Ligand source activities (1 row/activity)



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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 AssayType

 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
10696930 36088 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL144397 36088 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9897637 118932 0 None - 1 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
CHEMBL342323 118932 0 None - 1 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
10791244 35797 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL144128 35797 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10720301 39984 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL147851 39984 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10531639 121272 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
CHEMBL357830 121272 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
9984109 38877 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL146720 38877 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
11800592 120985 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL356277 120985 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10008868 121125 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
CHEMBL357478 121125 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
11797158 40040 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147901 40040 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9832057 52315 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 10.1016/s0960-894x(98)00090-0
CHEMBL158941 52315 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 10.1016/s0960-894x(98)00090-0
10836606 165533 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL424128 165533 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10647387 40191 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
CHEMBL148022 40191 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
10837858 39806 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147677 39806 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10671315 203011 0 None -186 2 Human 5.0 pEC50 = 5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL63258 203011 0 None -186 2 Human 5.0 pEC50 = 5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
40 1547 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
77993 1547 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
995 1547 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
CHEMBL1510 1547 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
DB00216 1547 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
18975369 101029 0 None -120 2 Human 6.9 pEC50 = 6.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL294547 101029 0 None -120 2 Human 6.9 pEC50 = 6.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
4806 4008 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
11796806 102717 0 None -169 2 Human 5.9 pEC50 = 5.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL304857 102717 0 None -169 2 Human 5.9 pEC50 = 5.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
2869 4152 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60 4152 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60857 4152 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
CHEMBL1185 4152 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
DB00315 4152 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
44592371 178994 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL470849 178994 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
10766570 203380 0 None -501 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1 10.1021/jm981133m
CHEMBL65321 203380 0 None -501 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1 10.1021/jm981133m
10600213 203109 0 None -575 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
CHEMBL64004 203109 0 None -575 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
145975946 163920 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 163920 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
24762221 19319 0 None -39 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290596 19319 0 None -39 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
11797999 40525 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL148314 40525 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10385855 14425 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL120055 14425 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL321818 14425 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
10791125 18961 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1 10.1021/jm9703552
CHEMBL128699 18961 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1 10.1021/jm9703552
10649124 19470 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL129813 19470 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
44592333 178838 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469376 178838 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
1220 187 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
31 187 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
7 187 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
CHEMBL56 187 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
10838063 78776 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL2112660 78776 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
145964150 164306 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 164306 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
10719687 202999 0 None -257 2 Human 6.5 pEC50 = 6.5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL63167 202999 0 None -257 2 Human 6.5 pEC50 = 6.5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
11797998 35692 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL144030 35692 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10601619 116836 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
CHEMBL338015 116836 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
52946290 19102 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 446 4 0 5 4.4 Cc1ccc2c(N3CCN(CCc4c(Cl)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289164 19102 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 446 4 0 5 4.4 Cc1ccc2c(N3CCN(CCc4c(Cl)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
2543 3707 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
5358 3707 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
54 3707 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
CHEMBL128 3707 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
DB00669 3707 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
24804774 19320 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 428 4 0 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290597 19320 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 428 4 0 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10809674 119196 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL343196 119196 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
5 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5202 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
CHEMBL39 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
DB08839 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
5202 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
CHEMBL39 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
DB08839 139 72 None -19 26 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
114 2254 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
6426760 2254 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
CHEMBL292779 2254 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
10503687 203077 0 None -50 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63799 203077 0 None -50 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10341917 168049 0 None -97 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
CHEMBL432332 168049 0 None -97 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
10076876 101712 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
CHEMBL29951 101712 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
52943811 19082 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289047 19082 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10551328 203721 0 None -97 2 Human 6.3 pEC50 = 6.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL67684 203721 0 None -97 2 Human 6.3 pEC50 = 6.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
10837853 168158 0 None -309 2 Human 5.3 pEC50 = 5.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL433108 168158 0 None -309 2 Human 5.3 pEC50 = 5.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
11 1187 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
124007 1187 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL304008 1187 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
44592208 179179 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL472289 179179 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
52948697 19083 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289048 19083 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592332 178837 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 430 5 0 5 3.7 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469375 178837 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 430 5 0 5 3.7 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
9844873 101058 0 None -48 2 Human 7.2 pEC50 = 7.2 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL294732 101058 0 None -48 2 Human 7.2 pEC50 = 7.2 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
2543 3707 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
5358 3707 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
54 3707 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
CHEMBL128 3707 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
DB00669 3707 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
10575553 203039 0 None -245 2 Human 6.1 pEC50 = 6.1 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63432 203039 0 None -245 2 Human 6.1 pEC50 = 6.1 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10621021 203384 0 None -66 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
CHEMBL65367 203384 0 None -66 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
9844873 101058 0 None -48 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.7b01788
CHEMBL294732 101058 0 None -48 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.7b01788
18975369 101029 0 None -120 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
CHEMBL294547 101029 0 None -120 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
145975946 163920 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 163920 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
145964150 164306 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 164306 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
146395245 189057 15 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 400 3 2 3 2.8 CC(=O)N1CCN([C@H]2CCC[C@@H](NC(=O)c3cc4c(F)ccc(C)c4[nH]3)C2)CC1 10.1021/acsmedchemlett.2c00167
CHEMBL5095235 189057 15 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 400 3 2 3 2.8 CC(=O)N1CCN([C@H]2CCC[C@@H](NC(=O)c3cc4c(F)ccc(C)c4[nH]3)C2)CC1 10.1021/acsmedchemlett.2c00167
11568826 132798 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 132798 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11662592 72344 0 None 15 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198463 72344 0 None 15 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11655728 16644 8 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16644 8 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
10447834 1933 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 1933 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 1933 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
44373817 11718 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1181270 11718 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL161046 11718 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
44373789 11721 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1181275 11721 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL161368 11721 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
10403687 2511 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 2511 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 2511 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
44373791 12233 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1184450 12233 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL349405 12233 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
11797998 35692 0 None - 1 Human 10.0 pKi = 10 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL144030 35692 0 None - 1 Human 10.0 pKi = 10 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
44405730 168919 0 None - 0 Human 10.0 pKi = 10 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL438619 168919 0 None - 0 Human 10.0 pKi = 10 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10720301 39984 0 None - 1 Human 10.0 pKi = 10.0 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL147851 39984 0 None - 1 Human 10.0 pKi = 10.0 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10008868 121125 0 None - 1 Human 9.9 pKi = 9.9 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
CHEMBL357478 121125 0 None - 1 Human 9.9 pKi = 9.9 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
11797158 40040 0 None - 1 Human 9.8 pKi = 9.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147901 40040 0 None - 1 Human 9.8 pKi = 9.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10837858 39806 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147677 39806 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10531639 121272 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
CHEMBL357830 121272 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
10791244 35797 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL144128 35797 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
11800592 120985 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL356277 120985 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10696930 36088 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL144397 36088 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9868889 72629 0 None - 0 Human 9.5 pKi = 9.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL199443 72629 0 None - 0 Human 9.5 pKi = 9.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10647387 40191 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
CHEMBL148022 40191 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
9984109 38877 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL146720 38877 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
9897637 118932 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
CHEMBL342323 118932 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
44405669 71971 0 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 465 4 0 8 3.5 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccsc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197344 71971 0 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 465 4 0 8 3.5 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccsc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10836606 165533 0 None - 1 Human 9.3 pKi = 9.3 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL424128 165533 0 None - 1 Human 9.3 pKi = 9.3 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405725 71835 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1c(Cl)cccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196914 71835 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1c(Cl)cccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464649 72449 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 459 4 0 7 3.4 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198836 72449 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 459 4 0 7 3.4 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405666 72873 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 451 4 0 8 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6c5OCC6)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL200315 72873 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 451 4 0 8 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6c5OCC6)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
9933975 133587 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5nccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL371221 133587 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5nccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900954 16652 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242081 16652 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900776 16639 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241824 16639 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900956 16654 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242167 16654 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
52942551 19300 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 400 4 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290486 19300 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 400 4 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
46900459 16638 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241738 16638 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
52947615 19136 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289394 19136 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
52947414 19301 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 0 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290487 19301 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 0 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
24804775 19343 0 None - 2 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290716 19343 0 None - 2 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44405702 72580 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cnccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL199269 72580 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cnccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900455 16633 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241641 16633 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
46900457 16634 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241642 16634 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900612 16636 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241736 16636 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46899639 16669 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242533 16669 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
11720815 16684 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 538 5 0 8 3.5 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCOCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242717 16684 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 538 5 0 8 3.5 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCOCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44138098 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL513715 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
44138098 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL513715 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44138098 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513715 189472 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44405573 71857 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 485 5 0 7 3.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5-c5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197007 71857 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 485 5 0 7 3.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5-c5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405574 72435 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 501 6 0 8 4.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Oc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198792 72435 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 501 6 0 8 4.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Oc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405575 72494 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 7 0 8 3.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198999 72494 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 7 0 8 3.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900610 16632 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 497 6 0 8 4.2 CCOC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241640 16632 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 497 6 0 8 4.2 CCOC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
11712756 16643 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241912 16643 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
22464842 71817 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 434 4 0 8 2.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5C#N)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL196862 71817 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 434 4 0 8 2.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5C#N)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
9872238 72514 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 439 5 0 8 2.3 COc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL199049 72514 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 439 5 0 8 2.3 COc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
46900451 16626 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241547 16626 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900778 16640 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 450 4 0 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C#N)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241825 16640 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 450 4 0 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C#N)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
11655728 16644 8 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16644 8 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899637 16660 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242345 16660 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899638 16664 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242436 16664 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899640 16676 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 5 0 7 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242623 16676 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 5 0 7 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900150 16696 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242904 16696 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
44138104 178833 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL469345 178833 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
11797999 40525 0 None - 1 Human 8.8 pKi = 8.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL148314 40525 0 None - 1 Human 8.8 pKi = 8.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405701 71931 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ncccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197240 71931 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ncccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22464720 72401 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 443 4 0 7 2.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Cl)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198696 72401 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 443 4 0 7 2.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Cl)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900453 16627 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241548 16627 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
46900958 16659 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242257 16659 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
9979309 192982 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL522257 192982 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
52942644 19342 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 398 4 1 4 3.7 Cc1ccc2c(N3CCN(CCc4cccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290715 19342 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 398 4 1 4 3.7 Cc1ccc2c(N3CCN(CCc4cccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592297 189490 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513875 189490 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
9979309 192982 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL522257 192982 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
14519851 116748 39 None - 0 Human 7.0 pKi = 7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 187 3 1 2 2.2 NCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL337539 116748 39 None - 0 Human 7.0 pKi = 7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 187 3 1 2 2.2 NCCOc1cccc2ccccc12 10.1021/jm970507t
2261792 116447 6 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 231 6 2 3 1.8 OCCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL336092 116447 6 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 231 6 2 3 1.8 OCCNCCOc1cccc2ccccc12 10.1021/jm970507t
44405655 71878 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 453 5 0 8 2.6 COc1ccc(C)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197064 71878 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 453 5 0 8 2.6 COc1ccc(C)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10584924 30410 0 None - 0 Human 6.0 pKi = 6.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 218 5 2 2 2.5 CC(C)NCCOc1cccc2[nH]ccc12 10.1021/jm970507t
CHEMBL139230 30410 0 None - 0 Human 6.0 pKi = 6.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 218 5 2 2 2.5 CC(C)NCCOc1cccc2[nH]ccc12 10.1021/jm970507t
22464806 71844 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 6 0 8 3.9 COc1ccc(-c2ccccc2)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196961 71844 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 6 0 8 3.9 COc1ccc(-c2ccccc2)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10775772 30107 2 None - 0 Human 6.9 pKi = 6.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 1 2 3.2 CC(C)NCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138963 30107 2 None - 0 Human 6.9 pKi = 6.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 1 2 3.2 CC(C)NCCOc1cccc2ccccc12 10.1021/jm970507t
10588458 27611 0 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 275 8 0 2 4.5 CCCN(C)CCCOc1ccccc1C1CCCC1 10.1021/jm970507t
CHEMBL136962 27611 0 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 275 8 0 2 4.5 CCCN(C)CCCOc1ccccc1C1CCCC1 10.1021/jm970507t
6422277 30036 5 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138907 30036 5 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm970507t
44592295 179009 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL471047 179009 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592252 189194 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 466 6 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC(F)F)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL511279 189194 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 466 6 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC(F)F)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592335 178925 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 462 5 0 5 4.2 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL470217 178925 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 462 5 0 5 4.2 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
10518850 35193 0 None - 0 Human 7.8 pKi = 7.8 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143512 35193 0 None - 0 Human 7.8 pKi = 7.8 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10809674 119196 0 None - 1 Human 8.6 pKi = 8.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL343196 119196 0 None - 1 Human 8.6 pKi = 8.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405586 71842 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 467 6 0 8 3.1 CC(C)Oc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196958 71842 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 467 6 0 8 3.1 CC(C)Oc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
11568826 132798 0 None 9 2 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 132798 0 None 9 2 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900606 16625 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241546 16625 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
46900614 16637 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 6 0 8 4.4 CO/N=C(\C)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241737 16637 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 6 0 8 4.4 CO/N=C(\C)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900782 16648 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241998 16648 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44592296 178836 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469374 178836 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
44592294 189263 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL511815 189263 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
10585509 29753 2 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 6 1 2 3.2 CCCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138683 29753 2 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 6 1 2 3.2 CCCNCCOc1cccc2ccccc12 10.1021/jm970507t
2543 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
5358 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
54 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
CHEMBL128 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
DB00669 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
2543 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
5358 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
54 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
CHEMBL128 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
DB00669 3707 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
9909089 186968 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL490417 186968 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
9909089 186968 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL490417 186968 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
23274477 29121 1 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138136 29121 1 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm970507t
2199302 30099 25 None - 0 Human 7.6 pKi = 7.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.4 CNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138958 30099 25 None - 0 Human 7.6 pKi = 7.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.4 CNCCOc1cccc2ccccc12 10.1021/jm970507t
1328538 31584 8 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 291 6 0 2 4.4 CN(CCOc1cccc2ccccc12)Cc1ccccc1 10.1021/jm970507t
CHEMBL140416 31584 8 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 291 6 0 2 4.4 CN(CCOc1cccc2ccccc12)Cc1ccccc1 10.1021/jm970507t
2176 3127 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
4828 3127 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
91 3127 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
CHEMBL500 3127 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
DB00960 3127 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
14519863 115201 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL334465 115201 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm970507t
9802530 35386 1 None -11 2 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143767 35386 1 None -11 2 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
14566707 119091 42 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.6 NCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL342704 119091 42 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.6 NCCCOc1cccc2ccccc12 10.1021/jm970507t
10365683 113078 0 None - 0 Human 8.5 pKi = 8.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 7 3 5 2.4 CC(=O)Nc1ccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)cc1 10.1021/jm960552l
CHEMBL331240 113078 0 None - 0 Human 8.5 pKi = 8.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 7 3 5 2.4 CC(=O)Nc1ccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)cc1 10.1021/jm960552l
44405677 71845 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1cc(Cl)ccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196962 71845 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1cc(Cl)ccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464831 71883 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 423 4 0 7 2.6 Cc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197078 71883 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 423 4 0 7 2.6 Cc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464606 72007 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1c(Cl)cc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197445 72007 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1c(Cl)cc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
44138104 178833 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
CHEMBL469345 178833 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
44138104 178833 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469345 178833 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592209 179180 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
CHEMBL472290 179180 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
52943861 19101 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 430 4 0 5 3.9 Cc1ccc2c(N3CCN(CCc4c(F)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289163 19101 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 430 4 0 5 3.9 Cc1ccc2c(N3CCN(CCc4c(F)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592207 189363 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL512724 189363 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
10654938 78818 11 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 179 4 1 2 1.9 CNCCOc1cccc(C)c1C 10.1021/jm970507t
CHEMBL2112766 78818 11 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 179 4 1 2 1.9 CNCCOc1cccc(C)c1C 10.1021/jm970507t
52947622 19153 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289510 19153 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
22464564 71832 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 461 4 0 9 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5ncnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL196907 71832 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 461 4 0 9 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5ncnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22067856 29540 52 None - 0 Human 5.5 pKi = 5.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm970507t
CHEMBL138509 29540 52 None - 0 Human 5.5 pKi = 5.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm970507t
22464634 73023 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccc6ccccc6n5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL200951 73023 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccc6ccccc6n5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10618751 35190 0 None -25 2 Human 7.4 pKi = 7.4 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143510 35190 0 None -25 2 Human 7.4 pKi = 7.4 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
52944840 18978 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1287827 18978 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2010.09.085
44405726 71965 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1cc(Cl)c(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197338 71965 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1cc(Cl)c(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
2303 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
4946 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
564 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
63 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
91536 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
CHEMBL27 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
CHEMBL452861 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
DB00571 3187 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
44405665 73021 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.3 COc1ccc(C(F)(F)F)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL200949 73021 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.3 COc1ccc(C(F)(F)F)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10635169 31582 0 None - 0 Human 6.4 pKi = 6.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 261 7 0 2 4.1 CCCN(C)CCOc1ccccc1C1CCCC1 10.1021/jm970507t
CHEMBL140415 31582 0 None - 0 Human 6.4 pKi = 6.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 261 7 0 2 4.1 CCCN(C)CCOc1ccccc1C1CCCC1 10.1021/jm970507t
13520547 27004 1 None - 0 Human 6.3 pKi = 6.3 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL136470 27004 1 None - 0 Human 6.3 pKi = 6.3 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm970507t
44592249 178851 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C(C)C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469567 178851 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C(C)C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592250 178852 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469568 178852 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
22464804 73022 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 489 5 0 8 3.4 COc1ccc2ccccc2c1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL200950 73022 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 489 5 0 8 3.4 COc1ccc2ccccc2c1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
44405587 133565 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 495 6 0 8 3.7 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCC(C)(C)C)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL371094 133565 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 495 6 0 8 3.7 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCC(C)(C)C)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22464614 71858 0 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 469 6 0 9 2.3 COc1ccc(OC)c(N2CCN(CCn3cnc4sc5c(c4c3=O)CCN(C)C5)CC2)c1 10.1016/j.bmcl.2005.04.077
CHEMBL197011 71858 0 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 469 6 0 9 2.3 COc1ccc(OC)c(N2CCN(CCn3cnc4sc5c(c4c3=O)CCN(C)C5)CC2)c1 10.1016/j.bmcl.2005.04.077
37732 26823 73 None - 0 Human 5.2 pKi = 5.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 151 4 1 2 1.3 CNCCOc1ccccc1 10.1021/jm970507t
CHEMBL136311 26823 73 None - 0 Human 5.2 pKi = 5.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 151 4 1 2 1.3 CNCCOc1ccccc1 10.1021/jm970507t
44592251 178907 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 456 6 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469995 178907 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 456 6 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
5 139 72 None -19 26 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
5202 139 72 None -19 26 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
CHEMBL39 139 72 None -19 26 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
DB08839 139 72 None -19 26 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
10560632 26732 1 None - 0 Human 7.2 pKi = 7.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 5 1 2 2.8 CCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL136236 26732 1 None - 0 Human 7.2 pKi = 7.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 5 1 2 2.8 CCNCCOc1cccc2ccccc12 10.1021/jm970507t
46900608 16631 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 427 4 0 8 2.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnnn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241639 16631 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 427 4 0 8 2.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnnn4-5)CC3)cccc2n1 10.1021/jm100482n
22002244 72343 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1ccc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL198462 72343 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1ccc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
14519865 31587 1 None - 0 Human 6.1 pKi = 6.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL140417 31587 1 None - 0 Human 6.1 pKi = 6.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
10263828 30873 17 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 1 2 3.6 CC(C)NCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL139737 30873 17 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 1 2 3.6 CC(C)NCCCOc1cccc2ccccc12 10.1021/jm970507t
44592334 178857 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 5 0 5 3.8 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469589 178857 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 5 0 5 3.8 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
10691904 35620 0 None -3 2 Human 7.1 pKi = 7.1 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143967 35620 0 None -3 2 Human 7.1 pKi = 7.1 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
11662592 72344 0 None 15 2 Human 8.0 pKi = 8.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198463 72344 0 None 15 2 Human 8.0 pKi = 8.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
3604129 30264 5 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL139103 30264 5 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
2105 3054 37 None -1 25 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 37 None -1 25 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 37 None -1 25 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 37 None -1 25 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 37 None -1 25 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
4223 3992 94 None -707 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 3992 94 None -707 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 3992 94 None -707 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 3992 94 None -707 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 3992 94 None -707 16 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
1220 187 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
31 187 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
7 187 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
CHEMBL56 187 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
137 138 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048565 138 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048566 138 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
1524 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
1524 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
197 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
197 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
3822 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
3822 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
88 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
88 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
CHEMBL51 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
CHEMBL51 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
DB12465 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
DB12465 2181 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
5074 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
5074 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
97 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
97 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
CHEMBL267777 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
CHEMBL267777 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
DB12693 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
DB12693 3332 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
16 2253 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
9847194 2253 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
CHEMBL313714 2253 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
46 2905 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
71351 2905 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
CHEMBL2104619 2905 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
DB06229 2905 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
110 1174 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
132552 1174 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
CHEMBL159332 1174 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
113 1852 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
128018 1852 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
CHEMBL119264 1852 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546


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Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
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ity		 Common
name		 GPCRdb
ID		 #Vendors

 Reference
ligand		 Fold
selectivity		 # Tested
GPCRs		 Species

 p-value
(-log)		 Activity
Type		 Activity
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Value		 Assay
Type		 Assay
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weight		 Rot
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 DOI
19066203 12089 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1183904 12089 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL323986 12089 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
19066163 11386 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL111302 11386 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1180017 11386 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
5 139 72 None -13 54 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
5202 139 72 None -13 54 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL39 139 72 None -13 54 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
DB08839 139 72 None -13 54 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL5078078 214535 7 None - 0 Human 5.6 pEC50 = 5.6 Binding
Safety47 Scan (DiscoverX - Eurofins)Safety47 Scan (DiscoverX - Eurofins)
ChEMBL None None None CC(C)(O)c1ccc(N2Cc3c(ccnc3-c3ccc(F)cc3OCC(F)(F)F)C2=O)cc1 10.6019/CHEMBL5303768
5 139 72 None -11 54 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
5202 139 72 None -11 54 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL39 139 72 None -11 54 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
DB08839 139 72 None -11 54 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
137634921 156250 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 586 3 2 9 4.5 O=C1CCc2cc3cc(c2N1Cc1ccccc1)OC/C=C/CO[C@H]1C[C@@H](CO)N(C1)c1cc(n2ncc(Cl)c2n1)N3 10.1021/acs.jmedchem.7b00359
CHEMBL4064865 156250 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 586 3 2 9 4.5 O=C1CCc2cc3cc(c2N1Cc1ccccc1)OC/C=C/CO[C@H]1C[C@@H](CO)N(C1)c1cc(n2ncc(Cl)c2n1)N3 10.1021/acs.jmedchem.7b00359
11539632 70561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 70561 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
1043 1582 14 None 4 28 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 1582 14 None 4 28 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 1582 14 None 4 28 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 1582 14 None 4 28 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 1582 14 None 4 28 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
9952249 52672 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 388 6 1 7 2.3 c1cnc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
CHEMBL159396 52672 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 388 6 1 7 2.3 c1cnc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
9846928 39679 15 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 457 6 3 5 4.0 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=N)N)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL147503 39679 15 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 457 6 3 5 4.0 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=N)N)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
2543 3707 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
5358 3707 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
54 3707 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
CHEMBL128 3707 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
DB00669 3707 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
11333554 96661 22 None - 1 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26379 96661 22 None - 1 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
10531 1420 21 None -5 23 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 1420 21 None -5 23 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 1420 21 None -5 23 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 1420 21 None -5 23 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 1420 21 None -5 23 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
10323598 38899 21 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL146735 38899 21 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
15646678 96659 27 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 214 1 3 2 2.3 Oc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26378 96659 27 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 214 1 3 2 2.3 Oc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
9881526 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
CHEMBL296161 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
9881526 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
CHEMBL296161 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
10718709 39284 19 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 458 6 2 5 3.8 COc1ccc(NC(=O)c2ccc(-c3ccc(C(N)=O)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL147071 39284 19 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 458 6 2 5 3.8 COc1ccc(NC(=O)c2ccc(-c3ccc(C(N)=O)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
9881526 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9704558
CHEMBL296161 101248 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9704558
107780 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
14 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
CHEMBL15928 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
107780 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
14 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
CHEMBL15928 1844 54 None -4 17 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
11344959 97293 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 216 1 2 1 2.7 Fc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26906 97293 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 216 1 2 1 2.7 Fc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
2543 3707 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
5358 3707 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
54 3707 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
CHEMBL128 3707 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
DB00669 3707 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
1588 2325 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 2325 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 2325 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 2325 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 2325 27 None -58 44 Rat 8.0 pIC50 = 8 Binding