Ligand source activities (1 row/activity)





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

53322111 57382 None 0 Human Functional pEC50 = 9 9.0 125 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 482 7 4 8 3.4 C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/ml100229v
CHEMBL1651721 57382 None 0 Human Functional pEC50 = 9 9.0 125 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 482 7 4 8 3.4 C#CCNC(=O)CNc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/ml100229v
53320793 57384 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651723 57384 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
11618319 79810 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 403 4 1 8 4.6 COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL211871 79810 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 403 4 1 8 4.6 COc1cccc(-c2nc(SC)nc3sc(C(=O)OC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
11509369 80039 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 390 3 2 6 4.3 CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
CHEMBL212815 80039 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 390 3 2 6 4.3 CSc1nc(-c2cccc(F)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
44440750 97380 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 610 13 3 7 6.2 CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL269261 97380 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 610 13 3 7 6.2 CC(C)(C)Oc1ccc(C[C@H](NC(=O)CCCCNc2cc(-c3cccnc3)nn2-c2ccc(C(C)(C)C)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44440752 169130 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 568 13 4 7 5.1 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL439392 169130 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 568 13 4 7 5.1 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@@H](Cc2cccc(O)c2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
11502667 78447 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 420 4 2 7 4.3 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F 10.1021/jm060247s
CHEMBL211129 78447 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 420 4 2 7 4.3 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1F 10.1021/jm060247s
44572264 179544 None 23 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
CHEMBL474041 179544 None 23 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase productionAgonist activity at human luteinizing hormone receptor expressed in CHOK1 cells assessed as c-AMP-mediated luciferase production
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
44440751 93881 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 554 12 4 7 5.3 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL247700 93881 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 554 12 4 7 5.3 CC(C)(C)c1ccc(-n2nc(-c3ccccn3)cc2NCCCCCC(=O)N[C@H](C(N)=O)c2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
44440753 148609 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 537 12 2 5 5.5 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL393847 148609 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 537 12 2 5 5.5 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@H](CC(N)=O)Cc2ccccc2)cc1 10.1016/j.bmcl.2006.12.062
11531195 138885 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 388 3 3 7 3.9 CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
CHEMBL378091 138885 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 388 3 3 7 3.9 CSc1nc(-c2cccc(O)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/jm060247s
9915237 93576 None 1 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL246321 93576 None 1 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44440784 93431 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL245663 93431 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(CCCCC(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)cc2-c2ccncc2)cc1 10.1016/j.bmcl.2006.12.062
53320759 57401 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651829 57401 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1136 18 5 17 10.1 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440746 152816 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL397316 152816 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3ccncc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
53323417 57395 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651823 57395 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
9887381 79562 None 27 Human Functional pEC50 = 6.5 6.5 27 2
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL211405 79562 None 27 Human Functional pEC50 = 6.5 6.5 27 2
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1021/jm060247s
53324744 57404 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651831 57404 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53320758 57396 None 0 Human Functional pEC50 = 7.4 7.4 21 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651824 57396 None 0 Human Functional pEC50 = 7.4 7.4 21 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44255904 57400 None 0 Human Functional pEC50 = 8.3 8.3 79 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 682 17 4 14 3.9 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651828 57400 None 0 Human Functional pEC50 = 8.3 8.3 79 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 682 17 4 14 3.9 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCN=[N+]=[N-])nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440748 93921 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 609 8 3 6 6.6 CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL247945 93921 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 609 8 3 6 6.6 CC(C)(C)c1ccc(-n2nc(-c3cc4ccccc4cn3)cc2-c2cccc(C(=O)N[C@@H](Cc3ccc(O)cc3)C(N)=O)c2)cc1 10.1016/j.bmcl.2006.12.062
53324743 57398 None 0 Human Functional pEC50 = 7.3 7.3 18 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651826 57398 None 0 Human Functional pEC50 = 7.3 7.3 18 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1313 30 5 21 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53318121 57394 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651822 57394 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53324742 57397 None 0 Human Functional pEC50 = 7.2 7.2 26 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651825 57397 None 0 Human Functional pEC50 = 7.2 7.2 26 2
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1269 27 5 20 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCOCCn4cc(COc5ccc([C@@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
53324741 57393 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651821 57393 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1225 24 5 19 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
44440754 167263 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 496 10 2 5 6.0 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)NCCc2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL429108 167263 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPAAgonist activity at human LH receptor expressed in CHO cells assessed as production of cAMP after 60 mins by SPA
ChEMBL 496 10 2 5 6.0 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)NCCc2ccc(O)cc2)cc1 10.1016/j.bmcl.2006.12.062
53320760 57403 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
CHEMBL1651830 57403 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assayAgonist activity at human LH receptor expressed in CHO-K1 cells assessed as stimulation of luciferase activity by CRE-driven luciferase reporter gene assay
ChEMBL 1180 21 5 18 10.2 CSc1nc(-c2cccc(NCC(=O)NCc3cn(CCOCCn4cc(COc5ccc([C@]6(C)CC(C)(C)N(C(C)=O)c7ccc(NC(=O)c8ccc(-c9ccccc9)cc8)cc76)cc5)nn4)nn3)c2)c2c(N)c(C(=O)NC(C)(C)C)sc2n1 10.1021/ml100229v
11654606 138507 None 1 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 416 4 1 7 4.5 COc1cccc(-c2nc(SC)nc3sc(C(=O)N(C)C(C)(C)C)c(N)c23)c1 10.1021/jm060247s
CHEMBL377399 138507 None 1 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 416 4 1 7 4.5 COc1cccc(-c2nc(SC)nc3sc(C(=O)N(C)C(C)(C)C)c(N)c23)c1 10.1021/jm060247s
11539288 138758 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 432 5 2 8 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1OC 10.1021/jm060247s
CHEMBL377769 138758 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulationAgonist activity at LHCGR expressed in HEK293 EM cells measured by intracellular cAMP accumulation
ChEMBL 432 5 2 8 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1OC 10.1021/jm060247s
155566723 176028 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 457 4 1 3 6.3 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4587440 176028 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 457 4 1 3 6.3 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155563159 175416 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4573509 175416 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(Cl)cc2)cc1 10.1021/acs.jmedchem.9b01382
155546314 173648 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 478 4 1 3 7.5 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4531781 173648 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 478 4 1 3 7.5 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155558589 174856 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 402 2 1 2 6.2 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1 10.1021/acs.jmedchem.9b01382
CHEMBL4560733 174856 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 402 2 1 2 6.2 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1 10.1021/acs.jmedchem.9b01382
155524816 171102 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 425 4 2 4 4.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(F)c(C(N)=O)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4456365 171102 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 425 4 2 4 4.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2ccc(F)c(C(N)=O)c2)cc1 10.1021/acs.jmedchem.9b01382
155516839 170211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1ccc(F)c(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4443605 170211 None 0 Human Functional pIC50 = 6.8 6.8 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1ccc(F)c(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600336 171240 None 17 Human Functional pIC50 = 6.7 6.7 -4 3
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4458424 171240 None 17 Human Functional pIC50 = 6.7 6.7 -4 3
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155530584 171657 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 438 2 1 2 6.5 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(F)c(F)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4464604 171657 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 438 2 1 2 6.5 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(F)c(F)c1 10.1021/acs.jmedchem.9b01382
155528786 171484 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 394 4 1 4 4.9 COc1cc(NC(=O)N2CCc3sccc3[C@@H]2c2ccccc2)cc(OC)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4461980 171484 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 394 4 1 4 4.9 COc1cc(NC(=O)N2CCc3sccc3[C@@H]2c2ccccc2)cc(OC)c1 10.1021/acs.jmedchem.9b01382
155542952 173289 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 424 5 1 5 5.0 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4522381 173289 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 424 5 1 5 5.0 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
2741928 176285 None 2 Rat Functional pIC50 = 6.7 6.7 1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4593222 176285 None 2 Rat Functional pIC50 = 6.7 6.7 1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Rat Functional pIC50 = 7.6 7.6 28 3
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Rat Functional pIC50 = 7.6 7.6 28 3
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155555227 174457 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 419 2 2 3 4.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(=O)[nH]c1 10.1021/acs.jmedchem.9b01382
CHEMBL4551301 174457 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 419 2 2 3 4.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(=O)[nH]c1 10.1021/acs.jmedchem.9b01382
155532999 171906 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 416 2 1 2 6.5 Cc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4468163 171906 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 416 2 1 2 6.5 Cc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155561384 175788 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4581889 175788 None 0 Human Functional pIC50 = 6.6 6.6 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 398 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cccc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155555948 174617 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 458 4 1 4 5.7 O=C(Nc1ccc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4555151 174617 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 458 4 1 4 5.7 O=C(Nc1ccc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155567488 176058 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccc(F)c1 10.1021/acs.jmedchem.9b01382
CHEMBL4588196 176058 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccc(F)c1 10.1021/acs.jmedchem.9b01382
155564366 175259 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1F 10.1021/acs.jmedchem.9b01382
CHEMBL4570127 175259 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 420 2 1 2 6.4 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccccc1F 10.1021/acs.jmedchem.9b01382
155565197 175678 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 460 4 1 3 7.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4579421 175678 None 0 Human Functional pIC50 = 6.5 6.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 460 4 1 3 7.4 O=C(Nc1cccc(Oc2ccccc2)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
155535600 172154 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 440 5 1 5 5.1 COc1ccc(C2c3ccsc3CCN2C(=S)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471875 172154 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 440 5 1 5 5.1 COc1ccc(C2c3ccsc3CCN2C(=S)Nc2cc(OC)cc(OC)c2)cc1 10.1021/acs.jmedchem.9b01382
155533073 171915 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 2 1 2 7.3 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4468307 171915 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 2 1 2 7.3 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(C(F)(F)F)cc1 10.1021/acs.jmedchem.9b01382
2741928 176285 None 2 Human Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4593222 176285 None 2 Human Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
29993669 172127 None 0 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471621 172127 None 0 Human Functional pIC50 = 6.4 6.4 1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
29993669 172127 None 0 Rat Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471621 172127 None 0 Rat Functional pIC50 = 6.4 6.4 -1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
139600336 171240 None 17 Rat Functional pIC50 = 7.3 7.3 4 3
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4458424 171240 None 17 Rat Functional pIC50 = 7.3 7.3 4 3
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.1021/acs.jmedchem.9b01382
155568207 176176 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 436 2 1 2 6.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4590976 176176 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 436 2 1 2 6.9 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
29993670 170636 None 0 Rat Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4449797 170636 None 0 Rat Functional pIC50 = 5.3 5.3 1 2
Antagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assayAntagonist activity at rat luteinizing hormone receptor expressed in rat ovary granulosa GLHR15 cell suspension assessed as reduction in agonist-induced cAMP production preincubated for 30 mins followed by agonist solution addition after 30 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155563505 175414 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccncc1 10.1021/acs.jmedchem.9b01382
CHEMBL4573451 175414 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1ccncc1 10.1021/acs.jmedchem.9b01382
155561534 175743 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 392 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4580951 175743 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 392 3 1 3 5.6 COc1ccc(C2c3ccsc3CCN2C(=O)Nc2cc(C)cc(C)c2)cc1 10.1021/acs.jmedchem.9b01382
29993670 170636 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4449797 170636 None 0 Human Functional pIC50 = 5.2 5.2 -1 2
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 432 3 1 3 6.2 COc1ccc([C@@H]2c3ccsc3CCN2C(=O)Nc2cc(Cl)cc(Cl)c2)cc1 10.1021/acs.jmedchem.9b01382
155534855 172091 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccnc1 10.1021/acs.jmedchem.9b01382
CHEMBL4471103 172091 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 403 2 1 3 5.6 O=C(Nc1cc(Cl)cc(Cl)c1)N1CCc2sccc2C1c1cccnc1 10.1021/acs.jmedchem.9b01382
155527311 171355 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 3 1 3 6.6 O=C(Nc1ccc(F)c(OC(F)(F)F)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4460075 171355 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 470 3 1 3 6.6 O=C(Nc1ccc(F)c(OC(F)(F)F)c1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
57325683 74979 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 368 2 1 2 5.6 O=C(Nc1ccccc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL2032175 74979 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 368 2 1 2 5.6 O=C(Nc1ccccc1)N1CCc2sccc2C1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Functional pIC50 = 7.0 7.0 -28 3
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Functional pIC50 = 7.0 7.0 -28 3
Antagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assayAntagonist activity at human luteinizing hormone receptor assessed as reduction in agonist-induced cAMP production preincubated for 20 mins followed by agonist solution addition after 60 mins by cell based TR-FRET assay
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL412984 215498 None 0 Rat Functional pKd = 9.4 9.4 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL None None None CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00130a019
44314940 82146 None 0 Rat Functional pKd = 9.3 9.3 - 0
Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL216617 82146 None 0 Rat Functional pKd = 9.3 9.3 - 0
Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)Luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44315218 98497 None 0 Rat Functional pKd = 8.7 8.7 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275694 98497 None 0 Rat Functional pKd = 8.7 8.7 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314845 161989 None 0 Rat Functional pKd = 8.0 8.0 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL415109 161989 None 0 Rat Functional pKd = 8.0 8.0 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314939 161427 None 0 Rat Functional pKd = 7.9 7.9 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL412573 161427 None 0 Rat Functional pKd = 7.9 7.9 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
14557614 89412 None 0 Rat Functional pKd = 7.8 7.8 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369800 89412 None 0 Rat Functional pKd = 7.8 7.8 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369798 212149 None 0 Rat Functional pKd = 7.8 7.8 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)Cc1ccc2ccccc2c1 10.1021/jm00130a019
14557592 89408 None 0 Rat Functional pKd = 6.7 6.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369791 89408 None 0 Rat Functional pKd = 6.7 6.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
14557629 89415 None 0 Rat Functional pKd = 5.7 5.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369809 89415 None 0 Rat Functional pKd = 5.7 5.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
14557620 89416 None 0 Rat Functional pKd = 6.7 6.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369810 89416 None 0 Rat Functional pKd = 6.7 6.7 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
44314797 167497 None 0 Rat Functional pKd = 7.6 7.6 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL429543 167497 None 0 Rat Functional pKd = 7.6 7.6 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557600 89417 None 0 Rat Functional pKd = 6.6 6.6 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369813 89417 None 0 Rat Functional pKd = 6.6 6.6 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557594 89407 None 0 Rat Functional pKd = 5.6 5.6 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369790 89407 None 0 Rat Functional pKd = 5.6 5.6 - 0
In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)In vivo luteinizing hormone inhibiting potency in rats is expressed as negative logarithm of the concentration (antagonist)
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
44314843 96783 None 0 Rat Functional pKd = 8.5 8.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL264298 96783 None 0 Rat Functional pKd = 8.5 8.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314937 96915 None 0 Rat Functional pKd = 8.5 8.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
CHEMBL265413 96915 None 0 Rat Functional pKd = 8.5 8.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
44314846 98325 None 0 Rat Functional pKd = 8.4 8.4 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL274609 98325 None 0 Rat Functional pKd = 8.4 8.4 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314897 160554 None 0 Rat Functional pKd = 7.5 7.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL411175 160554 None 0 Rat Functional pKd = 7.5 7.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369793 212148 None 0 Rat Functional pKd = 6.5 6.5 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)/C=C/c1ccc(OC)cc1 10.1021/jm00130a019
14557590 89414 None 0 Rat Functional pKd = 6.4 6.4 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369808 89414 None 0 Rat Functional pKd = 6.4 6.4 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44315053 98501 None 0 Rat Functional pKd = 8.2 8.2 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275709 98501 None 0 Rat Functional pKd = 8.2 8.2 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369807 212150 None 0 Rat Functional pKd = 8.2 8.2 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369787 212146 None 0 Rat Functional pKd = 7.2 7.2 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)/C=C\c1ccc(OC)cc1 10.1021/jm00130a019
44314898 141942 None 0 Rat Functional pKd = 7.1 7.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL386525 141942 None 0 Rat Functional pKd = 7.1 7.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44315220 161847 None 0 Rat Functional pKd = 8.1 8.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL413887 161847 None 0 Rat Functional pKd = 8.1 8.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557616 89410 None 0 Rat Functional pKd = 6.1 6.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369799 89410 None 0 Rat Functional pKd = 6.1 6.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557588 89413 None 0 Rat Functional pKd = 6.1 6.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369806 89413 None 0 Rat Functional pKd = 6.1 6.1 - 0
In vivo inhibition of leutenising hormone in rats.In vivo inhibition of leutenising hormone in rats.
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
1159 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
1159 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
CHEMBL1201419 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
CHEMBL1201419 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
DB00044 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
DB00044 2319 None 0 Human Functional pIC50 = 10.4 10.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095




Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name
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ligand
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Type
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p-value
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selectivity
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GPCRs
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weight
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LogP

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DOI

9887381 79562 None 27 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1039/c1md00145k
CHEMBL211405 79562 None 27 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at LHCGR (unknown origin)Agonist activity at LHCGR (unknown origin)
ChEMBL 402 4 2 7 4.2 COc1cccc(-c2nc(SC)nc3sc(C(=O)NC(C)(C)C)c(N)c23)c1 10.1039/c1md00145k
139600337 173897 None 15 Human Binding pIC50 = 5.9 5.9 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.9 5.9 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.8 5.8 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600336 171240 None 17 Human Binding pIC50 = 6.7 6.7 - 1
Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL5210121
CHEMBL4458424 171240 None 17 Human Binding pIC50 = 6.7 6.7 - 1
Affinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGRAffinity On-target Cellular interaction (Cell-based assay (LH Antagonism)) EUB0000240b LHCGR
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL5210121
139600336 171240 None 17 Human Binding pIC50 = 6.7 6.7 - 1
Cell-based assay (LH Antagonism)Cell-based assay (LH Antagonism)
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL4507317
CHEMBL4458424 171240 None 17 Human Binding pIC50 = 6.7 6.7 - 1
Cell-based assay (LH Antagonism)Cell-based assay (LH Antagonism)
ChEMBL 459 4 1 5 5.1 O=C(Nc1cnc(Oc2ccc(F)cc2)nc1)N1CCc2ncccc2[C@@H]1c1ccc(F)cc1 10.6019/CHEMBL4507317
139600337 173897 None 15 Human Binding pIC50 = 6.7 6.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 6.7 6.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 4 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 5.7 5.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.7 5.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 10 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 5.7 5.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.7 5.7 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 16 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
44572264 179544 None 23 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
CHEMBL474041 179544 None 23 Human Binding pIC50 = 5.6 5.6 - 0
Displacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cellsDisplacement of [3H]Org43553 from human luteinizing hormone receptor expressed in CHOK1 cells
ChEMBL 357 4 1 2 6.1 O=C(NC1CCCC1)Oc1cc(-c2ccccc2)cc(-c2ccccc2)c1 10.1021/jm801561h
139600337 173897 None 15 Human Binding pIC50 = 5.6 5.6 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 5.6 5.6 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 100 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 6.2 6.2 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 6.2 6.2 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in Org 43553-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
139600337 173897 None 15 Human Binding pIC50 = 7.0 7.0 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
CHEMBL4537998 173897 None 15 Human Binding pIC50 = 7.0 7.0 - 0
Negative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to controlNegative allosteric modulation of human luteinizing hormone receptor assessed as reduction in glycoprotein human luteinizing hormone-induced agonist activity preincubated for 20 mins followed by 1 times EC80 of agonist addition and measured after 60 mins by cell based TR-FRET assay relative to control
ChEMBL 473 4 1 3 6.8 O=C(Nc1ccc(Oc2ccc(F)cc2)cc1)N1CCc2ncccc2[C@@H]1c1ccc(Cl)cc1 10.1021/acs.jmedchem.9b01382
44267887 98534 None 0 Rat Binding pKd = 9.9 9.9 41 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 98534 None 0 Rat Binding pKd = 9.9 9.9 41 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267907 16338 None 0 Rat Binding pKd = 9.3 9.3 -1 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 16338 None 0 Rat Binding pKd = 9.3 9.3 -1 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
9854500 102327 None 0 Rat Binding pKd = 8.8 8.8 1 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 102327 None 0 Rat Binding pKd = 8.8 8.8 1 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267812 98156 None 0 Rat Binding pKd = 8.8 8.8 8 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 98156 None 0 Rat Binding pKd = 8.8 8.8 8 2
In vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cellsIn vitro binding ability against Luteinizing hormone-releasing hormone release in rat pituitary cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL412984 215498 None 0 Rat Binding pKi = 10.7 10.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00130a019
44350635 157305 None 0 Rat Binding pKi = 10.6 10.6 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1292 32 15 13 0.5 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL407606 157305 None 0 Rat Binding pKi = 10.6 10.6 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1292 32 15 13 0.5 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL407123 215101 None 0 Rat Binding pKi = 10.4 10.4 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(=O)O 10.1021/jm00099a017
44350493 155843 None 0 Rat Binding pKi = 10.1 10.1 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1296 32 15 14 -0.4 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL405737 155843 None 0 Rat Binding pKi = 10.1 10.1 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1296 32 15 14 -0.4 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350501 141683 None 0 Rat Binding pKi = 10.0 10.0 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1220 32 14 14 -0.8 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL385042 141683 None 0 Rat Binding pKi = 10.0 10.0 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1220 32 14 14 -0.8 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1cccc2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350636 162041 None 0 Rat Binding pKi = 9.8 9.8 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1200 33 14 15 -1.9 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL415571 162041 None 0 Rat Binding pKi = 9.8 9.8 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1200 33 14 15 -1.9 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1ccc(OC)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350565 141760 None 0 Rat Binding pKi = 9.7 9.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL385468 141760 None 0 Rat Binding pKi = 9.7 9.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1209 32 15 14 -1.4 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44350487 167335 None 0 Rat Binding pKi = 9.7 9.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1306 32 14 13 0.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL429240 167335 None 0 Rat Binding pKi = 9.7 9.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1306 32 14 13 0.9 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)N(C)C(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44314940 82146 None 0 Rat Binding pKi = 9.6 9.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL216617 82146 None 0 Rat Binding pKi = 9.6 9.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1041 26 10 10 2.8 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
9915237 93576 None 1 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]hCG from LH receptorDisplacement of [125I]hCG from LH receptor
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
CHEMBL246321 93576 None 1 Human Binding pKi = 9.5 9.5 - 1
Displacement of [125I]hCG from LH receptorDisplacement of [125I]hCG from LH receptor
ChEMBL 539 11 3 6 4.9 CC(C)(C)c1ccc(-n2nc(-c3cccnc3)cc2CCCCC(=O)N[C@@H](Cc2ccc(O)cc2)C(N)=O)cc1 10.1016/j.bmcl.2006.12.062
44350502 168934 None 0 Rat Binding pKi = 9.4 9.4 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1298 33 14 14 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
CHEMBL437798 168934 None 0 Rat Binding pKi = 9.4 9.4 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1298 33 14 14 -0.2 CCNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
44314937 96915 None 0 Rat Binding pKi = 9.3 9.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
CHEMBL265413 96915 None 0 Rat Binding pKi = 9.3 9.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1024 25 11 10 1.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CC12CC3CC(CC(C3)C1)C2 10.1021/jm00130a019
44315218 98497 None 0 Rat Binding pKi = 9.3 9.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275694 98497 None 0 Rat Binding pKi = 9.3 9.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314843 96783 None 0 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL264298 96783 None 0 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1106 28 10 10 3.9 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
11980076 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
36523 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
36523.0 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
638793 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
638793.0 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
CHEMBL1007 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
CHEMBL1981292 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
DB00644 210912 None 21 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00130a019
44315220 161847 None 0 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL413887 161847 None 0 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1044 27 11 10 2.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369787 212146 None 0 Rat Binding pKi = 8.9 8.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)/C=C\c1ccc(OC)cc1 10.1021/jm00130a019
44350492 97005 None 0 Rat Binding pKi = 8.9 8.9 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1223 32 14 14 -1.1 CCNC(=O)[C@H]1CCCN1C(=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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL266205 97005 None 0 Rat Binding pKi = 8.9 8.9 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary Luteinizing Hormone Releasing Hormone (LHRH) receptor binding assay
ChEMBL 1223 32 14 14 -1.1 CCNC(=O)[C@H]1CCCN1C(=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](CO)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
44314797 167497 None 0 Rat Binding pKi = 8.8 8.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL429543 167497 None 0 Rat Binding pKi = 8.8 8.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1030 26 11 10 2.1 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44314939 161427 None 0 Rat Binding pKi = 8.7 8.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL412573 161427 None 0 Rat Binding pKi = 8.7 8.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1032 26 11 11 1.5 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)COc1cccc2ccccc12 10.1021/jm00130a019
14557596 89400 None 0 Rat Binding pKi = 6.9 6.9 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 960 27 11 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369780 89400 None 0 Rat Binding pKi = 6.9 6.9 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 960 27 11 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557594 89407 None 0 Rat Binding pKi = 5.9 5.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369790 89407 None 0 Rat Binding pKi = 5.9 5.9 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 932 25 11 10 0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
14557629 89415 None 0 Rat Binding pKi = 5.8 5.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369809 89415 None 0 Rat Binding pKi = 5.8 5.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 906 25 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccnc1 10.1021/jm00130a019
CHEMBL2369793 212148 None 0 Rat Binding pKi = 6.8 6.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)/C=C/c1ccc(OC)cc1 10.1021/jm00130a019
14557588 89413 None 0 Rat Binding pKi = 7.8 7.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369806 89413 None 0 Rat Binding pKi = 7.8 7.8 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 980 26 11 10 0.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557627 89402 None 0 Rat Binding pKi = 5.8 5.8 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 908 26 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccnc1 10.1021/jm00130a019
CHEMBL2369783 89402 None 0 Rat Binding pKi = 5.8 5.8 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 908 26 10 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccnc1 10.1021/jm00130a019
44314897 160554 None 0 Rat Binding pKi = 7.7 7.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL411175 160554 None 0 Rat Binding pKi = 7.7 7.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1033 28 9 10 3.2 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557582 89403 None 0 Rat Binding pKi = 6.7 6.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 946 26 11 10 0.7 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369784 89403 None 0 Rat Binding pKi = 6.7 6.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 946 26 11 10 0.7 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
44350488 82454 None 0 Rat Binding pKi = 8.7 8.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1219 32 14 13 -0.2 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL217405 82454 None 0 Rat Binding pKi = 8.7 8.7 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1219 32 14 13 -0.2 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL2369807 212150 None 0 Rat Binding pKi = 8.7 8.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
10418860 98334 None 0 Rat Binding pKi = 8.6 8.6 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1211 33 14 14 -1.2 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
CHEMBL274682 98334 None 0 Rat Binding pKi = 8.6 8.6 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1211 33 14 14 -1.2 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)CN(C)C(C)=O 10.1021/jm00099a017
44315053 98501 None 0 Rat Binding pKi = 8.6 8.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL275709 98501 None 0 Rat Binding pKi = 8.6 8.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1027 25 10 10 2.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557592 89408 None 0 Rat Binding pKi = 6.7 6.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369791 89408 None 0 Rat Binding pKi = 6.7 6.7 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 918 24 11 10 0.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1c[nH]c2ccccc12 10.1021/jm00130a019
44314857 161907 None 0 Rat Binding pKi = 7.6 7.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1047 29 9 10 3.6 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL414382 161907 None 0 Rat Binding pKi = 7.6 7.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1047 29 9 10 3.6 CCNC(=O)C1CCCN1C(=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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557600 89417 None 0 Rat Binding pKi = 7.6 7.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369813 89417 None 0 Rat Binding pKi = 7.6 7.6 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 957 26 10 10 1.4 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
44314845 161989 None 0 Rat Binding pKi = 8.5 8.5 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL415109 161989 None 0 Rat Binding pKi = 8.5 8.5 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1067 28 9 10 3.4 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369798 212149 None 0 Rat Binding pKi = 8.4 8.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)Cc1ccc2ccccc2c1 10.1021/jm00130a019
14557616 89410 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369799 89410 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 983 25 10 10 1.9 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
44314846 98325 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL274609 98325 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1117 28 9 10 4.6 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](COCc1ccccc1)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369788 212147 None 0 Rat Binding pKi = 8.3 8.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369814 212151 None 0 Rat Binding pKi = 8.3 8.3 12 2
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL None None None CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)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](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
14557590 89414 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369808 89414 None 0 Rat Binding pKi = 7.4 7.4 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 986 26 11 10 1.7 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC1CCCCC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)CCc1c[nH]c2ccccc12 10.1021/jm00130a019
14557620 89416 None 0 Rat Binding pKi = 7.3 7.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369810 89416 None 0 Rat Binding pKi = 7.3 7.3 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 955 25 10 10 1.5 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)/C=C/c1cccc2ccccc12 10.1021/jm00130a019
44314898 141942 None 0 Rat Binding pKi = 8.2 8.2 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL386525 141942 None 0 Rat Binding pKi = 8.2 8.2 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 1120 29 10 10 4.3 CCNC(=O)C1CCCN1C(=O)[C@H](CCCN=C(N)N)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](COCc1ccccc1)NC(=O)CCc1cccc2ccccc12 10.1021/jm00130a019
14557608 89405 None 0 Rat Binding pKi = 7.2 7.2 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 943 25 10 10 1.0 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369789 89405 None 0 Rat Binding pKi = 7.2 7.2 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 943 25 10 10 1.0 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
14557606 89401 None 0 Rat Binding pKi = 6.1 6.1 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 929 24 10 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369781 89401 None 0 Rat Binding pKi = 6.1 6.1 - 1
In vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards Luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 929 24 10 10 1.1 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)c1cccc2ccccc12 10.1021/jm00130a019
14557576 89409 None 0 Rat Binding pKi = 7.1 7.1 10 2
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 961 26 12 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
CHEMBL2369794 89409 None 0 Rat Binding pKi = 7.1 7.1 10 2
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 961 26 12 11 -0.3 CCNC(=O)[C@@H]1CCCN1C(=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](CO)NC(=O)[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00130a019
44350486 161875 None 0 Rat Binding pKi = 8.0 8.0 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1204 32 14 14 -1.3 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
CHEMBL414071 161875 None 0 Rat Binding pKi = 8.0 8.0 - 1
Negative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assayNegative logarithm of equilibrium dissociation constant in the rat pituitary luteinizing releasing hormone receptor binding assay
ChEMBL 1204 32 14 14 -1.3 CCNC(=O)[C@H]1CCCN1C(=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](CO)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1 10.1021/jm00099a017
14557614 89412 None 0 Rat Binding pKi = 8.0 8.0 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369800 89412 None 0 Rat Binding pKi = 8.0 8.0 - 1
In vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity for Luteinizing hormone releasing hormone receptor from rat pituitary cells, expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 977 25 10 10 1.2 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)Cc1cccc2ccccc12 10.1021/jm00130a019
3860 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
436 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
50225 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
50225.0 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
CHEMBL2110824 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
DB06719 744 None 0 Human Binding pKd = 8.1 8.1 -57 2
NoneNone
Drug Central None None None None None
1160 1917 None 0 Human Binding pKd = 10.9 10.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12727981
1160 1917 None 0 Human Binding pKd = 10.9 10.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1922095
11980076 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
36523 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
36523.0 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
638793 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
638793.0 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1981292 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
DB00644 210912 None 21 Rat Binding pKi = 8.1 8.1 - 1
NoneNone
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None