 6 4.0 CCN(CC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL424538 172474 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 406 7 0 6 4.0 CCN(CC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2Br)n1 10.1021/jm980222w
10228129 14171 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 7 0 4 6.8 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1086504 14171 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 488 7 0 4 6.8 CCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
21916331 154267 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 449 7 0 5 6.3 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
CHEMBL393044 154267 1 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 449 7 0 5 6.3 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
44446725 175732 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL438888 175732 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
44446725 175732 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2008.07.063
CHEMBL438888 175732 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 376 7 0 3 6.5 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2008.07.063
44587455 194826 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 465 8 0 5 6.1 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(C(F)(F)F)cc2C(F)(F)F)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497651 194826 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 465 8 0 5 6.1 CCCN(CCC)c1c(C)nc(-c2c(OC)cc(C(F)(F)F)cc2C(F)(F)F)nc1OC 10.1016/j.bmcl.2008.07.063
11166919 173087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 417 5 0 4 6.1 CCC(CC)N1CCc2cn(-c3ccc(OC(F)(F)F)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL427168 173087 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 417 5 0 4 6.1 CCC(CC)N1CCc2cn(-c3ccc(OC(F)(F)F)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
44384801 139051 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 393 6 0 6 4.0 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
CHEMBL369700 139051 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 393 6 0 6 4.0 CCCN(CC1CC1)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
11798114 65581 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 457 9 0 5 6.4 CCCCN(CCCC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168823 65581 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 457 9 0 5 6.4 CCCCN(CCCC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9910700 65819 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169416 65819 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10295219 70787 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 413 9 1 6 5.2 CCc1nc(-c2ccc(OC(F)(F)F)cc2OC)c(OC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807057 70787 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 413 9 1 6 5.2 CCc1nc(-c2ccc(OC(F)(F)F)cc2OC)c(OC)nc1NC(CC)CC 10.1021/jm200365y
10303191 176054 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 561 8 1 4 8.8 FC(F)(F)CCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL441311 176054 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 561 8 1 4 8.8 FC(F)(F)CCN(Cc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
44392781 136449 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 371 6 0 5 5.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL367371 136449 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 371 6 0 5 5.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(C)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
10789145 39865 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 437 9 1 7 4.6 CCOCC(COCC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
CHEMBL141692 39865 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1Displacement of [125I]-tyrosine-ovine-CRF from human Corticotropin releasing factor receptor 1
ChEMBL 437 9 1 7 4.6 CCOCC(COCC)Nc1nc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1021/jm9904351
10142098 13263 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1082696 13263 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 506 7 0 4 6.9 Cc1cc(C)c(-n2c(Cl)cn3c(CN(CCC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
11212114 113168 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 412 9 0 5 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3085416 113168 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 412 9 0 5 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL3139409 113168 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 412 9 0 5 5.9 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
11576870 77347 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 380 4 0 4 5.4 CC[C@H]1Cn2nc(-c3ccc(C)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL194890 77347 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 380 4 0 4 5.4 CC[C@H]1Cn2nc(-c3ccc(C)cc3Cl)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11634953 78692 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 5 0 4 6.1 CCCCN1c2cc(C)nc3c(-c4ccc(Cl)cc4Cl)nn(c23)C[C@@H]1CC 10.1021/jm049085v
CHEMBL197197 78692 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 402 5 0 4 6.1 CCCCN1c2cc(C)nc3c(-c4ccc(Cl)cc4Cl)nn(c23)C[C@@H]1CC 10.1021/jm049085v
44305255 109531 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 416 4 0 4 6.5 CCCC1CCCCN1c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL305092 109531 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 416 4 0 4 6.5 CCCC1CCCCN1c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
21916296 153784 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 471 7 0 5 6.3 CCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL392655 153784 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 471 7 0 5 6.3 CCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3Cl)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
44342084 16798 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 392 8 0 4 5.2 COCCN(CCOC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115032 16798 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 392 8 0 4 5.2 COCCN(CCOC)c1cc(C)nc2c(-c3c(C)cc(C)cc3C)cccc12 10.1016/s0960-894x(03)00684-x
44396572 130166 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 444 8 1 7 4.5 COCC(Cc1ccccc1)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL361670 130166 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 444 8 1 7 4.5 COCC(Cc1ccccc1)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
11477320 77704 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 391 7 0 4 6.0 CCCC(CCC)N1CCc2cn(-c3ccc(OC)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL195152 77704 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 391 7 0 4 6.0 CCCC(CCC)N1CCc2cn(-c3ccc(OC)cc3C)c3nc(C)cc1c23 10.1021/jm050070m
9849255 202687 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 510 9 0 8 5.5 COCCN(CCOC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL559127 202687 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 510 9 0 8 5.5 COCCN(CCOC)c1nc(C)nc2c1sc(=S)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
44392805 71651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 463 6 0 5 4.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(I)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL182165 71651 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 463 6 0 5 4.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(I)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
44392643 71343 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 371 6 0 5 5.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL181548 71343 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 371 6 0 5 5.0 CCCN(CCC)c1cc(C)nc2c(-c3ncc(Cl)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
10672237 65485 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 475 9 0 7 4.4 COCCN(CCOC)c1nc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL168476 65485 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 475 9 0 7 4.4 COCCN(CCOC)c1nc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341816 16325 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 434 9 0 5 5.9 CCCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112336 16325 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 434 9 0 5 5.9 CCCCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
11339333 69851 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 426 10 0 5 6.3 CCCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL178836 69851 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 426 10 0 5 6.3 CCCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
44388403 172963 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL426419 172963 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 406 10 0 5 5.9 CCCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
44352448 25736 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 411 8 1 4 6.5 CCCN(Cc1sc(Nc2c(C)cc(C)cc2C)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL128713 25736 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 411 8 1 4 6.5 CCCN(Cc1sc(Nc2c(C)cc(C)cc2C)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
11188634 132733 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 395 7 0 7 3.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)nc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL364892 132733 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 395 7 0 7 3.7 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(OC)nc3)c3nc(C)cc1c32 10.1021/jm050384+
10662222 65279 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 303 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(OC)cc1SC 10.1021/jm980222w
CHEMBL168359 65279 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 303 5 0 5 4.0 CCN(c1nc(C)cc(C)n1)c1ccc(OC)cc1SC 10.1021/jm980222w
9951620 16353 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 376 6 1 3 5.8 CCCCN(CC)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
CHEMBL112478 16353 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 376 6 1 3 5.8 CCCCN(CC)c1cc(C)[nH]c2c(-c3ccc(Cl)cc3Cl)nnc1-2 10.1016/s0960-894x(03)00621-8
44587454 199941 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 415 10 1 6 4.7 CCCN(CCC)c1c(CC(C)(C)O)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL523074 199941 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 415 10 1 6 4.7 CCCN(CCC)c1c(CC(C)(C)O)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
20780008 14121 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 412 6 0 4 5.3 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1086259 14121 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 412 6 0 4 5.3 CCCN(CC1CC1)C(=O)c1c(C)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
20780037 138571 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 422 6 0 4 4.9 CCCN(CC(F)(F)F)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL369341 138571 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 422 6 0 4 4.9 CCCN(CC(F)(F)F)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
44388393 67327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL175902 67327 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCCC(c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
21916323 13862 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 486 4 0 4 6.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCC(c5ccccc5)C4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1085088 13862 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 486 4 0 4 6.7 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCC(c5ccccc5)C4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
20780251 71142 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 394 7 0 4 4.8 CCc1nc2n(c1C(=O)N(CC)CCC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181287 71142 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 394 7 0 4 4.8 CCc1nc2n(c1C(=O)N(CC)CCC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780070 134067 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 572 8 0 4 8.2 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL365858 134067 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 572 8 0 4 8.2 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CCC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
11077161 210269 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 291 4 2 3 3.2 C#Cc1cccc(/N=C(/NNc2ccccc2C)C(C)=O)c1 10.1021/jm025512y
CHEMBL66157 210269 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 291 4 2 3 3.2 C#Cc1cccc(/N=C(/NNc2ccccc2C)C(C)=O)c1 10.1021/jm025512y
9865345 16231 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 2 5 4.8 CCCC(CO)Nc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL111867 16231 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 392 6 2 5 4.8 CCCC(CO)Nc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
44307655 210465 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 393 8 0 5 5.8 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(CCC)c12 10.1016/s0960-894x(02)00358-x
CHEMBL67483 210465 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 393 8 0 5 5.8 CCCN(CCC)c1nc(C)nc2c(-c3c(C)cc(C)cc3C)nn(CCC)c12 10.1016/s0960-894x(02)00358-x
11222685 75782 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 378 4 0 4 5.4 CCC(CC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL192335 75782 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 378 4 0 4 5.4 CCC(CC)N1CCc2cn(-c3ccc(Cl)cc3C#N)c3nc(C)cc1c23 10.1021/jm050070m
44462209 112966 0 None - 1 Human 6.2 pKi = 6.2 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 409 10 0 6 4.5 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC(F)F)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL313823 112966 0 None - 1 Human 6.2 pKi = 6.2 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 409 10 0 6 4.5 CCCN(CCC)c1c(C)nc(-c2c(OC)cccc2OC(F)F)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
10857993 210342 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 253 4 2 3 2.9 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1 10.1021/jm025512y
CHEMBL66698 210342 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 253 4 2 3 2.9 CC(=O)/C(=N\c1ccccc1)NNc1ccccc1 10.1021/jm025512y
44306462 209820 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 385 9 0 5 4.7 CCCN(c1nccc(-c2c(F)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63457 209820 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 385 9 0 5 4.7 CCCN(c1nccc(-c2c(F)cc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
44306162 210286 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 413 7 0 3 5.9 CCCN(c1ncc(C)c(-c2ccc(Br)cc2C)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL66249 210286 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 413 7 0 3 5.9 CCCN(c1ncc(C)c(-c2ccc(Br)cc2C)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
10549990 174849 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Compound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneCompound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm990590f
CHEMBL432496 174849 0 None -1 2 Human 7.2 pKi = 7.2 Binding
Compound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membraneCompound was tested for the inhibition of binding of the radioligand, [125 I-Tyr0]-CRF to rat cerebral cortex membrane
ChEMBL 418 5 0 5 4.7 CCN(c1nc(C)cc(N2CCOCC2)n1)c1ccc(C(C)C)cc1Br 10.1021/jm990590f
20780280 71120 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 484 7 0 4 5.6 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)C(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181227 71120 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 484 7 0 4 5.6 CCc1nc2n(c1C(=O)N(CC1CC1)CC(F)(F)C(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
21916183 14353 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 476 7 0 4 6.5 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1087804 14353 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 476 7 0 4 6.5 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
11653680 78228 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 374 3 0 4 5.3 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC 10.1021/jm049085v
CHEMBL196146 78228 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 374 3 0 4 5.3 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1CC 10.1021/jm049085v
9887524 172937 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 404 5 0 5 5.0 CCC(COC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
CHEMBL426283 172937 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 404 5 0 5 5.0 CCC(COC)N1CCn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc1c32 10.1021/jm049085v
44392758 71972 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 7 3.7 CCCN(CC1CC1)c1cc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)n1 10.1016/j.bmcl.2004.05.072
CHEMBL182500 71972 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 399 10 0 7 3.7 CCCN(CC1CC1)c1cc(C)nc(C(=O)c2c(OC)cc(OC)cc2OC)n1 10.1016/j.bmcl.2004.05.072
10118581 70115 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 513 8 1 4 8.7 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CCCCC1 10.1016/j.bmcl.2004.10.055
CHEMBL179416 70115 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 513 8 1 4 8.7 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CCCCC1 10.1016/j.bmcl.2004.10.055
11374322 142495 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 449 8 1 6 5.6 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCCCC#N)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL372996 142495 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 449 8 1 6 5.6 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCCCC#N)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
10575478 175176 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 1 8 2.9 COCCN(CCO)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL434689 175176 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 448 8 1 8 2.9 COCCN(CCO)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341734 16990 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 10 0 4 7.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CCC)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL116010 16990 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 446 10 0 4 7.5 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(CCC)nc12 10.1016/s0960-894x(03)00621-8
44317977 212010 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 7 1 3 6.1 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(C(F)(F)F)c1 10.1021/jm049974i
CHEMBL78721 212010 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 412 7 1 3 6.1 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(C(F)(F)F)c1 10.1021/jm049974i
11792386 64331 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 353 6 0 7 3.5 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)nc1C 10.1021/jm980224g
CHEMBL166431 64331 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 353 6 0 7 3.5 CCCCN(CC)c1nc(C)nc2c1nnn2-c1c(C)cc(C)nc1C 10.1021/jm980224g
44307784 210859 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 293 4 1 5 3.3 CC(=O)/C(=N\Nc1ccccc1C#N)Oc1cccc(C)c1 10.1021/jm025512y
CHEMBL70143 210859 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 293 4 1 5 3.3 CC(=O)/C(=N\Nc1ccccc1C#N)Oc1cccc(C)c1 10.1021/jm025512y
20780249 71431 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 462 8 0 4 5.7 CCc1nc2n(c1C(=O)N(CCC1CC1)CCC(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181823 71431 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 462 8 0 4 5.7 CCc1nc2n(c1C(=O)N(CCC1CC1)CCC(F)(F)F)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
11034476 210582 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 317 5 2 4 3.8 COc1cccc(N/C(=N/Nc2ccccc2Cl)C(C)=O)c1 10.1021/jm025512y
CHEMBL68340 210582 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 317 5 2 4 3.8 COc1cccc(N/C(=N/Nc2ccccc2Cl)C(C)=O)c1 10.1021/jm025512y
20780069 74203 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 7 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL188945 74203 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 522 7 0 4 7.4 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
11759733 210455 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 345 4 2 3 3.9 C#Cc1cccc(/N=C(/NNc2ccccc2C(F)(F)F)C(C)=O)c1 10.1021/jm025512y
CHEMBL67438 210455 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 345 4 2 3 3.9 C#Cc1cccc(/N=C(/NNc2ccccc2C(F)(F)F)C(C)=O)c1 10.1021/jm025512y
10528613 65785 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 476 10 0 8 3.9 COCCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169195 65785 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 476 10 0 8 3.9 COCCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
20780271 128807 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 484 7 0 4 6.1 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)Cc1ccccc1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL359499 128807 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 484 7 0 4 6.1 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)Cc1ccccc1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780285 130689 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 366 7 0 4 4.9 CCCN(Cc1c(C)nc2n1CCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2005.05.117
CHEMBL362799 130689 0 None - 1 Human 5.2 pKi = 5.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 366 7 0 4 4.9 CCCN(Cc1c(C)nc2n1CCN2c1c(C)cc(C)cc1C)CC1CC1 10.1016/j.bmcl.2005.05.117
44266401 11693 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 6 1 6 5.7 CCN(c1nc(C)cc(-c2ccccc2-c2nn[nH]n2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10464 11693 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 477 6 1 6 5.7 CCN(c1nc(C)cc(-c2ccccc2-c2nn[nH]n2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
10204820 122143 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 459 9 0 4 7.2 CCCN(Cc1sc(N(CC)c2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL334976 122143 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 459 9 0 4 7.2 CCCN(Cc1sc(N(CC)c2c(C)cc(C)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
10832559 127202 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 362 2 0 2 5.9 Cc1cc(Cl)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL353774 127202 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 362 2 0 2 5.9 Cc1cc(Cl)c2ccn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
21916268 13950 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 6 0 4 6.1 C=C(C)CN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1085518 13950 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 6 0 4 6.1 C=C(C)CN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
44443643 101156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 458 8 1 6 6.1 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC1CCCC1 10.1016/j.bmcl.2007.09.008
CHEMBL250815 101156 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 458 8 1 6 6.1 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OC1CCCC1 10.1016/j.bmcl.2007.09.008
21916073 14451 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 484 8 0 4 6.8 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
CHEMBL1088626 14451 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 484 8 0 4 6.8 CCCN(CCc1ccccc1)Cc1c(C(F)(F)F)nc2n1CCCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2010.01.127
10113422 71094 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 427 4 1 4 6.2 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CC=CC1 10.1016/j.bmcl.2004.10.055
CHEMBL181121 71094 0 None - 1 Human 5.2 pKi = 5.2 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 427 4 1 4 6.2 FC(F)(F)c1nc(Nc2c(Cl)cc(Cl)cc2Cl)sc1CN1CC=CC1 10.1016/j.bmcl.2004.10.055
20780167 131255 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 510 7 0 4 7.4 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL364002 131255 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 510 7 0 4 7.4 CCCN(CCC(F)(F)F)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
10664736 64285 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 338 4 0 4 4.3 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980222w
CHEMBL166109 64285 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 338 4 0 4 4.3 CCN(c1nc(C)cc(C)n1)c1ccc(N(C)C)cc1C(F)(F)F 10.1021/jm980222w
9803991 175463 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 453 7 0 5 6.5 CCCCN(Cc1ccncc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL436564 175463 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 453 7 0 5 6.5 CCCCN(Cc1ccncc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
20780287 69282 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 406 7 0 4 4.8 CCc1nc2n(c1C(=O)N(CC1CC1)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL178165 69282 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 406 7 0 4 4.8 CCc1nc2n(c1C(=O)N(CC1CC1)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
53309402 70764 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 364 7 0 2 6.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1CC(CC)CC 10.1021/jm200365y
CHEMBL1807030 70764 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 364 7 0 2 6.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(CC)nc1CC(CC)CC 10.1021/jm200365y
12982784 22270 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 322 6 0 4 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL121614 22270 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 322 6 0 4 4.6 CCCN(CCC)c1cc(C)nc2c(-c3ccccc3)c(C)nn12 10.1016/j.bmcl.2004.05.019
21916111 13262 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 440 7 0 4 6.3 CCCN(CCC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1082686 13262 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 440 7 0 4 6.3 CCCN(CCC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
44305545 107481 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 362 5 1 4 5.5 CCCCNc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL292484 107481 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 362 5 1 4 5.5 CCCCNc1cc(C)nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
10739909 127355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 402 6 1 6 4.6 CCCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL354579 127355 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 402 6 1 6 4.6 CCCCNc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
11450550 136911 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 336 7 0 5 4.2 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C)CC 10.1021/jm049339c
CHEMBL367789 136911 0 None - 1 Human 6.2 pKi = 6.2 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 336 7 0 5 4.2 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C)CC 10.1021/jm049339c
10991736 210514 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 351 5 2 4 4.1 COc1cccc(N/C(=N/Nc2ccccc2C(F)(F)F)C(C)=O)c1 10.1021/jm025512y
CHEMBL67785 210514 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 351 5 2 4 4.1 COc1cccc(N/C(=N/Nc2ccccc2C(F)(F)F)C(C)=O)c1 10.1021/jm025512y
44385629 68071 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 413 8 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
CHEMBL176707 68071 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 413 8 0 8 2.5 COCCN(CCOC)c1nc(C)nc2c1n(C)c(=O)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00108-0
44462088 212688 0 None - 1 Human 8.2 pKi = 8.2 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 371 8 0 5 4.3 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL84007 212688 0 None - 1 Human 8.2 pKi = 8.2 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 371 8 0 5 4.3 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
10500067 64609 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 381 9 0 7 3.8 CCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
CHEMBL167095 64609 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 381 9 0 7 3.8 CCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
10832987 64942 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 370 9 0 6 4.3 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
CHEMBL168169 64942 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 370 9 0 6 4.3 CCCN(CCC)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
44341680 117819 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 432 8 0 4 7.0 CCCCN(c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12)C(CC)CC 10.1016/s0960-894x(03)00622-x
CHEMBL326284 117819 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 432 8 0 4 7.0 CCCCN(c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12)C(CC)CC 10.1016/s0960-894x(03)00622-x
44446731 101643 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 400 7 0 3 6.5 COc1cc(C)cc(C)c1-c1nc(C)c(N(CC2CC2)CC2CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253914 101643 0 None - 1 Human 8.2 pKi = 8.2 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 400 7 0 3 6.5 COc1cc(C)cc(C)c1-c1nc(C)c(N(CC2CC2)CC2CC2)c2ccccc12 10.1016/j.bmcl.2007.12.050
20780066 73677 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 508 6 0 4 7.0 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL186479 73677 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 508 6 0 4 7.0 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CC4CC4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
10503714 64212 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 449 8 0 8 3.4 COCC(COC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL165478 64212 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 449 8 0 8 3.4 COCC(COC)Oc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
10740327 65777 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 410 8 0 6 4.4 COCCN(CCOC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169083 65777 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 410 8 0 6 4.4 COCCN(CCOC)c1nc(C)nc2c1c(C)c(C)n2-c1c(C)cc(C)cc1C 10.1021/jm980224g
10712065 65796 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 338 5 1 6 4.0 CCCC(C)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169280 65796 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 338 5 1 6 4.0 CCCC(C)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL1077301 215270 0 None 12 2 Human 8.1 pKi = 8.1 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CO)[C@@H](C)CC)[C@@H](C)O)C(C)C)[C@@H](C)O)C(=O)N[C@@H](C)C(N)=O 10.1021/jm990590f
53310132 70716 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 9 1 5 5.8 CCc1nc(-c2ccc(OC(F)(F)F)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806730 70716 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 411 9 1 5 5.8 CCc1nc(-c2ccc(OC(F)(F)F)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
11751120 140402 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 406 6 0 4 6.2 CCCC(CCC)N1CCc2cn(-c3ccc(C#N)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL371407 140402 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 406 6 0 4 6.2 CCCC(CCC)N1CCc2cn(-c3ccc(C#N)cc3Cl)c3nc(C)cc1c23 10.1021/jm050070m
CHEMBL429560 220319 0 None -2 2 Human 8.1 pKi = 8.1 Binding
Binding affinity of the receptor corticotropin releasing factor receptor with peptidic agonistsBinding affinity of the receptor corticotropin releasing factor receptor with peptidic agonists
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H]1CCCN1C(=O)CNC(=O)[C@@H](N)CCC(N)=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)C(N)=O 10.1021/jm990590f
122193725 130743 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 476 7 0 4 5.6 CCN(CC)c1cc(C)nc2c1N(CCF)C(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
CHEMBL3628744 130743 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation countingDisplacement of [125I]-Tyr0-sauvagine from human CRF1 receptor expressed in HEK293T cells after 2 hrs by scintillation counting
ChEMBL 476 7 0 4 5.6 CCN(CC)c1cc(C)nc2c1N(CCF)C(=O)CN2c1ccc(C(C)C)cc1Br 10.1016/j.bmcl.2015.10.010
18449319 70715 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 357 9 1 5 4.9 CCc1nc(-c2ccc(OC)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806729 70715 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 357 9 1 5 4.9 CCc1nc(-c2ccc(OC)cc2OC)c(CC)nc1NC(CC)CC 10.1021/jm200365y
11305354 130607 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCCC(c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
CHEMBL362453 130607 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 444 10 0 5 6.4 CCCCC(c1ccc(F)cc1)N(CCC)c1nc(-c2ccc(Cl)cc2OC)n(C)n1 10.1021/jm049339c
11450996 129033 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 351 6 0 5 4.7 CCCN(CCC)c1cc(C)nc2c(-c3cnc(C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL359784 129033 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 351 6 0 5 4.7 CCCN(CCC)c1cc(C)nc2c(-c3cnc(C)cc3C)c(C)nn12 10.1021/jm040058e
9957619 65937 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 498 8 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
CHEMBL169955 65937 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 498 8 0 8 3.1 COCCN(CCOC)c1nc(C)nc2c1nnn2-c1ccc(Br)cc1Br 10.1021/jm980224g
9910700 65819 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169416 65819 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9932463 172475 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 0 6 5.0 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL424539 172475 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 430 7 0 6 5.0 CCCCN(CC)c1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44387042 172895 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 7 0 6 4.9 CCCN(CCC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL426044 172895 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 459 7 0 6 4.9 CCCN(CCC)c1nc(C)nc2c1n(C)c(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10690278 65941 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 7 1 6 4.8 CCCCC(CC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
CHEMBL169979 65941 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 366 7 1 6 4.8 CCCCC(CC)Nc1nc(C)nc2c1nnn2-c1c(C)cc(C)cc1C 10.1021/jm980224g
53310275 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 355 8 1 5 4.6 CCc1nc(-c2cnc(C)cc2N(C)C)c(CC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1806957 70750 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 355 8 1 5 4.6 CCc1nc(-c2cnc(C)cc2N(C)C)c(CC)nc1NC(CC)CC 10.1021/jm200365y
44352447 125250 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 603 8 1 4 7.8 CCCN(Cc1sc(Nc2c(Br)cc(Br)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL341313 125250 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 603 8 1 4 7.8 CCCN(Cc1sc(Nc2c(Br)cc(Br)cc2Br)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44266496 105291 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 459 5 0 3 7.6 CCN(c1nc(C)cc(-c2cccc3ccccc23)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL276184 105291 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 459 5 0 3 7.6 CCN(c1nc(C)cc(-c2cccc3ccccc23)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
22249028 70717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 371 10 1 5 5.3 CCOc1ccc(-c2nc(CC)c(NC(CC)CC)nc2CC)c(OC)c1 10.1021/jm200365y
CHEMBL1806731 70717 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 371 10 1 5 5.3 CCOc1ccc(-c2nc(CC)c(NC(CC)CC)nc2CC)c(OC)c1 10.1021/jm200365y
16730517 100351 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 451 7 0 5 6.0 CCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
CHEMBL246501 100351 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 451 7 0 5 6.0 CCN(CCc1ccccc1)Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12 10.1016/j.bmcl.2007.01.008
3520 10041 54 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050070m
9821250 10041 54 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050070m
CHEMBL309138 10041 54 None 1 2 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cellsInhibition of [125I]sauvagine binding to corticotropin releasing factor receptor 1 expressed in LtK- cells
ChEMBL 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10.1021/jm050070m
11710664 76449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 380 4 0 4 5.4 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL193522 76449 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 380 4 0 4 5.4 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3C)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11560105 78335 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 386 3 0 4 5.3 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](C)N2CC1CC1 10.1021/jm049085v
CHEMBL196307 78335 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 386 3 0 4 5.3 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3C[C@H](C)N2CC1CC1 10.1021/jm049085v
11525846 78599 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 442 5 0 4 6.6 CC[C@H]1Cn2nc(-c3ccc(C(C)C)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL196879 78599 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 442 5 0 4 6.6 CC[C@H]1Cn2nc(-c3ccc(C(C)C)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11691278 139916 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 468 4 0 4 6.5 CC[C@H]1Cn2nc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL370346 139916 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 468 4 0 4 6.5 CC[C@H]1Cn2nc(-c3ccc(C(F)(F)F)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
11524791 142004 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 430 5 0 5 5.4 CC[C@H]1Cn2nc(-c3ccc(OC)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
CHEMBL372365 142004 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 430 5 0 5 5.4 CC[C@H]1Cn2nc(-c3ccc(OC)cc3C(F)(F)F)c3nc(C)cc(c32)N1CC1CC1 10.1021/jm049085v
44341809 16991 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 414 9 0 5 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(OC)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL116011 16991 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 414 9 0 5 6.0 CCCCN(CCCC)c1cc(C)nc2c(-c3ccc(OC)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
10573028 38087 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)n1 10.1021/jm960149e
CHEMBL140175 38087 0 None - 1 Human 7.2 pKi = 7.2 Binding
Inhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 dosesInhibition of [125I]CRF binding to human Corticotropin releasing factor receptor 1 tested at 6-12 doses
ChEMBL 398 7 1 4 6.1 CCCN(CC1CC1)c1cc(C)nc(Nc2c(Cl)cc(Cl)cc2Cl)n1 10.1021/jm960149e
44267068 175707 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL 1428 40 17 18 -1.7 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(CCCCC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N1)C(C)C)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
CHEMBL438724 175707 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL 1428 40 17 18 -1.7 CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)C(CCCCC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2c[nH]cn2)C(=O)N1)C(C)C)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
44306535 169462 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 409 9 0 7 4.7 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2ccoc2)CC1 10.1016/j.bmcl.2004.02.053
CHEMBL417033 169462 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 409 9 0 7 4.7 CCCN(c1nccc(-c2c(OC)cc(OC)cc2OC)n1)C1(c2ccoc2)CC1 10.1016/j.bmcl.2004.02.053
20780050 100687 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 483 5 0 5 6.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(Cc5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL248162 100687 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 483 5 0 5 6.3 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(Cc5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
20780052 100688 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 497 6 0 5 6.7 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(CCc5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL248163 100688 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 497 6 0 5 6.7 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(CCc5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
20780120 73999 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 456 7 0 4 6.8 CCCCN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL187923 73999 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 456 7 0 4 6.8 CCCCN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
22249115 70767 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 371 6 1 3 6.3 CCc1nc(NC(CC)CC)c(Cl)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
CHEMBL1807033 70767 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 371 6 1 3 6.3 CCc1nc(NC(CC)CC)c(Cl)nc1-c1ccc(Cl)cc1Cl 10.1021/jm200365y
44443570 161552 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 342 9 0 5 4.7 CCCN(CCC)c1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
CHEMBL400154 161552 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 342 9 0 5 4.7 CCCN(CCC)c1nc(CC)c(Oc2cc(C)ccn2)nc1CC 10.1016/j.bmcl.2007.09.008
22324340 212845 0 None - 1 Human 7.1 pKi = 7.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 355 7 0 4 4.8 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL85416 212845 0 None - 1 Human 7.1 pKi = 7.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 355 7 0 4 4.8 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2C)n(CC)c1=O 10.1016/s0960-894x(03)00483-9
44337493 116562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 338 7 0 4 4.5 CCCN(c1nc(-c2ccc(C)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL323257 116562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 338 7 0 4 4.5 CCCN(c1nc(-c2ccc(C)cc2C)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
22324337 171181 0 None - 1 Human 6.1 pKi = 6.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 387 10 0 6 4.3 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CCC)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL421334 171181 0 None - 1 Human 6.1 pKi = 6.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 387 10 0 6 4.3 CCCN(CCC)c1c(C)nc(-c2ccc(OC)cc2OC)n(CCC)c1=O 10.1016/s0960-894x(03)00483-9
10644018 64358 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 387 2 0 3 5.7 Cc1cc(Cl)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
CHEMBL166732 64358 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 387 2 0 3 5.7 Cc1cc(Cl)c2c(C#N)cn(-c3ccc(C(C)C)cc3Br)c2n1 10.1021/jm980223o
44352454 123640 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 8 1 4 6.8 CCCN(Cc1sc(Nc2c(C)cc(Cl)cc2C)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL338154 123640 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 431 8 1 4 6.8 CCCN(Cc1sc(Nc2c(C)cc(Cl)cc2C)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
20780281 175032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 448 7 0 4 5.3 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL433768 175032 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 448 7 0 4 5.3 CCc1nc2n(c1C(=O)N(CCC(F)(F)F)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
10277887 71082 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 485 8 1 4 7.9 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CCC1 10.1016/j.bmcl.2004.10.055
CHEMBL181075 71082 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 485 8 1 4 7.9 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CCC1 10.1016/j.bmcl.2004.10.055
44317964 110933 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 428 7 1 3 5.9 O=C(CCc1ccncc1)C(Nc1ccccc1Cl)c1ccccc1Br 10.1021/jm049974i
CHEMBL309546 110933 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 428 7 1 3 5.9 O=C(CCc1ccncc1)C(Nc1ccccc1Cl)c1ccccc1Br 10.1021/jm049974i
20780269 137447 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 7 0 4 4.6 C=CCN(CCC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL368245 137447 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 7 0 4 4.6 C=CCN(CCC)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780071 132583 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 7.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
CHEMBL364809 132583 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 558 7 0 4 7.8 Cc1cc(C)c(-n2c3ccccc3n3c(CN(CCc4ccccc4)CC(F)(F)F)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2005.06.028
20780139 74229 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 496 6 0 4 7.0 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC(F)(F)F 10.1016/j.bmcl.2005.06.028
CHEMBL189115 74229 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 496 6 0 4 7.0 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC(F)(F)F 10.1016/j.bmcl.2005.06.028
20780138 129136 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 546 7 0 4 7.6 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC(F)(F)C(F)(F)F 10.1016/j.bmcl.2005.06.028
CHEMBL360000 129136 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 546 7 0 4 7.6 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12)CC(F)(F)C(F)(F)F 10.1016/j.bmcl.2005.06.028
20780278 72858 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 434 7 0 4 5.5 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(Cl)cc1Cl 10.1016/j.bmcl.2005.05.117
CHEMBL183824 72858 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 434 7 0 4 5.5 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(Cl)cc1Cl 10.1016/j.bmcl.2005.05.117
11375414 82364 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 497 7 1 6 6.3 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3cccc(C#N)c3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL204657 82364 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 497 7 1 6 6.3 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)c2ccc(OCc3cccc(C#N)c3)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
44317759 212359 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 390 8 1 3 6.0 C=Cc1ccccc1C(Nc1ccc(C)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
CHEMBL81376 212359 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 390 8 1 3 6.0 C=Cc1ccccc1C(Nc1ccc(C)cc1Cl)C(=O)CCc1ccncc1 10.1021/jm049974i
44587373 194769 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 10 0 5 5.4 CCCc1nc(-c2c(C)cc(C)cc2OC)nc(OC)c1N(CCC)CCC 10.1016/j.bmcl.2008.07.063
CHEMBL497287 194769 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 385 10 0 5 5.4 CCCc1nc(-c2c(C)cc(C)cc2OC)nc(OC)c1N(CCC)CCC 10.1016/j.bmcl.2008.07.063
21916339 14054 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 422 3 0 4 5.5 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CC=CCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086015 14054 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 422 3 0 4 5.5 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CC=CCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
46890890 13771 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccncc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1084722 13771 0 None - 1 Human 5.1 pKi = 5.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 475 6 0 5 5.8 Cc1cc(C)c(-n2c(Cl)cn3c(CN(C)CCc4ccncc4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
44307855 210441 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 357 6 0 5 4.6 CCCN(CCC)c1nc(C)nc2c(-c3ccccc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
CHEMBL67360 210441 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cellsDisplacement of [125I]-sauvagine from Corticotropin releasing factor receptor 1 endogenously expressed in IMR-32 human neuroblastoma cells
ChEMBL 357 6 0 5 4.6 CCCN(CCC)c1nc(C)nc2c(-c3ccccc3Cl)n(C)nc12 10.1016/s0960-894x(02)00358-x
44305202 209635 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 356 6 0 4 5.3 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL62533 209635 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 356 6 0 4 5.3 CCCCN(CC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(C)nn12 10.1016/s0960-894x(98)00372-2
20780250 70133 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 408 8 0 4 5.2 CCCN(CCC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL179499 70133 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 408 8 0 4 5.2 CCCN(CCC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
18672270 130106 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 497 8 1 5 7.9 CCCN(Cc1ccco1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL361647 130106 0 None - 1 Human 6.1 pKi = 6.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 497 8 1 5 7.9 CCCN(Cc1ccco1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
20780117 74545 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 518 8 0 4 8.0 CCCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL190823 74545 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 518 8 0 4 8.0 CCCCN(Cc1ccccc1)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c3ccccc3n12 10.1016/j.bmcl.2005.06.028
44307783 210858 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 309 5 1 6 3.0 COc1cccc(O/C(=N/Nc2ccccc2C#N)C(C)=O)c1 10.1021/jm025512y
CHEMBL70142 210858 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 309 5 1 6 3.0 COc1cccc(O/C(=N/Nc2ccccc2C#N)C(C)=O)c1 10.1021/jm025512y
44392723 130486 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 423 8 0 7 3.8 COCCN(CCOC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL362203 130486 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 423 8 0 7 3.8 COCCN(CCOC)c1cc(C)nc2c(-c3ncc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.056
21916321 14094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 440 7 0 4 6.3 CCCCN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
CHEMBL1086142 14094 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 440 7 0 4 6.3 CCCCN(CC)Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12 10.1016/j.bmcl.2010.04.094
18691321 214893 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 452 6 0 4 6.6 CCN(c1nc(C)cc(-c2ccccc2N(C)C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL9794 214893 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 452 6 0 4 6.6 CCN(c1nc(C)cc(-c2ccccc2N(C)C)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
44392801 129302 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 7 1 4 4.4 CCCN(CC1CC1)c1cc(C(O)c2c(C)cc(C)cc2C)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL360128 129302 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 353 7 1 4 4.4 CCCN(CC1CC1)c1cc(C(O)c2c(C)cc(C)cc2C)nc(C)n1 10.1016/j.bmcl.2004.05.072
10666432 127638 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 362 2 0 2 5.9 Cc1cc(Cl)nc2c1ccn2-c1ccc(C(C)C)cc1Br 10.1021/jm980223o
CHEMBL355882 127638 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 362 2 0 2 5.9 Cc1cc(Cl)nc2c1ccn2-c1ccc(C(C)C)cc1Br 10.1021/jm980223o
12967652 71365 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 507 8 1 4 7.9 CCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
CHEMBL181662 71365 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 507 8 1 4 7.9 CCN(CCc1ccccc1)Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F 10.1016/j.bmcl.2004.10.055
11703243 130919 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 2 0 4 4.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2C(C)C 10.1021/jm049085v
CHEMBL363394 130919 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 360 2 0 4 4.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2C(C)C 10.1021/jm049085v
11706059 131112 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 3 0 4 5.7 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1C(C)C 10.1021/jm049085v
CHEMBL363616 131112 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 388 3 0 4 5.7 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1C(C)C 10.1021/jm049085v
11516283 140405 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 372 3 0 4 4.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2CC1CC1 10.1021/jm049085v
CHEMBL371453 140405 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 372 3 0 4 4.9 Cc1cc2c3c(n1)c(-c1ccc(Cl)cc1Cl)nn3CCN2CC1CC1 10.1021/jm049085v
11602680 78597 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 346 2 1 4 4.9 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1 10.1021/jm049085v
CHEMBL196873 78597 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagineBinding affinity for human corticotropin releasing factor receptor 1 expressed in LtK- cells using [125I]sauvagine
ChEMBL 346 2 1 4 4.9 CC[C@H]1Cn2nc(-c3ccc(Cl)cc3Cl)c3nc(C)cc(c32)N1 10.1021/jm049085v
11474047 132302 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 366 5 0 6 3.5 CCC(CC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL364680 132302 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 366 5 0 6 3.5 CCC(CC)N1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
10622647 127578 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 5 5.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
CHEMBL355544 127578 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 5 5.5 CCCCN(CC)c1cc(C)nc(N(CC)c2ccc(C(C)=O)cc2Br)n1 10.1021/jm980222w
10548743 171762 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 395 10 0 7 4.2 CCCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
CHEMBL422555 171762 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 395 10 0 7 4.2 CCCCN(CCC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
10571912 176231 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 381 9 0 7 3.8 CCCCN(CC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
CHEMBL442773 176231 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 381 9 0 7 3.8 CCCCN(CC#N)c1nc(C)nc(N(CC)c2ccc(N(C)C)cc2C)n1 10.1021/jm980222w
44381468 127220 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 445 8 1 6 5.2 CCC(CCOC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL353891 127220 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 445 8 1 6 5.2 CCC(CCOC)Nc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
23068426 70778 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 367 7 1 4 5.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807048 70778 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 367 7 1 4 5.6 CCc1nc(-c2ccc(Cl)cc2Cl)c(OC)nc1NC(CC)CC 10.1021/jm200365y
9891049 14273 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 474 6 0 4 6.1 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CC2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
CHEMBL1087165 14273 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cellsDisplacement of [125I]Tyr-o-CRF from human CRFR1 expressed in human IMR32 cells
ChEMBL 474 6 0 4 6.1 Cc1cc(C)c(N2CCCn3c2nc(C(F)(F)F)c3CN(CC2CC2)CC(F)(F)F)c(C)c1 10.1016/j.bmcl.2010.01.127
44446726 101609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 476 11 0 3 7.5 CCCN(CCC)c1c(C)nc(-c2c(CC(F)F)cc(CC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253699 101609 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 476 11 0 3 7.5 CCCN(CCC)c1c(C)nc(-c2c(CC(F)F)cc(CC(F)F)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
44587456 194827 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 344 7 0 5 4.7 CCC(CC)Oc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497652 194827 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 344 7 0 5 4.7 CCC(CC)Oc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
127033836 145405 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3848 124 56 50 -13.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
CHEMBL3775830 145405 0 None -1 2 Human 8.1 pKi = 8.1 Binding
Displacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assayDisplacement of [125ITyr0-Glu1,Nle17]-PS-Svg in human CRF-R1 expressed in COS-M6 cells after 90 mins by gamma counting assay
ChEMBL 3848 124 56 50 -13.2 CCCCC(NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@H](NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)C(CCCC)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(=O)O)NC(C)=O)[C@@H](C)O)C(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc2cnc[nH]2)C(=O)N1)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@H](C)C(=O)N[C@H](C(N)=O)[C@@H](C)CC 10.1021/acs.jmedchem.5b00926
44341814 117441 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 422 8 0 6 4.4 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL325918 117441 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 422 8 0 6 4.4 COCCN(CCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
21916322 159598 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 429 7 0 5 5.9 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
CHEMBL397389 159598 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 429 7 0 5 5.9 CCCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CCC1 10.1016/j.bmcl.2007.01.008
21916270 13166 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 480 6 0 4 6.5 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC(F)(F)F 10.1016/j.bmcl.2010.04.094
CHEMBL1082302 13166 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 480 6 0 4 6.5 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC(F)(F)F 10.1016/j.bmcl.2010.04.094
44266431 11249 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 485 6 0 3 8.2 CCN(c1nc(C)cc(-c2ccccc2-c2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10189 11249 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 485 6 0 3 8.2 CCN(c1nc(C)cc(-c2ccccc2-c2ccccc2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
22249051 70776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 369 7 1 5 5.1 CCC(CC)Nc1nc(OC)c(-c2ccc(Cl)cc2Cl)nc1OC 10.1021/jm200365y
CHEMBL1807042 70776 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 369 7 1 5 5.1 CCC(CC)Nc1nc(OC)c(-c2ccc(Cl)cc2Cl)nc1OC 10.1021/jm200365y
20780048 155358 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 4 0 5 6.2 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(c5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
CHEMBL393901 155358 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 469 4 0 5 6.2 Cc1cc(C)c(-n2c3ncccc3n3c(CN4CCC(c5ccccc5)C4)c(C)nc23)c(Cl)c1 10.1016/j.bmcl.2007.01.008
9824147 169498 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 432 8 0 8 4.5 COCCN(CCOC)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL417091 169498 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 432 8 0 8 4.5 COCCN(CCOC)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
9869432 25618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 471 8 1 4 7.5 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
CHEMBL128100 25618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 471 8 1 4 7.5 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2003.08.055
44347436 23148 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 450 7 0 5 5.4 CCCN(CC1CC1)c1cc([S+](C)[O-])nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
CHEMBL122960 23148 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to the cloned human corticotropin releasing factor receptor 1Binding affinity to the cloned human corticotropin releasing factor receptor 1
ChEMBL 450 7 0 5 5.4 CCCN(CC1CC1)c1cc([S+](C)[O-])nc2c(-c3ccc(Cl)cc3Cl)c(C)nn12 10.1016/j.bmcl.2004.05.019
15490817 105334 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 495 6 0 5 6.4 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL276599 105334 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 495 6 0 5 6.4 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
22249156 70773 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 351 6 1 3 5.9 CCc1nc(-c2ccc(Cl)cc2Cl)c(C)nc1NC(CC)CC 10.1021/jm200365y
CHEMBL1807039 70773 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from human CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting
ChEMBL 351 6 1 3 5.9 CCc1nc(-c2ccc(Cl)cc2Cl)c(C)nc1NC(CC)CC 10.1021/jm200365y
9869432 25618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 471 8 1 4 7.5 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
CHEMBL128100 25618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 471 8 1 4 7.5 CCCN(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)CC1CC1 10.1016/j.bmcl.2004.10.055
11235359 73062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 414 6 0 6 5.3 CCCN(c1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL184752 73062 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 414 6 0 6 5.3 CCCN(c1ccccc1)c1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
44341733 16689 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)cccc12 10.1016/s0960-894x(03)00684-x
CHEMBL114419 16689 1 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)cccc12 10.1016/s0960-894x(03)00684-x
44341456 117462 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 496 9 0 5 7.1 CCCCN(CCc1ccc(OC)cc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL325996 117462 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 496 9 0 5 7.1 CCCCN(CCc1ccc(OC)cc1)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)n(C)nc12 10.1016/s0960-894x(03)00621-8
11383809 12143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 8 0 4 5.7 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(CC)n1)C(C1CC1)C1CC1 10.1021/jm049339c
CHEMBL106972 12143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 8 0 4 5.7 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(CC)n1)C(C1CC1)C1CC1 10.1021/jm049339c
11383809 12143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 392 8 0 4 5.7 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(CC)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL106972 12143 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 392 8 0 4 5.7 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(CC)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
9998456 34204 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 357 9 1 7 3.6 CCCN(CC1CC1)c1nc(C)nc(Nc2ccc(OC)cc2OC)n1 10.1021/jm960148m
CHEMBL136828 34204 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1Inhibition of [125I]CRF binding to human corticotropin releasing factor receptor 1
ChEMBL 357 9 1 7 3.6 CCCN(CC1CC1)c1nc(C)nc(Nc2ccc(OC)cc2OC)n1 10.1021/jm960148m
44315525 110967 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 387 10 1 8 3.6 CCCN(CC1CC1)c1nc(C)nc(Nc2c(OC)cc(OC)cc2OC)n1 10.1021/jm9900117
CHEMBL309789 110967 0 None - 1 Human 5.1 pKi = 5.1 Binding
Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.Inhibition of [125I]CRH binding to human Corticotropin releasing factor receptor 1.
ChEMBL 387 10 1 8 3.6 CCCN(CC1CC1)c1nc(C)nc(Nc2c(OC)cc(OC)cc2OC)n1 10.1021/jm9900117
CHEMBL413613 219857 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.Binding affinity at human CRF1 receptor (CRFR1) on HeLA cell membranes.
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)=O)NC(=O)[C@@H]1CCCCNC(=O)CC[C@@H](NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1)[C@@H](C)CC)C(N)=O 10.1021/jm034180+
44341463 117196 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 356 6 0 4 5.2 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)n(C)nc12 10.1016/s0960-894x(03)00621-8
CHEMBL324495 117196 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cellsBinding affinity to the human corticotropin releasing factor receptor 1 expressed in HEK273 cells
ChEMBL 356 6 0 4 5.2 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)n(C)nc12 10.1016/s0960-894x(03)00621-8
44392734 72038 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 337 7 0 4 4.3 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2ccccc2C)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL182803 72038 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 337 7 0 4 4.3 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2ccccc2C)c1C 10.1016/j.bmcl.2004.05.072
44392787 138569 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 383 9 0 6 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2ccc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
CHEMBL369333 138569 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 383 9 0 6 4.0 CCCN(CC1CC1)c1nc(C)nc(C(=O)c2ccc(OC)cc2OC)c1C 10.1016/j.bmcl.2004.05.072
44443645 161538 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 434 9 2 7 4.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCO 10.1016/j.bmcl.2007.09.008
CHEMBL400082 161538 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cellsDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in IMR32 cells
ChEMBL 434 9 2 7 4.2 CCc1nc(Oc2cc(C)ccn2)c(CC)nc1N[C@@H]1c2ccccc2C[C@@H]1OCCO 10.1016/j.bmcl.2007.09.008
10295681 25639 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 419 7 1 4 6.4 CCCN(CCC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
CHEMBL128201 25639 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.Binding affinity by displacement of [125I]Tyr-o-CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cell.
ChEMBL 419 7 1 4 6.4 CCCN(CCC)C(=O)c1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C 10.1016/j.bmcl.2003.08.055
10622505 65835 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 8 0 7 4.3 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
CHEMBL169521 65835 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 429 8 0 7 4.3 CCCCN(CC)c1cc(C)nc2c1nnn2-c1ccc(C(C)C)cc1S(C)(=O)=O 10.1021/jm980224g
11453549 77344 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 442 10 0 6 5.9 CCCC(c1ccccc1)N(CCC)c1nc(-c2cc(OC)c(OC)cc2Cl)n(C)n1 10.1021/jm049339c
CHEMBL194877 77344 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 442 10 0 6 5.9 CCCC(c1ccccc1)N(CCC)c1nc(-c2cc(OC)c(OC)cc2Cl)n(C)n1 10.1021/jm049339c
44266513 10994 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 485 6 0 3 8.2 CCN(c1nc(C)cc(-c2cccc(-c3ccccc3)c2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
CHEMBL10032 10994 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 485 6 0 3 8.2 CCN(c1nc(C)cc(-c2cccc(-c3ccccc3)c2)n1)c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00132-8
11291132 71991 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL182595 71991 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N)cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
11291132 71991 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL182595 71991 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 352 6 1 6 3.9 CCCN(CCC)c1cc(C)nc2c(-c3ncc(N)cc3C)c(C)nn12 10.1021/jm040058e
44407873 105012 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 414 5 1 4 5.7 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)Cc2ccc(Cl)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
CHEMBL274388 105012 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenatesDisplacement of [125I]Tyr-o-CRF from CRF1 receptor in rat frontal cortex homogenates
ChEMBL 414 5 1 4 5.7 Cc1cc(C)c(Nc2nc(C)ccc2S(=O)(=O)Cc2ccc(Cl)cc2)c(C)c1 10.1016/j.bmcl.2005.10.097
44306205 209834 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 10 0 5 5.1 CCCN(c1ncc(CC)c(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
CHEMBL63585 209834 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cellsBinding affinity towards human Corticotropin releasing factor receptor 1 by the displacement of [125I]CRF from CHO cells
ChEMBL 395 10 0 5 5.1 CCCN(c1ncc(CC)c(-c2ccc(OC)cc2OC)n1)C(C1CC1)C1CC1 10.1016/j.bmcl.2004.02.053
10958953 210330 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 346 5 1 5 3.7 CC(=O)/C(=N\Nc1ccccc1[N+](=O)[O-])N(C)c1cccc(Cl)c1 10.1021/jm025512y
CHEMBL66602 210330 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human Corticotropin releasing factor receptor 1Binding affinity against human Corticotropin releasing factor receptor 1
ChEMBL 346 5 1 5 3.7 CC(=O)/C(=N\Nc1ccccc1[N+](=O)[O-])N(C)c1cccc(Cl)c1 10.1021/jm025512y
44392724 129890 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 357 6 0 5 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cn3)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL361099 129890 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 357 6 0 5 4.7 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cn3)c(C)nn12 10.1016/j.bmcl.2004.05.056
11348744 133955 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 352 5 0 6 3.1 CCCCN1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL365745 133955 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 352 5 0 6 3.1 CCCCN1CCn2c(=O)n(-c3ccc(OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
44385524 172893 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 445 7 1 6 5.3 CCCCN(CC)c1nc(C)nc2c1nc(O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
CHEMBL426026 172893 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligandBinding affinity for transfected human Corticotropin releasing factor receptor expressed in HEK 293E cells using [125I]TYR-oCRH as the displaced radioligand
ChEMBL 445 7 1 6 5.3 CCCCN(CC)c1nc(C)nc2c1nc(O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00108-0
10717634 11264 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCN(CCC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL10203 11264 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 432 9 0 4 6.5 CCCN(CCC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10026532 104057 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 444 9 0 4 6.5 CCCN(CC1CC1)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL268993 104057 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 444 9 0 4 6.5 CCCN(CC1CC1)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
10576982 127230 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 488 6 0 4 5.2 CCN(CC)c1cc(C)nc(N(CC)c2ccc(I)cc2Br)n1 10.1021/jm980222w
CHEMBL353973 127230 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 488 6 0 4 5.2 CCN(CC)c1cc(C)nc(N(CC)c2ccc(I)cc2Br)n1 10.1021/jm980222w
44341714 16881 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 382 7 0 3 6.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(OC)ccc12 10.1016/s0960-894x(03)00684-x
CHEMBL115566 16881 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligandBinding affinity towards cloned human Corticotropin releasing factor receptor 1 expressed in CHO cells using [125I]o-CRF as the radioligand
ChEMBL 382 7 0 3 6.5 CCCN(CCC)c1cc(C)nc2c(-c3ccc(Cl)cc3)c(OC)ccc12 10.1016/s0960-894x(03)00684-x
10138067 13409 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 6 0 4 6.0 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
CHEMBL1083319 13409 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 438 6 0 4 6.0 CCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
10717634 11264 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 432 9 0 4 6.5 CCCN(CCC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1016/s0960-894x(99)00132-8
CHEMBL10203 11264 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 432 9 0 4 6.5 CCCN(CCC)c1cc(C)nc(N(CC)c2ccc(C(C)C)cc2Br)n1 10.1016/s0960-894x(99)00132-8
44446729 101642 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 390 8 0 3 6.7 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253913 101642 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 390 8 0 3 6.7 CCCN(CCC)c1c(CC)nc(-c2c(C)cc(C)cc2OC)c2ccccc12 10.1016/j.bmcl.2007.12.050
24971237 194828 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL497653 194828 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 380 8 0 6 4.7 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(Cl)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
44587457 194945 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 396 9 0 6 5.0 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(C(F)F)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL498667 194945 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 396 9 0 6 5.0 CCC(CC)Oc1c(C)nc(-c2c(OC)cc(C(F)F)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
11338351 85106 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2094044 85106 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
CHEMBL2109792 85106 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 392 9 0 5 5.6 CCC[C@@H](c1ccccc1)N(CCC)c1nc(-c2ccc(OC)cc2C)n(C)n1 10.1021/jm049339c
9886113 15995 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 378 7 0 4 5.2 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
CHEMBL110609 15995 0 None - 1 Human 8.1 pKi = 8.1 Binding
Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.Inhibition of [125I]o-CRF binding to human Corticotropin releasing factor receptor 1 expressed in CHO cells.
ChEMBL 378 7 0 4 5.2 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1016/s0960-894x(01)00657-6
11773483 72347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
CHEMBL183148 72347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1016/j.bmcl.2004.05.056
20780255 14161 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 7 0 4 6.3 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
CHEMBL1086468 14161 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 452 7 0 4 6.3 CCCN(Cc1c(C(F)(F)F)nc2n(-c3c(C)cc(C)cc3C)c(Cl)cn12)CC1CC1 10.1016/j.bmcl.2010.04.094
15490818 11714 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 461 6 0 5 6.0 CCN(c1nc(C)cc(-c2ccccc2Cl)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL10473 11714 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 461 6 0 5 6.0 CCN(c1nc(C)cc(-c2ccccc2Cl)n1)c1c(Br)cc(OC)cc1OC 10.1016/s0960-894x(99)00132-8
11773483 72347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL183148 72347 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 382 7 0 7 4.3 CCCN(CCC)c1cc(C)nc2c(-c3ncc([N+](=O)[O-])cc3C)c(C)nn12 10.1021/jm040058e
9929418 168547 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 372 4 0 6 5.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
CHEMBL413968 168547 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 372 4 0 6 5.3 CCN(CC)c1nc(C)nc2c1sc(=S)n2-c1c(C)cc(C)cc1C 10.1016/s0960-894x(99)00159-6
10836468 127043 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 431 7 0 6 4.5 CCN(CCOC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL352438 127043 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 431 7 0 6 4.5 CCN(CCOC)c1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9886113 15995 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 7 0 4 5.2 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1021/jm049339c
CHEMBL110609 15995 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 7 0 4 5.2 CCCN(c1nc(-c2ccc(Cl)cc2Cl)n(C)n1)C(C1CC1)C1CC1 10.1021/jm049339c
9803011 105628 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 434 5 0 6 4.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
CHEMBL278895 105628 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRHBinding affinity against human Corticotropin releasing factor receptor 1 expressed in HEK 293E cells using [125I]TYR-oCRH
ChEMBL 434 5 0 6 4.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1016/s0960-894x(99)00159-6
9910700 65819 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169416 65819 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 1 7 4.2 CCC(COC)Nc1nc(C)nc2c1nnn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
9803011 105628 0 None - 1 Human 8.0 pKi = 8.0 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 434 5 0 6 4.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
CHEMBL278895 105628 0 None - 1 Human 8.0 pKi = 8.0 Binding
Compound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptorsCompound was tested for the binding affinity to human corticotropin releasing factor 1 (hCRF1) receptors
ChEMBL 434 5 0 6 4.9 CCN(CC)c1nc(C)nc2c1sc(=O)n2-c1ccc(C(C)C)cc1Br 10.1021/jm990590f
18691325 10963 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 508 6 0 5 6.5 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1c(Br)cc(N(C)C)cc1OC 10.1016/s0960-894x(99)00132-8
CHEMBL10015 10963 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cellsDisplacement of [125I]-TYR-ovine CRH from cloned human corticotropin releasing factor receptor 1 expressed in 293 EBNA cells
ChEMBL 508 6 0 5 6.5 CCN(c1nc(C)cc(-c2ccccc2C(F)(F)F)n1)c1c(Br)cc(N(C)C)cc1OC 10.1016/s0960-894x(99)00132-8
11326060 73791 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 6 1 6 4.4 CCC(CC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
CHEMBL186992 73791 0 None - 1 Human 8.0 pKi = 8.0 Binding
Inhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptorInhibition of [125I]o-CRF binding to CHO cells expressing human CRF1 receptor
ChEMBL 366 6 1 6 4.4 CCC(CC)Nc1cc(C)nc2c(-c3cnc(N(C)C)cc3C)c(C)nn12 10.1021/jm040058e
10646423 66135 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 0 6 4.8 CCC(COC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL170788 66135 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 432 7 0 6 4.8 CCC(COC)Oc1nc(C)nc2c1ncn2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341805 117295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 6 0 5 5.1 COCCN(c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12)C(C)C 10.1016/s0960-894x(03)00622-x
CHEMBL325051 117295 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 406 6 0 5 5.1 COCCN(c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12)C(C)C 10.1016/s0960-894x(03)00622-x
10528542 65863 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 474 9 0 6 5.0 COCCN(CCOC)c1cc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
CHEMBL169641 65863 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cellsBinding affinity to recombinant human Corticotropin releasing factor receptor 1 (hCRF1) expressed in 293EBNA cells
ChEMBL 474 9 0 6 5.0 COCCN(CCOC)c1cc(C)nc2c1nc(C)n2-c1ccc(C(C)C)cc1Br 10.1021/jm980224g
44341835 16267 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 8 0 5 5.5 CCCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
CHEMBL112045 16267 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cellsBinding affinity towards Corticotropin releasing factor receptor 1 was measured through displacement of [125I]sauvagine expressed in HEK293 cells
ChEMBL 420 8 0 5 5.5 CCCN(CCCOC)c1cc(C)nc2c(-c3ccc(Cl)cc3Cl)nn(C)c12 10.1016/s0960-894x(03)00622-x
9822241 70783 8 None -9 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
CHEMBL1807053 70783 8 None -9 2 Rat 8.0 pKi = 8.0 Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation countingDisplacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
ChEMBL 399 8 1 6 5.0 CCC(CC)Nc1nc(C)c(-c2ccc(OC(F)(F)F)cc2OC)nc1OC 10.1021/jm200365y
11546255 194896 0 None 12022 2 Human 8.0 pKi = 8 Binding
Binding affinity to human recombinant CRF1 in HEK cell line assessed as inhibition constant incubated for 2 hrs by MicroBeta scintillation counter methodBinding affinity to human recombinant CRF1 in HEK cell line assessed as inhibition constant incubated for 2 hrs by MicroBeta scintillation counter method
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1016/j.ejmech.2021.113867
CHEMBL498311 194896 0 None 12022 2 Human 8.0 pKi = 8 Binding
Binding affinity to human recombinant CRF1 in HEK cell line assessed as inhibition constant incubated for 2 hrs by MicroBeta scintillation counter methodBinding affinity to human recombinant CRF1 in HEK cell line assessed as inhibition constant incubated for 2 hrs by MicroBeta scintillation counter method
ChEMBL 419 5 0 7 4.9 CCC(CC)c1cc(C)nn2c(-c3sc(N4CCOCC4)nc3Cl)c(C)nc12 10.1016/j.ejmech.2021.113867
9950645 112020 0 None - 1 Human 7.1 pKi = 7.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 357 7 0 5 4.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
CHEMBL311520 112020 0 None - 1 Human 7.1 pKi = 7.1 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 357 7 0 5 4.0 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)n(C)c1=O 10.1016/s0960-894x(03)00483-9
10686834 127237 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 315 5 0 5 4.2 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)=O)cc1SC 10.1021/jm980222w
CHEMBL354022 127237 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1Binding affinity for human recombinant corticotropin releasing factor receptor 1
ChEMBL 315 5 0 5 4.2 CCN(c1nc(C)cc(C)n1)c1ccc(C(C)=O)cc1SC 10.1021/jm980222w
44392742 130351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 409 11 0 4 5.8 CCCN(CC1CC1)c1cc(C(OC)c2c(CC)cc(CC)cc2CC)nc(C)n1 10.1016/j.bmcl.2004.05.072
CHEMBL361831 130351 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for recombinant human CRF1 receptorBinding affinity for recombinant human CRF1 receptor
ChEMBL 409 11 0 4 5.8 CCCN(CC1CC1)c1cc(C(OC)c2c(CC)cc(CC)cc2CC)nc(C)n1 10.1016/j.bmcl.2004.05.072
11440355 69783 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 8 0 5 5.0 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C(C)C)C(C)C 10.1021/jm049339c
CHEMBL178702 69783 0 None - 1 Human 6.0 pKi = 6.0 Binding
Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells Inhibition of [125I][Tyr0]-sauvagine binding to human Corticotropin releasing factor receptor 1 expressed in mouse fibroblast Ltk- cells
ChEMBL 378 8 0 5 5.0 CCCN(c1nc(-c2ccc(Cl)cc2OC)n(C)n1)C(C(C)C)C(C)C 10.1021/jm049339c
11304752 74429 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 422 7 0 7 4.1 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(=O)OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
CHEMBL190661 74429 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cellsBinding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
ChEMBL 422 7 0 7 4.1 CCCC(CCC)N1CCn2c(=O)n(-c3ccc(C(=O)OC)cc3)c3nc(C)cc1c32 10.1021/jm050384+
21916077 14056 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 442 3 0 5 5.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCSCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
CHEMBL1086017 14056 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 minsDisplacement of [125I] Tyr-o-CRF from human CRF[125I]receptor expressed in human IMR-3[125I]cells after 100 mins
ChEMBL 442 3 0 5 5.3 Cc1cc(C)c(-n2c(Cl)cn3c(CN4CCSCC4)c(C(F)(F)F)nc23)c(C)c1 10.1016/j.bmcl.2010.04.094
44317760 212334 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 378 7 1 3 5.7 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(Cl)c1 10.1021/jm049974i
CHEMBL81117 212334 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human corticotropin releasing factor (h-CRF1) receptorBinding affinity towards human corticotropin releasing factor (h-CRF1) receptor
ChEMBL 378 7 1 3 5.7 Cc1ccc(NC(C(=O)CCc2ccncc2)c2ccccc2C)c(Cl)c1 10.1021/jm049974i
44305209 210210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 424 6 0 4 6.6 CCCCN(CC)c1cc(C)nc2c(-c3c(Cl)cc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
CHEMBL65724 210210 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cellsDisplacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
ChEMBL 424 6 0 4 6.6 CCCCN(CC)c1cc(C)nc2c(-c3c(Cl)cc(Cl)cc3Cl)c(C)nn12 10.1016/s0960-894x(98)00372-2
20780175 173382 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 401 6 0 5 5.1 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
CHEMBL428048 173382 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP productionDisplacement of [125I]Tyr-o-CRF from CRF1 receptor expressed in IMR32 cells assessed as inhibition of CRF stimulated cAMP production
ChEMBL 401 6 0 5 5.1 CCN(Cc1c(C)nc2n(-c3c(C)cc(C)cc3C)c3ncccc3n12)CC1CC1 10.1016/j.bmcl.2007.01.008
135553002 212469 0 None - 1 Human 6.0 pKi = 6.0 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 343 7 1 5 4.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1O 10.1016/s0960-894x(03)00483-9
CHEMBL82265 212469 0 None - 1 Human 6.0 pKi = 6.0 Binding
Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.Affinity for Corticotropin releasing factor receptor 1 on IMR-32 (human neuroblastoma) cells by [125I]-sauvagine displacement.
ChEMBL 343 7 1 5 4.4 CCCN(CCC)c1c(C)nc(-c2c(C)cc(C)cc2OC)nc1O 10.1016/s0960-894x(03)00483-9
44397631 73920 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 460 7 0 4 6.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12 10.1016/j.bmcl.2005.06.028
CHEMBL187577 73920 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for human corticotropin releasing factor receptor 1Binding affinity for human corticotropin releasing factor receptor 1
ChEMBL 460 7 0 4 6.2 CCCN(CC1CC1)C(=O)c1c(CC)nc2n(-c3c(C)cc(C)cc3C)c3ccc(F)cc3n12 10.1016/j.bmcl.2005.06.028
11689443 71141 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 6 0 4 4.4 CCc1nc2n(c1C(=O)N(CC)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
CHEMBL181283 71141 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 380 6 0 4 4.4 CCc1nc2n(c1C(=O)N(CC)CC1CC1)CCN2c1c(C)cc(C)cc1C 10.1016/j.bmcl.2005.05.117
20780028 138150 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 414 7 0 4 5.1 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1Cl 10.1016/j.bmcl.2005.05.117
CHEMBL368879 138150 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cellsDisplacement of [125I]-Tyr-o- CRF from human corticotropin releasing factor receptor 1 expressed in IMR-32 cells
ChEMBL 414 7 0 4 5.1 CCCN(CC1CC1)C(=O)c1c(CC)nc2n1CCN2c1c(C)cc(C)cc1Cl 10.1016/j.bmcl.2005.05.117
44587377 179706 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 343 7 1 5 4.7 CCC(CC)Nc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
CHEMBL451660 179706 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cellsDisplacement of [125I]sauvagine from human CRF1 receptor expressed in IMR32 cells
ChEMBL 343 7 1 5 4.7 CCC(CC)Nc1c(C)nc(-c2c(C)cc(C)cc2OC)nc1OC 10.1016/j.bmcl.2008.07.063
10616689 65511 1 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 333 3 0 3 4.7 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980223o
CHEMBL168568 65511 1 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was determined against corticotropin releasing factor receptor 1Binding affinity was determined against corticotropin releasing factor receptor 1
ChEMBL 333 3 0 3 4.7 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980223o
10616689 65511 1 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 333 3 0 3 4.7 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
CHEMBL168568 65511 1 None - 1 Rat 7.0 pKi = 7.0 Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1Binding affinity was measured on rat Corticotropin releasing factor receptor 1
ChEMBL 333 3 0 3 4.7 Cc1cc(C)nc(N(C)c2ccc(C(C)C)cc2Br)n1 10.1021/jm980222w
44446719 101553 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2007.12.050
CHEMBL253286 101553 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cellsDisplacement of [125I]sauvagine from CRF1 receptor expressed in human IMR32 cells
ChEMBL 352 6 0 2 6.5 CCCN(CCC)c1c(C)nc(-c2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2007.12.050
44389088 69748 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 6 1 4 7.5 CC(C)N(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)C(C)C 10.1016/j.bmcl.2004.10.055
CHEMBL178523 69748 0 None - 1 Human 5.0 pKi = 5.0 Binding
Inhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cellsInhibition of [125I]Tyr-o-CRF binding to Corticotropin releasing factor receptor 1 expressed in IMR-32 human neuroblastoma cells
ChEMBL 459 6 1 4 7.5 CC(C)N(Cc1sc(Nc2c(Cl)cc(Cl)cc2Cl)nc1C(F)(F)F)C(C)C 10.1016/j.bmcl.2004.10.055
10379 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
9884366 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
CHEMBL482950 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
DB12572 9833 39 None - 1 Human 6.5 pIC50 = 6.5 Binding
Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.Displacement of ovine [125-I]-CRF from human CRF1 receptor expressed in CHO cell membranes.
Guide to Pharmacology 340 5 1 7 3.3 CC[C@H](Nc1nc(C)nc2n1nc(c2c1ccc(nc1C)OC)C)C 28174066
10377 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding to rat cortex.In vitro binding to rat cortex.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
9818802 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding to rat cortex.In vitro binding to rat cortex.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
CHEMBL270738 7962 27 None 1 2 Rat 8.2 pIC50 = 8.2 Binding
In vitro binding to rat cortex.In vitro binding to rat cortex.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7477349
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7692441
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8612563
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9326293
912 7950 0 None 1 4 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9851694
913 7951 0 None 44 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
913 7951 0 None 44 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15450949
913 7951 0 None 44 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9326293
913 7951 0 None 44 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9851694
16133798 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
16133798 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9851694
16133798 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
925 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
925 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9851694
925 7294 0 None -3 4 Human 8.3 pKd = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
920 10721 0 None -1 3 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
920 10721 0 None -1 3 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11416224
920 10721 0 None -1 3 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7477349
920 10721 0 None -1 3 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8612563
920 10721 0 None -1 3 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
919 10722 0 None -1 4 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
919 10722 0 None -1 4 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15450949
919 10722 0 None -1 4 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8612563
921 10724 0 None -8912 4 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15450949
CHEMBL429970 10724 0 None -8912 4 Human 5.4 pKd None 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15450949
155817385 7148 0 None -31 3 Human 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
923 7148 0 None -31 3 Human 7.6 pKd None 7.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 15450949
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7477349
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8612563
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9326293
918 10261 0 None -3 4 Human 8.0 pKd None 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9918582
922 10729 0 None 1 3 Human 8.6 pKd None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11123370
922 10729 0 None 1 3 Human 8.6 pKd None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7477349
177990 7214 23 125I-Sauvagine -1 2 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
3489 7214 23 125I-Sauvagine -1 2 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
CHEMBL296641 7214 23 125I-Sauvagine -1 2 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
177990 7214 23 3H-NBI 35965 + GTP GammaS -1 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
3489 7214 23 3H-NBI 35965 + GTP GammaS -1 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
CHEMBL296641 7214 23 3H-NBI 35965 + GTP GammaS -1 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
177990 7214 23 125I-Sauvigine + GTP GammaS -1 2 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
3489 7214 23 125I-Sauvigine + GTP GammaS -1 2 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
CHEMBL296641 7214 23 125I-Sauvigine + GTP GammaS -1 2 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
177990 7214 23 125I-Sauvagine -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
3489 7214 23 125I-Sauvagine -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
CHEMBL296641 7214 23 125I-Sauvagine -1 2 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
177990 7214 23 125I-Astressin + GTP GammaS -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
3489 7214 23 125I-Astressin + GTP GammaS -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
CHEMBL296641 7214 23 125I-Astressin + GTP GammaS -1 2 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC None
10377 7962 27 None -1 2 Human 8.1 pKi = 8.1 Binding
Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
9818802 7962 27 None -1 2 Human 8.1 pKi = 8.1 Binding
Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
CHEMBL270738 7962 27 None -1 2 Human 8.1 pKi = 8.1 Binding
Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.Antagonism of CRF-stimulated adenylate cyclase activity by the CRF1 receptor endogenously expressed in human IMR32 cells.
Guide to Pharmacology 327 6 0 3 6.0 CCC(Oc1cc(C)nc(c1C)Oc1c(C)cc(cc1C)C)CC 18260619
10378 10757 37 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 21074436
11596613 10757 37 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 21074436
CHEMBL1287935 10757 37 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 21074436
DB12512 10757 37 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 8 4.6 COc1ccc(c(c1)C)c1c(C)nn2c1nc(C)cc2N[C@H](c1onc(n1)C)CC 21074436
10375 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 16078829
9888194 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 16078829
CHEMBL188907 9516 18 None - 1 Human 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 416 6 0 4 6.5 CCCC(N1CCn2c3c1cc(C)nc3c(n2)c1ccc(cc1Cl)Cl)CCC 16078829
11025 9517 7 None -1 2 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 12957366
11713007 9517 7 None -1 2 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 12957366
CHEMBL380800 9517 7 None -1 2 Rat 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 400 4 0 4 5.7 CC[C@H]1Cn2nc(c3c2c(N1CC1CC1)cc(n3)C)c1ccc(cc1Cl)Cl 12957366
177990 7214 23 None -1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 8940412
3489 7214 23 None -1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 8940412
CHEMBL296641 7214 23 None -1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 378 6 0 4 5.9 CCCCN(c1nc(C)nc2c1c(C)c(n2c1c(C)cc(cc1C)C)C)CC 8940412
3499 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10669572
9909468 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10669572
CHEMBL44698 8230 28 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 409 7 1 7 3.8 COCC(Nc1nc(C)nc2n1nc(c2c1ccc(cc1Cl)Cl)C)COC 10669572
176157 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 8893829
3512 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 8893829
CHEMBL45281 9515 28 None 9 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 7 1 4 6.8 CCCN(c1nc(C)nc(c1Cl)Nc1c(Cl)cc(cc1Cl)Cl)CC1CC1 8893829
3520 10041 54 None 1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10867111
9821250 10041 54 None 1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10867111
CHEMBL309138 10041 54 None 1 2 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 380 7 0 6 4.4 CCCN(c1cc(C)nc2n1nc(c2c1cnc(cc1C)N(C)C)C)CCC 10867111
16133798 7294 0 None -3 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24269930
925 7294 0 None -3 4 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 24269930
3533 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 11907190
5282340 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 11907190
CHEMBL291657 7989 24 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 482 8 0 4 7.5 C#CCN([C@H](c1ccc(c(c1)F)C)CC1CC1)c1sc(c(n1)c1cc(C)c(cc1Cl)OC)C 11907190