Ligand source activities (1 row/activity)





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

10696930 36088 None 0 Human Functional pEC50 = 10.1 10.1 - 1
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 None 0 Human Functional pEC50 = 10.1 10.1 - 1
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 None 0 Human Functional pEC50 = 10 10.0 - 1
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 None 0 Human Functional pEC50 = 10 10.0 - 1
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 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 None 0 Human Functional pEC50 = 9.7 9.7 - 1
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 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 None 0 Human Functional pEC50 = 9.6 9.6 - 1
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 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 None 0 Human Functional pEC50 = 9.5 9.5 - 1
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 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 None 0 Human Functional pEC50 = 9.4 9.4 - 1
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 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 None 0 Human Functional pEC50 = 9.2 9.2 - 1
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 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 None 0 Human Functional pEC50 = 9.1 9.1 - 1
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 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 None 0 Human Functional pEC50 = 8.8 8.8 - 1
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 None 0 Human Functional pEC50 = 5 5.0 -186 2
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 None 0 Human Functional pEC50 = 5 5.0 -186 2
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 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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
77993.0 1547 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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 None 58 Human Functional pEC50 = 7.9 7.9 1 8
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 None 0 Human Functional pEC50 = 6.9 6.9 -120 2
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 None 0 Human Functional pEC50 = 6.9 6.9 -120 2
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 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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
71768094.0 4008 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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
9966051.0 4008 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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 None 88 Human Functional pEC50 = 6.9 6.9 1 3
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 None 0 Human Functional pEC50 = 5.9 5.9 -169 2
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 None 0 Human Functional pEC50 = 5.9 5.9 -169 2
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 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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
60857.0 4152 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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 None 89 Human Functional pEC50 = 7.8 7.8 -3 5
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 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 None 0 Human Functional pEC50 = 7.8 7.8 - 1
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 None 0 Human Functional pEC50 = 5.8 5.8 -501 2
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 None 0 Human Functional pEC50 = 5.8 5.8 -501 2
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 None 0 Human Functional pEC50 = 5.8 5.8 -575 2
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 None 0 Human Functional pEC50 = 5.8 5.8 -575 2
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 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 None 0 Human Functional pEC50 = 6.8 6.8 - 1
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 None 0 Human Functional pEC50 = 6.7 6.7 -39 2
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 None 0 Human Functional pEC50 = 6.7 6.7 -39 2
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 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 None 0 Human Functional pEC50 = 8.7 8.7 - 1
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 None 0 Human Functional pEC50 = 8.7 8.7 -3 3
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 None 0 Human Functional pEC50 = 8.7 8.7 -3 3
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 None 0 Human Functional pEC50 = 8.7 8.7 -3 3
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 55 Human Functional pEC50 = 6.6 6.6 -109 9
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 None 55 Human Functional pEC50 = 6.6 6.6 -109 9
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 None 55 Human Functional pEC50 = 6.6 6.6 -109 9
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 None 55 Human Functional pEC50 = 6.6 6.6 -109 9
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.6 7.6 - 1
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 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 None 0 Human Functional pEC50 = 6.5 6.5 -257 2
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 None 0 Human Functional pEC50 = 6.5 6.5 -257 2
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 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 None 0 Human Functional pEC50 = 8.5 8.5 - 1
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 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 None 0 Human Functional pEC50 = 7.5 7.5 - 1
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 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 None 0 Human Functional pEC50 = 6.5 6.5 - 1
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 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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
5358.0 3707 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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 None 68 Human Functional pEC50 = 7.4 7.4 2 14
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 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 None 0 Human Functional pEC50 = 6.4 6.4 - 1
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 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 None 0 Human Functional pEC50 = 8.4 8.4 - 1
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 72 Human Functional pEC50 = 8.3 8.3 -19 26
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 None 14 Human Functional pEC50 = 6.4 6.4 -169 6
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 None 14 Human Functional pEC50 = 6.4 6.4 -169 6
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 None 14 Human Functional pEC50 = 6.4 6.4 -169 6
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 None 0 Human Functional pEC50 = 6.4 6.4 -50 2
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 None 0 Human Functional pEC50 = 6.4 6.4 -50 2
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 None 0 Human Functional pEC50 = 6.4 6.4 -97 2
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 None 0 Human Functional pEC50 = 6.4 6.4 -97 2
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 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 None 0 Human Functional pEC50 = 7.3 7.3 - 1
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 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 None 0 Human Functional pEC50 = 6.3 6.3 - 1
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 None 0 Human Functional pEC50 = 6.3 6.3 -97 2
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 None 0 Human Functional pEC50 = 6.3 6.3 -97 2
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 None 0 Human Functional pEC50 = 5.3 5.3 -309 2
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 None 0 Human Functional pEC50 = 5.3 5.3 -309 2
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 None 19 Rat Functional pEC50 = 7.3 7.3 75 4
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 None 19 Rat Functional pEC50 = 7.3 7.3 75 4
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 None 19 Rat Functional pEC50 = 7.3 7.3 75 4
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 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 None 0 Human Functional pEC50 = 8.2 8.2 - 1
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 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 None 0 Human Functional pEC50 = 7.2 7.2 - 1
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 None 0 Human Functional pEC50 = 7.2 7.2 -48 2
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 None 0 Human Functional pEC50 = 7.2 7.2 -48 2
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 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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
5358.0 3707 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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 None 68 Human Functional pEC50 = 7.1 7.1 2 14
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 None 0 Human Functional pEC50 = 6.1 6.1 -245 2
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 None 0 Human Functional pEC50 = 6.1 6.1 -245 2
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 None 0 Human Functional pIC50 = 8.0 8.0 -66 2
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 None 0 Human Functional pIC50 = 8.0 8.0 -66 2
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 None 0 Human Functional pIC50 = 7.8 7.8 -48 2
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 None 0 Human Functional pIC50 = 7.8 7.8 -48 2
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 None 0 Human Functional pIC50 = 7.7 7.7 -120 2
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 None 0 Human Functional pIC50 = 7.7 7.7 -120 2
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 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 None 0 Human Functional pIC50 = 5.7 5.7 - 1
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 None 15 Human Functional pIC50 = 5.5 5.5 4 2
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 None 15 Human Functional pIC50 = 5.5 5.5 4 2
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 None 0 Human Functional pIC50 = 7.5 7.5 9 2
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 None 0 Human Functional pIC50 = 7.5 7.5 9 2
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 None 0 Human Functional pIC50 = 7.1 7.1 15 2
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 None 0 Human Functional pIC50 = 7.1 7.1 15 2
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 None 8 Human Functional pKd = 8.9 8.9 - 0
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 None 8 Human Functional pKd = 8.9 8.9 - 0
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 None 4 Human Functional pKd = 4.9 4.9 - 3
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 None 4 Human Functional pKd = 4.9 4.9 - 3
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 None 4 Human Functional pKd = 4.9 4.9 - 3
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 None 0 Human Functional pKd = 5.7 5.7 - 0
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 None 0 Human Functional pKd = 5.7 5.7 - 0
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 None 0 Human Functional pKd = 5.7 5.7 - 0
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 None 0 Human Functional pKd = 6.7 6.7 - 0
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 None 0 Human Functional pKd = 6.7 6.7 - 0
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 None 0 Human Functional pKd = 6.7 6.7 - 0
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 None 3 Human Functional pKd = 5.1 5.1 - 2
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 None 3 Human Functional pKd = 5.1 5.1 - 2
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 None 3 Human Functional pKd = 5.1 5.1 - 2
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 None 0 Human Functional pKd = 6.1 6.1 - 0
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 None 0 Human Functional pKd = 6.1 6.1 - 0
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 None 0 Human Functional pKd = 6.1 6.1 - 0
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 None 0 Human Functional pKi = 10 10.0 - 1
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 None 0 Human Functional pKi = 10 10.0 - 1
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 None 0 Human Functional pKi = 10 10.0 - 0
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 None 0 Human Functional pKi = 10 10.0 - 0
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 None 0 Human Functional pKi = 10.0 10.0 - 1
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 None 0 Human Functional pKi = 10.0 10.0 - 1
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 None 0 Human Functional pKi = 9.9 9.9 - 1
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 None 0 Human Functional pKi = 9.9 9.9 - 1
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 None 0 Human Functional pKi = 9.8 9.8 - 1
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 None 0 Human Functional pKi = 9.8 9.8 - 1
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 None 0 Human Functional pKi = 9.7 9.7 - 1
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 None 0 Human Functional pKi = 9.7 9.7 - 1
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 None 0 Human Functional pKi = 9.7 9.7 - 1
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 None 0 Human Functional pKi = 9.7 9.7 - 1
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 None 0 Human Functional pKi = 9.6 9.6 - 1
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 None 0 Human Functional pKi = 9.6 9.6 - 1
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 None 0 Human Functional pKi = 9.6 9.6 - 1
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 None 0 Human Functional pKi = 9.6 9.6 - 1
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 None 0 Human Functional pKi = 9.5 9.5 - 1
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 None 0 Human Functional pKi = 9.5 9.5 - 1
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 None 0 Human Functional pKi = 9.5 9.5 - 0
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 None 0 Human Functional pKi = 9.5 9.5 - 0
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 None 0 Human Functional pKi = 9.5 9.5 - 1
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 None 0 Human Functional pKi = 9.5 9.5 - 1
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 None 0 Human Functional pKi = 9.4 9.4 - 1
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 None 0 Human Functional pKi = 9.4 9.4 - 1
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 None 0 Human Functional pKi = 9.4 9.4 - 1
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 None 0 Human Functional pKi = 9.4 9.4 - 1
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 None 0 Human Functional pKi = 9.4 9.4 - 0
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 None 0 Human Functional pKi = 9.4 9.4 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 1
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 None 0 Human Functional pKi = 9.3 9.3 - 1
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.3 9.3 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.2 9.2 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 2
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 None 0 Human Functional pKi = 9.1 9.1 - 2
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9.1 9.1 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9 9.0 - 0
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 None 0 Human Functional pKi = 9.0 9.0 - 0
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 None 0 Human Functional pKi = 9.0 9.0 - 0
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 None 0 Human Functional pKi = 9.0 9.0 - 0
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 None 0 Human Functional pKi = 9.0 9.0 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.9 8.9 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 8 Human Functional pKi = 8.8 8.8 - 0
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 None 8 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 1
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 None 0 Human Functional pKi = 8.8 8.8 - 1
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.8 8.8 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 0 Human Functional pKi = 8.7 8.7 - 0
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 None 39 Human Functional pKi = 7 7.0 - 0
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 None 39 Human Functional pKi = 7 7.0 - 0
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 None 6 Human Functional pKi = 7.0 7.0 - 0
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 None 6 Human Functional pKi = 7.0 7.0 - 0
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 None 0 Human Functional pKi = 7.9 7.9 - 0
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 None 0 Human Functional pKi = 7.9 7.9 - 0
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 None 0 Human Functional pKi = 6.0 6.0 - 0
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 None 0 Human Functional pKi = 6.0 6.0 - 0
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 None 0 Human Functional pKi = 6.9 6.9 - 0
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 None 0 Human Functional pKi = 6.9 6.9 - 0
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 None 2 Human Functional pKi = 6.9 6.9 - 0
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 None 2 Human Functional pKi = 6.9 6.9 - 0
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 None 0 Human Functional pKi = 5.9 5.9 - 0
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 None 0 Human Functional pKi = 5.9 5.9 - 0
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 None 5 Human Functional pKi = 5.9 5.9 - 0
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 None 5 Human Functional pKi = 5.9 5.9 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 6.8 6.8 - 0
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 None 0 Human Functional pKi = 6.8 6.8 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 7.8 7.8 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 1
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 None 0 Human Functional pKi = 8.6 8.6 - 1
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 9 2
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 None 0 Human Functional pKi = 8.6 8.6 9 2
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 0 Human Functional pKi = 8.6 8.6 - 0
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 None 2 Human Functional pKi = 6.7 6.7 - 0
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 None 2 Human Functional pKi = 6.7 6.7 - 0
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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
5358.0 3707 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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
5358.0 3707 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 68 Human Functional pKi = 7.6 7.6 2 14
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 None 0 Human Functional pKi = 6.6 6.6 - 1
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 None 0 Human Functional pKi = 6.6 6.6 - 1
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 None 0 Human Functional pKi = 6.6 6.6 - 1
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 None 0 Human Functional pKi = 6.6 6.6 - 1
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 None 1 Human Functional pKi = 6.6 6.6 - 0
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 None 1 Human Functional pKi = 6.6 6.6 - 0
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 None 25 Human Functional pKi = 7.6 7.6 - 0
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 None 25 Human Functional pKi = 7.6 7.6 - 0
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 None 8 Human Functional pKi = 6.6 6.6 - 0
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 None 8 Human Functional pKi = 6.6 6.6 - 0
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 None 68 Human Functional pKi = 5.6 5.6 - 8
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 None 68 Human Functional pKi = 5.6 5.6 - 8
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
4828.0 3127 None 68 Human Functional pKi = 5.6 5.6 - 8
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 None 68 Human Functional pKi = 5.6 5.6 - 8
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 None 68 Human Functional pKi = 5.6 5.6 - 8
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 None 68 Human Functional pKi = 5.6 5.6 - 8
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 None 1 Human Functional pKi = 5.6 5.6 - 0
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 None 1 Human Functional pKi = 5.6 5.6 - 0
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 None 1 Human Functional pKi = 7.6 7.6 -11 2
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 None 1 Human Functional pKi = 7.6 7.6 -11 2
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 None 42 Human Functional pKi = 6.5 6.5 - 0
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 None 42 Human Functional pKi = 6.5 6.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.5 8.5 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 8.4 8.4 - 0
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 None 0 Human Functional pKi = 7.5 7.5 - 0
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 None 0 Human Functional pKi = 7.5 7.5 - 0
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 None 0 Human Functional pKi = 7.5 7.5 - 0
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 None 0 Human Functional pKi = 7.5 7.5 - 0
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 None 11 Human Functional pKi = 6.5 6.5 - 0
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 None 11 Human Functional pKi = 6.5 6.5 - 0
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 None 0 Human Functional pKi = 6.5 6.5 - 0
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 None 0 Human Functional pKi = 6.5 6.5 - 0
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 None 0 Human Functional pKi = 6.5 6.5 - 0
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 None 0 Human Functional pKi = 6.5 6.5 - 0
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 None 52 Human Functional pKi = 5.5 5.5 - 0
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 None 52 Human Functional pKi = 5.5 5.5 - 0
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 None 0 Human Functional pKi = 7.4 7.4 - 0
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 None 0 Human Functional pKi = 7.4 7.4 - 0
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 None 0 Human Functional pKi = 7.4 7.4 -25 2
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 None 0 Human Functional pKi = 7.4 7.4 -25 2
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 None 0 Human Functional pKi = 6.4 6.4 - 0
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 None 0 Human Functional pKi = 6.4 6.4 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 68 Human Functional pKi = 5.4 5.4 - 20
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 None 0 Human Functional pKi = 7.4 7.4 - 0
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 None 0 Human Functional pKi = 7.4 7.4 - 0
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 None 0 Human Functional pKi = 6.4 6.4 - 0
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 None 0 Human Functional pKi = 6.4 6.4 - 0
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 None 1 Human Functional pKi = 6.3 6.3 - 0
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 None 1 Human Functional pKi = 6.3 6.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 8.3 8.3 - 0
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 None 0 Human Functional pKi = 7.3 7.3 - 0
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 None 0 Human Functional pKi = 7.3 7.3 - 0
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 None 73 Human Functional pKi = 5.2 5.2 - 0
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 None 73 Human Functional pKi = 5.2 5.2 - 0
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 None 0 Human Functional pKi = 8.2 8.2 - 0
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 None 0 Human Functional pKi = 8.2 8.2 - 0
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 None 72 Human Functional pKi = 8.2 8.2 -19 26
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 None 72 Human Functional pKi = 8.2 8.2 -19 26
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 None 72 Human Functional pKi = 8.2 8.2 -19 26
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 None 72 Human Functional pKi = 8.2 8.2 -19 26
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 None 1 Human Functional pKi = 7.2 7.2 - 0
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 None 1 Human Functional pKi = 7.2 7.2 - 0
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 None 0 Human Functional pKi = 8.1 8.1 - 0
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 None 0 Human Functional pKi = 8.1 8.1 - 0
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 None 0 Human Functional pKi = 7.2 7.2 - 0
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 None 0 Human Functional pKi = 7.2 7.2 - 0
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 None 1 Human Functional pKi = 6.1 6.1 - 0
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 None 1 Human Functional pKi = 6.1 6.1 - 0
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 None 17 Human Functional pKi = 5.1 5.1 - 0
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 None 17 Human Functional pKi = 5.1 5.1 - 0
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 None 0 Human Functional pKi = 6.1 6.1 - 0
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 None 0 Human Functional pKi = 6.1 6.1 - 0
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 None 0 Human Functional pKi = 7.1 7.1 -3 2
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 None 0 Human Functional pKi = 7.1 7.1 -3 2
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 None 0 Human Functional pKi = 8.0 8.0 15 2
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 None 0 Human Functional pKi = 8.0 8.0 15 2
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 None 5 Human Functional pKi = 7.0 7.0 - 0
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 None 5 Human Functional pKi = 7.0 7.0 - 0
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 None 37 Human Functional pEC50 = 8.2 8.2 -1 25
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 None 37 Human Functional pEC50 = 8.2 8.2 -1 25
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 None 37 Human Functional pEC50 = 8.2 8.2 -1 25
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 None 37 Human Functional pEC50 = 8.2 8.2 -1 25
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 None 37 Human Functional pEC50 = 8.2 8.2 -1 25
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 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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
6918314.0 3992 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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 None 94 Rat Functional pIC50 = 8.3 8.3 -707 16
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 None 55 Human Functional pIC50 = 6.2 6.2 -109 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
31 187 None 55 Human Functional pIC50 = 6.2 6.2 -109 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
7 187 None 55 Human Functional pIC50 = 6.2 6.2 -109 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
CHEMBL56 187 None 55 Human Functional pIC50 = 6.2 6.2 -109 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
137 138 None 0 Human Functional pIC50 None 11.9 11.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048565 138 None 0 Human Functional pIC50 None 11.9 11.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048566 138 None 0 Human Functional pIC50 None 11.9 11.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
1524 2181 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
3822.0 2181 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
3822.0 2181 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 96 Human Functional pIC50 None 5.3 5.3 -125 18
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 80 Human Functional pIC50 None 6.3 6.3 -33 8
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 None 8 Human Functional pIC50 None 6.8 6.8 -177 5
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 None 8 Human Functional pIC50 None 6.8 6.8 -177 5
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 None 8 Human Functional pIC50 None 6.8 6.8 -177 5
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 None 0 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
71351 2905 None 0 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
CHEMBL2104619 2905 None 0 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
DB06229 2905 None 0 Human Functional pIC50 None 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
110 1174 None 18 Human Functional pIC50 None 7.6 7.6 -1 2
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 None 18 Human Functional pIC50 None 7.6 7.6 -1 2
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 None 18 Human Functional pIC50 None 7.6 7.6 -1 2
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 None 14 Human Functional pKB = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
128018 1852 None 14 Human Functional pKB = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
CHEMBL119264 1852 None 14 Human Functional pKB = 7.4 7.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546




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

19066203 12089 None 0 Human Binding pEC50 = 8.7 8.7 47 3
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 None 0 Human Binding pEC50 = 8.7 8.7 47 3
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 None 0 Human Binding pEC50 = 8.7 8.7 47 3
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 None 0 Human Binding pEC50 = 8 8.0 28 3
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 None 0 Human Binding pEC50 = 8 8.0 28 3
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 None 0 Human Binding pEC50 = 8 8.0 28 3
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 None 72 Rat Binding pEC50 = 7.6 7.6 -13 54
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 None 72 Rat Binding pEC50 = 7.6 7.6 -13 54
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 None 72 Rat Binding pEC50 = 7.6 7.6 -13 54
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 None 72 Rat Binding pEC50 = 7.6 7.6 -13 54
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 None 7 Human Binding pEC50 = 5.6 5.6 - 0
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 None 72 Human Binding pEC50 = 7.5 7.5 -11 54
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 None 72 Human Binding pEC50 = 7.5 7.5 -11 54
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 None 72 Human Binding pEC50 = 7.5 7.5 -11 54
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 None 72 Human Binding pEC50 = 7.5 7.5 -11 54
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 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 None 0 Human Binding pEC50 = 6.2 6.2 - 0
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 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 None 0 Human Binding pIC50 = 9.7 9.7 - 0
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 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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
8223.0 1582 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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 None 14 Rat Binding pIC50 = 9.7 9.7 4 28
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 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 None 0 Human Binding pIC50 = 9.3 9.3 - 0
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 None 15 Rat Binding pIC50 = 9.3 9.3 - 0
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 None 15 Rat Binding pIC50 = 9.3 9.3 - 0
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 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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
5358.0 3707 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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 None 68 Human Binding pIC50 = 9.3 9.3 -3 32
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 None 22 Rat Binding pIC50 = 9.1 9.1 - 1
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 None 22 Rat Binding pIC50 = 9.1 9.1 - 1
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 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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
10531.0 1420 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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 None 21 Rat Binding pIC50 = 9.1 9.1 -5 23
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 None 21 Rat Binding pIC50 = 9.0 9.0 - 0
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 None 21 Rat Binding pIC50 = 9.0 9.0 - 0
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 None 27 Rat Binding pIC50 = 8.9 8.9 - 1
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 None 27 Rat Binding pIC50 = 8.9 8.9 - 1
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 19 Rat Binding pIC50 = 8.9 8.9 - 0
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 None 19 Rat Binding pIC50 = 8.9 8.9 - 0
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 1 Human Binding pIC50 = 8.9 8.9 - 0
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 54 Rat Binding pIC50 = 8.8 8.8 -4 17
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 None 38 Rat Binding pIC50 = 8.7 8.7 - 1
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 None 38 Rat Binding pIC50 = 8.7 8.7 - 1
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 None 68 Human Binding pIC50 = 8 8.0 -3 32
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 None 68 Human Binding pIC50 = 8 8.0 -3 32
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
5358.0 3707 None 68 Human Binding pIC50 = 8 8.0 -3 32
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 None 68 Human Binding pIC50 = 8 8.0 -3 32
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 None 68 Human Binding pIC50 = 8 8.0 -3 32
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 None 68 Human Binding pIC50 = 8 8.0 -3 32
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 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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
28864.0 2325 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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 None 27 Rat Binding pIC50 = 8 8.0 -58 44
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
10552663 121139 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 478 8 1 6 3.5 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1 10.1021/jm9910021
CHEMBL357634 121139 None 0 Human Binding pIC50 = 8 8.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 478 8 1 6 3.5 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1 10.1021/jm9910021
10578117 44041 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 529 8 1 7 5.4 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OCCF)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
CHEMBL151420 44041 None 0 Rat Binding pIC50 = 8 8.0 - 0
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 529 8 1 7 5.4 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OCCF)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
10790076 39988 None 0 Human Binding pIC50 = 7 7.0 - 0
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 458 10 3 6 3.3 OC[C@@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL147853 39988 None 0 Human Binding pIC50 = 7 7.0 - 0
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 458 10 3 6 3.3 OC[C@@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10076176 106435 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3126382 106435 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3139683 106435 None 0 Human Binding pIC50 = 7 7.0 - 0
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
10576874 41976 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 9 2 6 4.2 CC(=O)Nc1ccc(CN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL149488 41976 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 9 2 6 4.2 CC(=O)Nc1ccc(CN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10836986 168307 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 443 9 3 5 4.1 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL434125 168307 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 443 9 3 5 4.1 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10526736 10222 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
CHEMBL116031 10222 None 0 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
10671211 202727 None 0 Rat Binding pIC50 = 6 6.0 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL61818 202727 None 0 Rat Binding pIC50 = 6 6.0 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 449 6 0 5 4.8 Cn1c(=O)sc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
122186880 122980 None 0 Human Binding pIC50 = 6 6.0 - 5
Agonist activity at 5HT1B receptor (unknown origin)Agonist activity at 5HT1B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3608450 122980 None 0 Human Binding pIC50 = 6 6.0 - 5
Agonist activity at 5HT1B receptor (unknown origin)Agonist activity at 5HT1B receptor (unknown origin)
ChEMBL 415 3 0 5 4.8 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
2470 3653 None 50 Rat Binding pIC50 = 6 6.0 -43651 59
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00401a007
3300 3653 None 50 Rat Binding pIC50 = 6 6.0 -43651 59
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00401a007
5265 3653 None 50 Rat Binding pIC50 = 6 6.0 -43651 59
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00401a007
99 3653 None 50 Rat Binding pIC50 = 6 6.0 -43651 59
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00401a007
CHEMBL267930 3653 None 50 Rat Binding pIC50 = 6 6.0 -43651 59
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00401a007
10476735 13731 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1195096 13731 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL553833 13731 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 411 9 0 7 3.5 CCCN(CCCCn1c(=O)oc2cccnc21)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10342423 99469 None 0 Rat Binding pIC50 = 6 6.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28312 99469 None 0 Rat Binding pIC50 = 6 6.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL48925 99469 None 0 Rat Binding pIC50 = 6 6.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 426 11 1 5 3.9 CCCN(CCCCNC(=O)c1ccccc1OC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 99559 None 8 Rat Binding pIC50 = 6 6.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99559 None 8 Rat Binding pIC50 = 6 6.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10072866 197475 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL51561 197475 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL56990 197475 None 0 Rat Binding pIC50 = 6 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 458 9 0 6 3.3 CCCN(CCCCN1C(=O)c2ccccc2S1(=O)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10671315 203011 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL63258 203011 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
10575553 203039 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63432 203039 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10767140 203370 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 482 8 1 5 4.5 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
CHEMBL65215 203370 None 0 Human Binding pIC50 = 6 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 482 8 1 5 4.5 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
121852 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251234 11245 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11245 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11245 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10024943 97390 None 0 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26975 97390 None 0 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52485 97390 None 0 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 416 9 0 5 3.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5 5.0 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
10571450 101871 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 374 3 0 4 4.3 Cc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL300692 101871 None 0 Rat Binding pIC50 = 5 5.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 374 3 0 4 4.3 Cc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
57397383 67952 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of 5-HT1BInhibition of 5-HT1B
ChEMBL 374 2 2 4 3.8 Cc1nnc(-c2ccc(C)c(-c3ccc4c(c3)NC(=O)C43CCOCC3)c2)[nH]1 10.1016/j.bmcl.2011.09.006
CHEMBL1911194 67952 None 0 Human Binding pIC50 = 5 5.0 - 0
Inhibition of 5-HT1BInhibition of 5-HT1B
ChEMBL 374 2 2 4 3.8 Cc1nnc(-c2ccc(C)c(-c3ccc4c(c3)NC(=O)C43CCOCC3)c2)[nH]1 10.1016/j.bmcl.2011.09.006
10014217 99748 None 0 Rat Binding pIC50 = 4 4.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
CHEMBL285010 99748 None 0 Rat Binding pIC50 = 4 4.0 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 233 2 0 3 2.1 COc1cccc2c1CC(N1CCCC1)CO2 10.1021/jm00038a007
10719202 56557 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 471 8 1 6 3.1 CN(C)C(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL164035 56557 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 471 8 1 6 3.1 CN(C)C(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
9863146 194992 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL54720 194992 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
9863146 194992 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL54720 194992 None 1 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm960501o
10852612 203432 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 0 5 3.1 c1cc2c(N3CCN(CC4CC4)CC3)nc3ccsc3n2c1 10.1021/jm950543x
CHEMBL65736 203432 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 0 5 3.1 c1cc2c(N3CCN(CC4CC4)CC3)nc3ccsc3n2c1 10.1021/jm950543x
31101 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
31101.0 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 729 None 40 Rat Binding pIC50 = 7.0 7.0 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
10849641 113090 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 270 1 1 4 2.0 Fc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm970376w
CHEMBL331304 113090 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 270 1 1 4 2.0 Fc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm970376w
10590360 203336 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 300 3 0 5 3.1 CCCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL64948 203336 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 300 3 0 5 3.1 CCCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
10621021 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.5b00258
CHEMBL65367 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.5b00258
2543 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
5358 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
5358.0 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
54 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
CHEMBL128 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
DB00669 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
10621021 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL65367 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
2543 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
5358 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
5358.0 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
54 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
CHEMBL128 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
DB00669 3707 None 68 Human Binding pIC50 = 8.0 8.0 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
10789334 165341 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 442 8 1 5 3.7 CC(=O)N(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL423599 165341 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 442 8 1 5 3.7 CC(=O)N(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10621021 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL65367 203384 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
2543 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358.0 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
54 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL128 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB00669 3707 None 68 Rat Binding pIC50 = 7.0 7.0 -17 32
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
10646958 11407 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL118012 11407 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10787241 54592 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 401 8 2 6 2.8 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)ccn1 10.1021/jm9805687
CHEMBL161066 54592 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 401 8 2 6 2.8 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)ccn1 10.1021/jm9805687
10788620 40047 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 427 8 2 4 5.1 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL147907 40047 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 427 8 2 4 5.1 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4ccnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10131112 1552 None 25 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in calfInhibitory activity against 5-hydroxytryptamine 1B receptor in calf
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1552 None 25 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in calfInhibitory activity against 5-hydroxytryptamine 1B receptor in calf
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1552 None 25 Human Binding pIC50 = 7.0 7.0 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in calfInhibitory activity against 5-hydroxytryptamine 1B receptor in calf
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
15951404 125389 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 308 3 2 3 3.2 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4ccco4)cc23)C1 nan
CHEMBL3645480 125389 None 0 Rat Binding pIC50 = 6.0 6.0 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 308 3 2 3 3.2 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4ccco4)cc23)C1 nan
10635163 164927 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 261 3 0 3 2.9 CCCN1CCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
CHEMBL422453 164927 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 261 3 0 3 2.9 CCCN1CCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
18366015 78372 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2110300 78372 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10550367 115207 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
CHEMBL334498 115207 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.Compound was evaluated for binding affinity on 5-HT1B receptors using rat cortex+striatum+ globus pallidus,[ 3H]-5-OH-tryptamine, and serotonin for NSB.
ChEMBL 426 7 1 4 4.2 COc1cccc2c1CC1(CCCCN1CCCCNC(=O)c1ccc(F)cc1)CO2 10.1021/jm950861w
10664878 89270 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 340 4 3 3 2.2 CC1(C)NC(=O)N(CCc2ccc3[nH]cc([C@H]4C[C@H](N)C4)c3c2)C1=O 10.1021/jm000956k
CHEMBL2368255 89270 None 0 Human Binding pIC50 = 6.0 6.0 - 0
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 340 4 3 3 2.2 CC1(C)NC(=O)N(CCc2ccc3[nH]cc([C@H]4C[C@H](N)C4)c3c2)C1=O 10.1021/jm000956k
10516340 203466 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 272 1 0 5 2.3 CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL65974 203466 None 0 Rat Binding pIC50 = 5.0 5.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 272 1 0 5 2.3 CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
10529106 98314 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
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 490 5 3 5 3.4 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C(N)=O)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL274922 98314 None 0 Rat Binding pIC50 = 7.0 7.0 - 0
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 490 5 3 5 3.4 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C(N)=O)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10646958 11407 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
CHEMBL118012 11407 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
5 139 None 72 Human Binding pIC50 = 7.9 7.9 -11 54
Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assayBinding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
5202 139 None 72 Human Binding pIC50 = 7.9 7.9 -11 54
Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assayBinding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
CHEMBL39 139 None 72 Human Binding pIC50 = 7.9 7.9 -11 54
Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assayBinding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
DB08839 139 None 72 Human Binding pIC50 = 7.9 7.9 -11 54
Binding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assayBinding affinity to 5-HT1B receptor (unknown origin) by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2013.03.016
73356443 89701 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376490 89701 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 294 2 2 2 4.6 Cc1[nH]c2ccc(-c3ccsc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
11794750 119904 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 390 8 2 6 3.0 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)co1 10.1021/jm9805687
CHEMBL349185 119904 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 390 8 2 6 3.0 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)co1 10.1021/jm9805687
10838684 119140 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 487 10 3 7 3.6 NC(=O)OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL342805 119140 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 487 10 3 7 3.6 NC(=O)OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10814424 99004 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 475 6 2 4 4.8 COc1ccc(NC(=O)N2CCC(CCc3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL280000 99004 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 475 6 2 4 4.8 COc1ccc(NC(=O)N2CCC(CCc3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10574762 10143 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL115750 10143 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10597901 10653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL117046 10653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10574762 10143 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
CHEMBL115750 10143 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
10601144 119388 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 490 11 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
CHEMBL344537 119388 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 490 11 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
9803620 162460 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)C1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL416688 162460 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)C1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
10575553 203039 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63432 203039 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10714071 89277 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 368 5 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)NC(C)(C)C4=O)cc32)C1 10.1021/jm000956k
CHEMBL2368262 89277 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 368 5 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)NC(C)(C)C4=O)cc32)C1 10.1021/jm000956k
10597901 10653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704558
CHEMBL117046 10653 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704558
10740531 119866 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 414 9 2 5 3.4 c1ccc(CCNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL348815 119866 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 414 9 2 5 3.4 c1ccc(CCNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
2477 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
2477.0 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
36 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
437 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
CHEMBL49 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
DB00490 745 None 59 Rat Binding pIC50 = 4.9 4.9 -16 29
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00401a007
10617292 194709 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 342 3 0 4 3.8 c1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL53416 194709 None 0 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 342 3 0 4 3.8 c1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
2585 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2585.0 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 None 103 Rat Binding pIC50 = 5.9 5.9 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
10667886 56015 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 386 6 1 5 3.5 c1ccc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL162463 56015 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 386 6 1 5 3.5 c1ccc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
44214559 56498 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163462 56498 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10573843 120147 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 414 7 1 5 4.1 CC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL351346 120147 None 0 Human Binding pIC50 = 7.9 7.9 - 0
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 414 7 1 5 4.1 CC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10504600 39948 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 10 2 6 4.0 CN(C)C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL147818 39948 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 10 2 6 4.0 CN(C)C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
71459969 79530 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F 10.1021/jm981133m
CHEMBL2114040 79530 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F 10.1021/jm981133m
15226949 102027 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1 10.1021/jm950543x
CHEMBL301765 102027 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1 10.1021/jm950543x
15226949 102027 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1 10.1021/jm960501o
CHEMBL301765 102027 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 258 1 1 5 2.0 c1cc2c(N3CCNCC3)nc3ccsc3n2c1 10.1021/jm960501o
10764869 119737 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 425 7 1 6 3.4 N#Cc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL347665 119737 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 425 7 1 6 3.4 N#Cc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
9911120 9623 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 9623 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
10837591 118761 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL341854 118761 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(Cn4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10694177 203108 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
CHEMBL64003 203108 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
9841032 194737 None 1 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 343 3 0 5 3.2 c1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL53573 194737 None 1 Rat Binding pIC50 = 4.9 4.9 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 343 3 0 5 3.2 c1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1 10.1021/jm960501o
14450355 119968 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 259 3 0 3 3.0 CCCN1CCC=C2c3c(OC)cccc3OCC21 10.1021/jm00123a039
CHEMBL349824 119968 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol, binds to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 259 3 0 3 3.0 CCCN1CCC=C2c3c(OC)cccc3OCC21 10.1021/jm00123a039
10696635 98909 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 10 3 5 4.3 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
CHEMBL279320 98909 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
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 10 3 5 4.3 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
10612178 119865 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 271 4 2 2 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(N)=O)cc32)C1 10.1021/jm000956k
CHEMBL348811 119865 None 0 Human Binding pIC50 = 5.9 5.9 - 0
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 271 4 2 2 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(N)=O)cc32)C1 10.1021/jm000956k
3823 50221 None 42 Rat Binding pIC50 = 4.9 4.9 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 50221 None 42 Rat Binding pIC50 = 4.9 4.9 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 50221 None 42 Rat Binding pIC50 = 4.9 4.9 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
213 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533.0 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3853 None 55 Rat Binding pIC50 = 5.9 5.9 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2247 505 None 81 Rat Binding pIC50 = 5.9 5.9 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Rat Binding pIC50 = 5.9 5.9 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Rat Binding pIC50 = 5.9 5.9 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Rat Binding pIC50 = 5.9 5.9 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Rat Binding pIC50 = 5.9 5.9 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
72548703 161567 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
CHEMBL4128926 161567 None 0 Rat Binding pIC50 = 7.9 7.9 - 0
Displacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysisDisplacement of [125I]-CYP from rat brain 5-HT1B receptor after 120 mins by scintillation counting analysis
ChEMBL 583 8 3 6 5.8 CC(C)(C)NS(=O)(=O)c1ccc(-c2sc(C(=O)N[C@H]3C[C@H](C(=O)O)C3)nc2CC2CCCCC2)c2ccccc12 10.1016/j.bmcl.2018.03.093
10551206 119258 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 2 5 4.7 C[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL343648 119258 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 2 5 4.7 C[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10719687 202999 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL63167 202999 None 0 Human Binding pIC50 = 7.9 7.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
110 1174 None 18 Human Binding pIC50 = 7.8 7.8 - 0
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 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
132552 1174 None 18 Human Binding pIC50 = 7.8 7.8 - 0
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 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
CHEMBL159332 1174 None 18 Human Binding pIC50 = 7.8 7.8 - 0
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 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
10718714 38142 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 458 10 3 6 3.3 OC[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146131 38142 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 458 10 3 6 3.3 OC[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
73351905 89702 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376491 89702 None 0 Rat Binding pIC50 = 6.9 6.9 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 288 2 2 1 4.5 Cc1[nH]c2ccc(-c3ccccc3)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
10835665 38891 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm9910021
CHEMBL146729 38891 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm9910021
10549785 39085 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1cncc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9910021
CHEMBL146891 39085 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1cncc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9910021
10625408 39720 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 506 9 1 7 3.7 CN(Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL147555 39720 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 506 9 1 7 3.7 CN(Cc1ccc(S(C)(=O)=O)cc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10766277 40537 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 457 7 2 5 4.3 CN(C(=O)Nc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL148325 40537 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 457 7 2 5 4.3 CN(C(=O)Nc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
11796806 102717 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL304857 102717 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10717709 165282 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 434 8 1 6 4.3 CN(Cc1cccs1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL423212 165282 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 434 8 1 6 4.3 CN(Cc1cccs1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
11796806 102717 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL304857 102717 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
10504100 47740 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL154787 47740 None 0 Rat Binding pIC50 = 5.9 5.9 - 0
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
ChEMBL 458 7 1 8 4.2 COc1ccccc1C1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
10592324 103462 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 327 5 2 3 2.7 CN(C)[C@H]1C[C@H](Cc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1 10.1021/jm000956k
CHEMBL3084967 103462 None 0 Human Binding pIC50 = 6.9 6.9 - 0
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 327 5 2 3 2.7 CN(C)[C@H]1C[C@H](Cc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1 10.1021/jm000956k
11793287 163277 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 366 3 0 5 4.0 Fc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL418678 163277 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 366 3 0 5 4.0 Fc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
19978059 162447 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 420 3 0 6 4.2 Clc1ccc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12 10.1021/jm960501o
CHEMBL416662 162447 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 420 3 0 6 4.2 Clc1ccc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12 10.1021/jm960501o
11796806 102717 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
CHEMBL304857 102717 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
10614907 98185 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 310 5 2 5 1.6 c1cc2[nH]cc(CCCN3CCNCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL274001 98185 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 310 5 2 5 1.6 c1cc2[nH]cc(CCCN3CCNCC3)c2cc1-n1cnnc1 10.1021/jm980569z
9930155 164032 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL420874 164032 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
9930155 164032 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420874 164032 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
11792032 202821 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 2 0 5 4.0 CN1CCN(c2nc3cc(-c4ccccc4)sc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL62366 202821 None 0 Rat Binding pIC50 = 4.8 4.8 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 2 0 5 4.0 CN1CCN(c2nc3cc(-c4ccccc4)sc3n3cccc23)CC1 10.1021/jm950543x
10733696 113328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL331612 113328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
150 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226.0 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2509 None 21 Rat Binding pIC50 = 7.8 7.8 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
9844873 101058 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.5b00258
CHEMBL294732 101058 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.5b00258
10733696 113328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL331612 113328 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10597902 53000 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 414 8 1 5 3.9 CN(Cc1ccccc1)C[C@@H]1CCCN1CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
CHEMBL159683 53000 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 414 8 1 5 3.9 CN(Cc1ccccc1)C[C@@H]1CCCN1CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
9844873 101058 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL294732 101058 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
11 1187 None 19 Rat Binding pIC50 = 7.8 7.8 - 1
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 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
124007 1187 None 19 Rat Binding pIC50 = 7.8 7.8 - 1
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 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL304008 1187 None 19 Rat Binding pIC50 = 7.8 7.8 - 1
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 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
10766319 38758 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 458 10 3 6 3.9 OCCC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146628 38758 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 458 10 3 6 3.9 OCCC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
16 2253 None 8 Human Binding pIC50 = 6.8 6.8 - 1
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
9847194 2253 None 8 Human Binding pIC50 = 6.8 6.8 - 1
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
CHEMBL313714 2253 None 8 Human Binding pIC50 = 6.8 6.8 - 1
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9910021
10813769 120989 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 9 3 6 3.9 C[C@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL356315 120989 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 9 3 6 3.9 C[C@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
109 902 None 31 Rat Binding pIC50 = 6.8 6.8 - 7
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 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
2689 902 None 31 Rat Binding pIC50 = 6.8 6.8 - 7
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 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
CHEMBL27403 902 None 31 Rat Binding pIC50 = 6.8 6.8 - 7
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 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
10753377 194723 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 253 1 1 5 1.3 c1cnc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm960501o
CHEMBL53490 194723 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 253 1 1 5 1.3 c1cnc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm960501o
10757342 55107 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 310 4 1 4 3.3 Cc1noc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1 10.1021/jm000956k
CHEMBL161694 55107 None 0 Human Binding pIC50 = 5.8 5.8 - 0
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 310 4 1 4 3.3 Cc1noc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1 10.1021/jm000956k
44267168 9855 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 497 8 0 6 3.9 CCCN1CCN(CCCCN2C(=O)CC3(CCCC3)CC2=O)CC12COc1cccc(OC)c1C2 10.1016/0960-894X(96)00174-6
CHEMBL11409 9855 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 497 8 0 6 3.9 CCCN1CCN(CCCCN2C(=O)CC3(CCCC3)CC2=O)CC12COc1cccc(OC)c1C2 10.1016/0960-894X(96)00174-6
2543 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
5358 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
5358.0 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
54 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
CHEMBL128 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
DB00669 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
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 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
2543 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
5358 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
5358.0 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
54 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
CHEMBL128 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
DB00669 3707 None 68 Human Binding pIC50 = 7.8 7.8 -3 32
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704560
10813413 203681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1ccccc1CCC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL67460 203681 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1ccccc1CCC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
5 139 None 72 Human Binding pIC50 = 7.8 7.8 -11 54
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 139 None 72 Human Binding pIC50 = 7.8 7.8 -11 54
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 139 None 72 Human Binding pIC50 = 7.8 7.8 -11 54
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 139 None 72 Human Binding pIC50 = 7.8 7.8 -11 54
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
15951194 71638 None 12 Rat Binding pIC50 = 6.8 6.8 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 336 3 2 3 4.0 CN1CC=C(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)CC1 nan
CHEMBL1963527 71638 None 12 Rat Binding pIC50 = 6.8 6.8 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 336 3 2 3 4.0 CN1CC=C(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)CC1 nan
11797562 38143 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 444 9 3 6 3.5 OC[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146132 38143 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 444 9 3 6 3.5 OC[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10695596 102793 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 468 8 1 5 3.9 Fc1cccc(CCN2CCN(CC(F)(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL305301 102793 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 468 8 1 5 3.9 Fc1cccc(CCN2CCN(CC(F)(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
18366015 78372 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2110300 78372 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10718668 119919 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 457 9 3 6 3.4 CC(=O)Nc1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL349390 119919 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 457 9 3 6 3.4 CC(=O)Nc1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10502763 120142 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 430 9 3 6 2.9 OC[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL351303 120142 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 430 9 3 6 2.9 OC[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10645471 11042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL117633 11042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10516184 14529 None 4 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 270 1 1 4 2.0 Fc1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm970376w
CHEMBL120216 14529 None 4 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 270 1 1 4 2.0 Fc1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm970376w
10789399 119874 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 443 9 2 6 3.3 CNCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL348962 119874 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 443 9 2 6 3.3 CNCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10551207 38598 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 442 9 2 5 4.4 C[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146502 38598 None 0 Human Binding pIC50 = 6.8 6.8 - 0
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 442 9 2 5 4.4 C[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10696275 38009 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 10 3 6 3.9 CC(=O)Nc1ccc(CCNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146023 38009 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 10 3 6 3.9 CC(=O)Nc1ccc(CCNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10645471 11042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
CHEMBL117633 11042 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
10814273 114352 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1cccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9704560
CHEMBL333089 114352 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1cccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9704560
67650695 79527 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 500 8 2 5 4.9 F[C@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F 10.1021/jm981133m
CHEMBL2114038 79527 None 0 Human Binding pIC50 = 6.8 6.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 500 8 2 5 4.9 F[C@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F 10.1021/jm981133m
134 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681.0 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2514 None 24 Rat Binding pIC50 = 6.8 6.8 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
2543 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358.0 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
54 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL128 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB00669 3707 None 68 Rat Binding pIC50 = 7.8 7.8 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
10620429 56264 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 390 7 1 6 3.1 c1coc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL162805 56264 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 390 7 1 6 3.1 c1coc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10644750 56512 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 401 7 1 6 2.9 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
CHEMBL163573 56512 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 401 7 1 6 2.9 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
10574671 120225 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 430 7 1 5 3.8 S=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
CHEMBL352159 120225 None 0 Human Binding pIC50 = 7.8 7.8 - 0
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 430 7 1 5 3.8 S=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
10719938 37960 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 492 9 1 6 3.7 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1 10.1021/jm9910021
CHEMBL145982 37960 None 0 Human Binding pIC50 = 7.8 7.8 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 492 9 1 6 3.7 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)S(=O)(=O)c1ccccc1 10.1021/jm9910021
18691541 78371 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 285 3 3 3 2.0 N[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2110299 78371 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 285 3 3 3 2.0 N[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10809876 102653 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
CHEMBL304438 102653 None 0 Rat Binding pIC50 = 6.8 6.8 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 381 5 0 5 2.4 COc1ccccc1N1CCN(CCc2ccc3c(c2)OCC(=O)N3C)CC1 10.1021/jm970298c
10131112 1552 None 25 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
8428 1552 None 25 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
CHEMBL364005 1552 None 25 Rat Binding pIC50 = 6.8 6.8 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
ChEMBL 246 1 2 1 3.5 Clc1ccc2c(c1)c(C1=CCNCC1)c([nH]2)C 10.1016/j.bmcl.2005.06.067
10837853 168158 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL433108 168158 None 0 Human Binding pIC50 = 5.8 5.8 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
7059581 167045 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm00401a007
CHEMBL428892 167045 None 3 Rat Binding pIC50 = 6.7 6.7 - 2
Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity towards 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm00401a007
16 2253 None 8 Human Binding pIC50 = 6.7 6.7 - 1
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 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
9847194 2253 None 8 Human Binding pIC50 = 6.7 6.7 - 1
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 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
CHEMBL313714 2253 None 8 Human Binding pIC50 = 6.7 6.7 - 1
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 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
2351 3286 None 64 Rat Binding pIC50 = 5.7 5.7 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3286 None 64 Rat Binding pIC50 = 5.7 5.7 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3286 None 64 Rat Binding pIC50 = 5.7 5.7 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3286 None 64 Rat Binding pIC50 = 5.7 5.7 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3286 None 64 Rat Binding pIC50 = 5.7 5.7 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
10717512 203068 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 0 5 4.9 FC(F)(F)c1ccccc1CCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL63713 203068 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 0 5 4.9 FC(F)(F)c1ccccc1CCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
15516682 10290 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 450 7 2 6 3.6 CC1(C)CCCN(CC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)C1 10.1016/s0960-894x(99)00614-9
CHEMBL116161 10290 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 450 7 2 6 3.6 CC1(C)CCCN(CC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)C1 10.1016/s0960-894x(99)00614-9
133 2496 None 52 Rat Binding pIC50 = 7.7 7.7 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 None 52 Rat Binding pIC50 = 7.7 7.7 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 None 52 Rat Binding pIC50 = 7.7 7.7 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 None 52 Rat Binding pIC50 = 7.7 7.7 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 None 52 Rat Binding pIC50 = 7.7 7.7 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
18975369 101029 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.5b00258
CHEMBL294547 101029 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cellsDisplacement of [3H]-5-HT from human 5HT-1B receptor expressed in CHO cells
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.5b00258
18975369 101029 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL294547 101029 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
10576618 202940 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 478 3 0 5 6.6 FC(F)(F)c1cccc(N2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)c1 10.1021/jm950543x
CHEMBL62902 202940 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 478 3 0 5 6.6 FC(F)(F)c1cccc(N2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)c1 10.1021/jm950543x
10738329 101734 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 376 3 0 4 4.5 Clc1ccc2c(c1)nc(N1CCN(Cc3ccccc3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL299634 101734 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 376 3 0 4 4.5 Clc1ccc2c(c1)nc(N1CCN(Cc3ccccc3)CC1)c1cccn12 10.1021/jm960501o
1212 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372.0 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 None 50 Rat Binding pIC50 = 5.7 5.7 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44305547 203330 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 380 4 0 5 4.0 Fc1ccc(CN2CCN(Cc3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL64903 203330 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 380 4 0 5 4.0 Fc1ccc(CN2CCN(Cc3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
10569395 101648 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 343 3 0 5 3.3 C=CCN1CCN(c2nc3ccc4ncccc4c3n3cccc23)CC1 10.1021/jm960501o
CHEMBL299097 101648 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 343 3 0 5 3.3 C=CCN1CCN(c2nc3ccc4ncccc4c3n3cccc23)CC1 10.1021/jm960501o
124 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 47 Rat Binding pIC50 = 8.7 8.7 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
130 3500 None 47 Rat Binding pIC50 = 8.7 8.7 -8 13
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 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
3378093 3500 None 47 Rat Binding pIC50 = 8.7 8.7 -8 13
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 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
CHEMBL281350 3500 None 47 Rat Binding pIC50 = 8.7 8.7 -8 13
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 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
108029 3414 None 57 Rat Binding pIC50 = 8.7 8.7 -3 13
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 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
23 3414 None 57 Rat Binding pIC50 = 8.7 8.7 -3 13
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 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL18785 3414 None 57 Rat Binding pIC50 = 8.7 8.7 -3 13
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 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
10838923 52635 None 0 Rat Binding pIC50 = 8.7 8.7 - 3
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 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm9811054
CHEMBL15933 52635 None 0 Rat Binding pIC50 = 8.7 8.7 - 3
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 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm9811054
11798094 54719 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 457 8 2 6 3.5 CC(=O)Nc1cccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL161176 54719 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 457 8 2 6 3.5 CC(=O)Nc1cccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10787240 119806 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 401 8 1 5 4.0 c1ccc(COC[C@@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
CHEMBL348304 119806 None 0 Human Binding pIC50 = 8.6 8.6 - 0
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 401 8 1 5 4.0 c1ccc(COC[C@@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
1042 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884.0 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1581 None 23 Rat Binding pIC50 = 8.6 8.6 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
196129 67798 None 17 Rat Binding pIC50 = 8.5 8.5 -1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67798 None 17 Rat Binding pIC50 = 8.5 8.5 -1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
10547091 202098 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL60885 202098 None 0 Rat Binding pIC50 = 7.7 7.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 369 5 1 6 3.4 COc1ccccc1N1CCN(CCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
10716915 55145 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 418 7 1 5 3.6 Fc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL161723 55145 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 418 7 1 5 3.6 Fc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10572483 119887 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 390 8 2 6 3.0 c1coc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
CHEMBL349041 119887 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 390 8 2 6 3.0 c1coc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
10522029 203149 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 353 4 0 5 3.0 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4)CC3)ccc21 10.1021/jm970298c
CHEMBL64167 203149 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 353 4 0 5 3.0 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4)CC3)ccc21 10.1021/jm970298c
10524876 203325 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL64878 203325 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 397 7 1 6 4.2 COc1ccccc1N1CCN(CCCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
10504095 165261 None 1 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](O)c1ccccc1 10.1021/jm9910021
CHEMBL423022 165261 None 1 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](O)c1ccccc1 10.1021/jm9910021
73347306 89694 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376483 89694 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 230 1 2 1 3.0 Cc1[nH]c2ccc(F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
10645715 40263 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 418 8 1 6 3.9 CN(Cc1ccoc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL148085 40263 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 418 8 1 6 3.9 CN(Cc1ccoc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
9980269 99083 None 0 Rat Binding pIC50 = 5.7 5.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL280586 99083 None 0 Rat Binding pIC50 = 5.7 5.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54266 99083 None 0 Rat Binding pIC50 = 5.7 5.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 432 10 1 5 3.4 CCCN(CCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10251234 11245 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11245 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11245 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9978353 11253 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL1178987 11253 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
CHEMBL52785 11253 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 7 1 5 3.1 COc1cccc2c1CC(NCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm00038a007
10095594 12368 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1185501 12368 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL417550 12368 None 0 Rat Binding pIC50 = 4.7 4.7 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 456 10 0 5 4.6 CCCN(CCCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
9981024 96097 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 96097 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 96097 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10252000 98547 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27650 98547 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50188 98547 None 0 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 428 8 0 5 3.8 CCCN(CCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 99559 None 8 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99559 None 8 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
3082597 99559 None 8 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL283606 99559 None 8 Rat Binding pIC50 = 4.7 4.7 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm950861w
18691565 89272 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
CHEMBL2368257 89272 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
10643940 89276 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 387 5 1 3 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)c5ccccc5C4=O)cc32)C1 10.1021/jm000956k
CHEMBL2368261 89276 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 387 5 1 3 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CCN4C(=O)c5ccccc5C4=O)cc32)C1 10.1021/jm000956k
10637485 101665 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 293 3 0 5 2.2 C=CCN1CCN(c2nc3cccnc3n3cccc23)CC1 10.1021/jm960501o
CHEMBL299231 101665 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 293 3 0 5 2.2 C=CCN1CCN(c2nc3cccnc3n3cccc23)CC1 10.1021/jm960501o
4189 206922 None 96 Rat Binding pIC50 = 4.7 4.7 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Rat Binding pIC50 = 4.7 4.7 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Rat Binding pIC50 = 4.7 4.7 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10621020 110385 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL324287 110385 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10805623 99252 None 0 Rat Binding pIC50 = 7.7 7.7 - 1
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 320 1 1 4 2.9 FC(F)(F)c1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm00170a007
CHEMBL28178 99252 None 0 Rat Binding pIC50 = 7.7 7.7 - 1
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 320 1 1 4 2.9 FC(F)(F)c1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm00170a007
10575878 35528 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](O)c1ccccc1 10.1021/jm9910021
CHEMBL143890 35528 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](O)c1ccccc1 10.1021/jm9910021
10766318 37773 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 10 2 6 4.1 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL145815 37773 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 10 2 6 4.1 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10551857 165372 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
CHEMBL423749 165372 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
10621020 110385 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
CHEMBL324287 110385 None 0 Human Binding pIC50 = 6.7 6.7 - 0
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 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
10766235 78860 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 456 7 3 6 3.4 O[C@@H]1Cc2ccccc2[C@H]1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL2112862 78860 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 456 7 3 6 3.4 O[C@@H]1Cc2ccccc2[C@H]1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10624003 203663 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.5 CN(Cc1ccccc1)C1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL67367 203663 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.5 CN(Cc1ccccc1)C1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
135398737 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
135398737.0 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 None 93 Rat Binding pIC50 = 5.7 5.7 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
146420029 184762 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
CHEMBL4851044 184762 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 379 3 1 3 4.2 CN1CCC(=C(F)c2cccc(NC(=O)c3c(F)cc(F)cc3F)n2)CC1 10.1016/j.ejmech.2021.113782
10834909 164920 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 401 7 1 6 2.9 c1cncc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL422366 164920 None 0 Human Binding pIC50 = 7.7 7.7 - 0
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 401 7 1 6 2.9 c1cncc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10503687 203077 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63799 203077 None 0 Human Binding pIC50 = 7.7 7.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
67650716 79528 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F 10.1021/jm981133m
CHEMBL2114039 79528 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@@H]1F 10.1021/jm981133m
71450983 79649 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F 10.1021/jm981133m
CHEMBL2115112 79649 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 514 8 1 5 5.2 CN(Cc1ccccc1C(F)(F)F)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F 10.1021/jm981133m
44323506 207022 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F 10.1021/jm981133m
CHEMBL91534 207022 None 0 Human Binding pIC50 = 6.7 6.7 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 446 8 1 5 4.2 CN(Cc1ccccc1)[C@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C[C@H]1F 10.1021/jm981133m
25014630 83539 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
CHEMBL2203713 83539 None 1 Human Binding pIC50 = 5.7 5.7 - 0
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 326 3 3 4 3.3 N=C(Nc1ccc2c(c1)CCN2C1CCNCC1)c1cccs1 10.1016/j.ejmech.2012.07.006
3198 205513 None 76 Rat Binding pIC50 = 4.7 4.7 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Rat Binding pIC50 = 4.7 4.7 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Rat Binding pIC50 = 4.7 4.7 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
11744707 164909 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL422283 164909 None 0 Rat Binding pIC50 = 5.7 5.7 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 454 6 0 5 4.3 COc1cccc2c1CC1(CCCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
10696986 52963 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 508 7 3 5 4.1 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15965 52963 None 0 Rat Binding pIC50 = 6.7 6.7 - 0
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 508 7 3 5 4.1 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
44267181 9611 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11262 9611 None 0 Human Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 277 7 0 3 3.4 CCCN(CCC)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
10552023 98603 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 462 2 2 3 5.1 CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12 10.1021/jm9811054
CHEMBL276928 98603 None 0 Rat Binding pIC50 = 7.6 7.6 - 0
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 462 2 2 3 5.1 CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12 10.1021/jm9811054
11795333 56271 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 401 7 1 6 2.9 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm980569z
CHEMBL162858 56271 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 401 7 1 6 2.9 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm980569z
10813272 38319 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 446 8 2 5 4.6 CC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
CHEMBL146285 38319 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 446 8 2 5 4.6 CC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
3191 102858 None 97 Rat Binding pIC50 = 5.6 5.6 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
3191.0 102858 None 97 Rat Binding pIC50 = 5.6 5.6 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 None 97 Rat Binding pIC50 = 5.6 5.6 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 102858 None 97 Rat Binding pIC50 = 5.6 5.6 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10378253 111397 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 266 1 0 4 2.2 CN1CCN(c2nc3ccccc3n3cccc23)CC1 10.1021/jm970376w
CHEMBL327197 111397 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 266 1 0 4 2.2 CN1CCN(c2nc3ccccc3n3cccc23)CC1 10.1021/jm970376w
10647243 98949 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 451 4 2 4 4.1 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)C2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL279646 98949 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 451 4 2 4 4.1 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)C2)cc1N1CCN(C)CC1 10.1021/jm9811054
10622257 102132 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 424 4 0 5 5.5 c1ccc(CN2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL302447 102132 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 424 4 0 5 5.5 c1ccc(CN2CCN(c3nc4scc(-c5ccccc5)c4n4cccc34)CC2)cc1 10.1021/jm950543x
107715 200945 None 22 Rat Binding pIC50 = 7.6 7.6 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200945 None 22 Rat Binding pIC50 = 7.6 7.6 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200945 None 22 Rat Binding pIC50 = 7.6 7.6 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
10577311 39792 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 2 6 4.5 CC(=O)Nc1ccc(CN(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL147660 39792 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 2 6 4.5 CC(=O)Nc1ccc(CN(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10835928 121071 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 420 9 1 5 4.4 CC(C)=CCCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL357007 121071 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 420 9 1 5 4.4 CC(C)=CCCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
25060119 104315 None 0 Rat Binding pIC50 = 5.6 5.6 -32359 7
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 104315 None 0 Rat Binding pIC50 = 5.6 5.6 -32359 7
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
19978038 195019 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3cccnc3n3cccc23)CC1 10.1021/jm960501o
CHEMBL54914 195019 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3cccnc3n3cccc23)CC1 10.1021/jm960501o
10623614 121050 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 454 8 2 5 4.7 c1ccc2c(c1)CCC2NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL356808 121050 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 454 8 2 5 4.7 c1ccc2c(c1)CCC2NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10647181 100866 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1ccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL293614 100866 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 Fc1ccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
135398737 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
135398737.0 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
38 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
722 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
CHEMBL42 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
DB00363 958 None 93 Rat Binding pIC50 = 5.6 5.6 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1021/jm970298c
10838153 14101 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
CHEMBL119785 14101 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
10832055 202734 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 355 4 2 6 3.1 Oc1nc2ccc(CCN3CCN(c4ccccc4O)CC3)cc2s1 10.1021/jm970298c
CHEMBL61869 202734 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 355 4 2 6 3.1 Oc1nc2ccc(CCN3CCN(c4ccccc4O)CC3)cc2s1 10.1021/jm970298c
10838153 14101 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL119785 14101 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
11796081 54737 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 414 9 2 5 3.5 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(Cn5cncn5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL161192 54737 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 414 9 2 5 3.5 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(Cn5cncn5)cc34)C2)cc1 10.1021/jm9805687
10691928 39924 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 392 8 1 5 3.5 CN(CC1CC1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL147786 39924 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 392 8 1 5 3.5 CN(CC1CC1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10671996 118766 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 468 10 3 4 4.0 CNS(=O)(=O)Cc1ccc2[nH]cc(CCCN3CCC(N[C@H](C)c4ccccc4)CC3)c2c1 10.1021/jm9910021
CHEMBL341897 118766 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 468 10 3 4 4.0 CNS(=O)(=O)Cc1ccc2[nH]cc(CCCN3CCC(N[C@H](C)c4ccccc4)CC3)c2c1 10.1021/jm9910021
2477 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
2477.0 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
36 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
437 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
CHEMBL49 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
DB00490 745 None 59 Rat Binding pIC50 = 4.6 4.6 -16 29
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
42 2063 None 57 Rat Binding pIC50 = 4.6 4.6 -1778 18
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
56971 2063 None 57 Rat Binding pIC50 = 4.6 4.6 -1778 18
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
CHEMBL8412 2063 None 57 Rat Binding pIC50 = 4.6 4.6 -1778 18
Binding affinity towards 5-HT1B was determinedBinding affinity towards 5-HT1B was determined
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00384a001
10546537 120026 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 361 6 2 2 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(=O)NCc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL350277 120026 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 361 6 2 2 3.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC(=O)NCc4ccccc4)cc32)C1 10.1021/jm000956k
10519608 193428 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 318 4 0 4 3.2 c1ccc(CN2CCN(c3ncccc3-n3cccc3)CC2)cc1 10.1021/jm960501o
CHEMBL52612 193428 None 0 Rat Binding pIC50 = 4.6 4.6 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 318 4 0 4 3.2 c1ccc(CN2CCN(c3ncccc3-n3cccc3)CC2)cc1 10.1021/jm960501o
2274 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917.0 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 None 58 Rat Binding pIC50 = 5.6 5.6 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
10838188 167617 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 472 4 2 5 4.2 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C#N)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL430122 167617 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
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 472 4 2 5 4.2 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C#N)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10781299 11676 None 7 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%
ChEMBL 194 1 1 2 2.1 Clc1ccc(C2=CCNCC2)cn1 10.1016/s0960-894x(99)00575-2
CHEMBL1181152 11676 None 7 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%
ChEMBL 194 1 1 2 2.1 Clc1ccc(C2=CCNCC2)cn1 10.1016/s0960-894x(99)00575-2
CHEMBL157110 11676 None 7 Rat Binding pIC50 = 5.6 5.6 - 0
Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%Inhibition of [3H]-5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatum; Residual radioligand binding higher than 50%
ChEMBL 194 1 1 2 2.1 Clc1ccc(C2=CCNCC2)cn1 10.1016/s0960-894x(99)00575-2
19956256 115298 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against 5-hydroxytryptamine 1B receptorCompound was tested for binding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C 10.1016/s0960-894x(00)00691-0
CHEMBL334923 115298 None 0 Human Binding pIC50 = 5.6 5.6 - 0
Compound was tested for binding affinity against 5-hydroxytryptamine 1B receptorCompound was tested for binding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 275 4 0 5 2.5 Cc1csc2c1-n1cccc1/C2=N/OCCN(C)C 10.1016/s0960-894x(00)00691-0
44341707 9464 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 464 9 2 6 4.0 CN(CC1CCCCC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL111899 9464 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 464 9 2 6 4.0 CN(CC1CCCCC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
15516681 10202 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 422 9 2 6 2.9 CN(CC1CC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL115989 10202 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 422 9 2 6 2.9 CN(CC1CC1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
2543 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
5358 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
5358.0 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
54 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
CHEMBL128 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
DB00669 3707 None 68 Human Binding pIC50 = 7.6 7.6 -3 32
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 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/jm9704560
10596566 56569 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 390 7 1 6 3.1 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm980569z
CHEMBL164111 56569 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 390 7 1 6 3.1 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm980569z
10765655 114446 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL333341 114446 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
115 3791 None 80 Rat Binding pIC50 = 7.6 7.6 1 27
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 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
4296 3791 None 80 Rat Binding pIC50 = 7.6 7.6 1 27
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 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
CHEMBL274866 3791 None 80 Rat Binding pIC50 = 7.6 7.6 1 27
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 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
10526642 169273 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 430 9 3 6 2.9 OC[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL441296 169273 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 430 9 3 6 2.9 OC[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10838030 23507 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 468 8 0 5 4.7 CCCN1CCCC12COc1cccc(OCCCCN3C(=O)CC4(CCCC4)CC3=O)c1C2 10.1021/jm950861w
CHEMBL133375 23507 None 0 Rat Binding pIC50 = 5.6 5.6 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 468 8 0 5 4.7 CCCN1CCCC12COc1cccc(OCCCCN3C(=O)CC4(CCCC4)CC3=O)c1C2 10.1021/jm950861w
2812 4779 None 101 Rat Binding pIC50 = 4.6 4.6 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 None 101 Rat Binding pIC50 = 4.6 4.6 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
10596387 168459 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL435060 168459 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10805740 89274 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 321 5 2 3 2.0 CNS(=O)(=O)Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
CHEMBL2368259 89274 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 321 5 2 3 2.0 CNS(=O)(=O)Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
277 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913.0 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 None 62 Rat Binding pIC50 = 5.6 5.6 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
10765655 114446 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
CHEMBL333341 114446 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
10468938 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL116092 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10468938 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL116092 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
10468938 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9910021
CHEMBL116092 10244 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9910021
10812465 35531 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 2 5 4.2 c1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL143893 35531 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 2 5 4.2 c1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10551328 203721 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL67684 203721 None 0 Human Binding pIC50 = 7.6 7.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
10718277 203262 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL64610 203262 None 0 Rat Binding pIC50 = 6.6 6.6 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 447 6 0 4 4.2 CN1C(=O)COc2cc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
9930155 164032 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420874 164032 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
10836850 40277 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 440 7 2 5 4.4 c1ccc2c(c1)CCC2NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL148095 40277 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 440 7 2 5 4.4 c1ccc2c(c1)CCC2NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10766570 203380 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
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 None 0 Human Binding pIC50 = 6.6 6.6 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1 10.1021/jm981133m
9866484 56278 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 414 7 1 5 3.0 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
CHEMBL162899 56278 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 414 7 1 5 3.0 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
11798502 56493 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 468 7 1 5 4.5 FC(F)(F)c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL163376 56493 None 0 Human Binding pIC50 = 6.6 6.6 - 0
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 468 7 1 5 4.5 FC(F)(F)c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
73351903 89695 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376484 89695 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 360 3 2 4 3.1 Cc1[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
5 139 None 72 Human Binding pIC50 = 7.5 7.5 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 None 72 Human Binding pIC50 = 7.5 7.5 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 None 72 Human Binding pIC50 = 7.5 7.5 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 None 72 Human Binding pIC50 = 7.5 7.5 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
15951337 125387 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 338 4 2 3 3.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12 nan
CHEMBL3645476 125387 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 338 4 2 3 3.9 CN1CCC[C@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12 nan
CHEMBL1200558 208599 None 21 Rat Binding pIC50 = 5.5 5.5 - 1
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL None None None CC[C@H](C)[C@H](N)C1=N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H]2CCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H](CCCN)NC2=O)[C@@H](C)CC)CS1 nan
10550857 203446 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 Fc1ccccc1CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL65824 203446 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 Fc1ccccc1CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
2763724 98477 None 64 Rat Binding pIC50 = 8.5 8.5 - 1
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 276 1 2 1 3.3 Brc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL27592 98477 None 64 Rat Binding pIC50 = 8.5 8.5 - 1
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 276 1 2 1 3.3 Brc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
10573904 121308 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.9 c1ccc(NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm9910021
CHEMBL358072 121308 None 0 Human Binding pIC50 = 8.5 8.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.9 c1ccc(NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm9910021
3050532 99447 None 7 Rat Binding pIC50 = 8.5 8.5 - 1
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 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL282994 99447 None 7 Rat Binding pIC50 = 8.5 8.5 - 1
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 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
53263 99495 None 17 Rat Binding pIC50 = 8.5 8.5 - 1
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 243 2 2 3 2.5 O=[N+]([O-])c1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL283257 99495 None 17 Rat Binding pIC50 = 8.5 8.5 - 1
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 243 2 2 3 2.5 O=[N+]([O-])c1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
2761023 98766 None 71 Rat Binding pIC50 = 8.4 8.4 - 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1021/jm00170a007
CHEMBL2011570 98766 None 71 Rat Binding pIC50 = 8.4 8.4 - 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1021/jm00170a007
CHEMBL27811 98766 None 71 Rat Binding pIC50 = 8.4 8.4 - 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 198 1 2 1 2.5 C1=C(c2c[nH]c3ccccc23)CCNC1 10.1021/jm00170a007
44341625 111317 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 501 10 4 7 3.3 CC(=O)Nc1ccc(CNCC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1016/s0960-894x(99)00614-9
CHEMBL326723 111317 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 501 10 4 7 3.3 CC(=O)Nc1ccc(CNCC2(O)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1016/s0960-894x(99)00614-9
10477461 113393 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 424 9 2 6 3.1 CC(C)CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL331819 113393 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 424 9 2 6 3.1 CC(C)CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
73453 29616 None 24 Rat Binding pIC50 = 7.5 7.5 -26 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29616 None 24 Rat Binding pIC50 = 7.5 7.5 -26 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
10468938 10244 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL116092 10244 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
10468938 10244 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704560
CHEMBL116092 10244 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704560
9821397 100921 None 21 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL293923 100921 None 21 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 383 5 0 6 3.0 COc1ccccc1N1CCN(CCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
10759541 200154 None 1 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 339 4 1 5 3.4 Oc1nc2ccc(CCN3CCN(c4ccccc4)CC3)cc2s1 10.1021/jm970298c
CHEMBL59637 200154 None 1 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 339 4 1 5 3.4 Oc1nc2ccc(CCN3CCN(c4ccccc4)CC3)cc2s1 10.1021/jm970298c
10501785 202728 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL61819 202728 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 411 7 0 6 3.8 COc1ccccc1N1CCN(CCCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
10625376 52451 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 505 5 3 4 4.7 CN1CCC2(CC1)COc1ccc(NC(=O)NCCN3CCC(c4c[nH]c5cc(F)ccc45)CC3)cc12 10.1021/jm9811054
CHEMBL15909 52451 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
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 505 5 3 4 4.7 CN1CCC2(CC1)COc1ccc(NC(=O)NCCN3CCC(c4c[nH]c5cc(F)ccc45)CC3)cc12 10.1021/jm9811054
44364110 35535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 456 7 3 6 3.4 O[C@H]1Cc2ccccc2C1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL143894 35535 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 456 7 3 6 3.4 O[C@H]1Cc2ccccc2C1NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
71461714 79648 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 500 8 2 5 4.9 F[C@@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F 10.1021/jm981133m
CHEMBL2115111 79648 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 500 8 2 5 4.9 F[C@@H]1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC[C@@H]1NCc1ccccc1C(F)(F)F 10.1021/jm981133m
10809238 201141 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21 10.1021/jm970298c
CHEMBL60318 201141 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 371 4 0 5 3.1 Cn1c(=O)sc2cc(CCN3CCN(c4ccc(F)cc4)CC3)ccc21 10.1021/jm970298c
10319624 98987 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL27991 98987 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL298534 98987 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 10 1 4 4.1 CCCN(CCCCNC(=O)c1ccc(F)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10070029 165417 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL423841 165417 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL54089 165417 None 0 Rat Binding pIC50 = 5.5 5.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 408 8 0 5 3.4 CCCN(CCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10812693 102753 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 433 8 1 5 4.3 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL305062 102753 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 433 8 1 5 4.3 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
10251234 11245 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1178932 11245 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50530 11245 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 414 9 0 5 3.3 CCCN(CCCCN1C(=O)C2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10092409 12046 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL1183479 12046 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL299561 12046 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 400 9 0 4 3.7 CCCN(CCCCN1CC2CCCC2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10047322 97140 None 0 Rat Binding pIC50 = 4.5 4.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL26783 97140 None 0 Rat Binding pIC50 = 4.5 4.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
CHEMBL50993 97140 None 0 Rat Binding pIC50 = 4.5 4.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 412 8 0 4 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2ccccc2C1 10.1021/jm00038a007
11743327 98702 None 0 Rat Binding pIC50 = 4.5 4.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
CHEMBL27763 98702 None 0 Rat Binding pIC50 = 4.5 4.5 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 428 8 1 5 3.9 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(O)c2C1 10.1021/jm00038a007
10265863 193324 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
CHEMBL52438 193324 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 283 5 0 2 4.3 CCCN(CCC)C1COc2ccc3ccccc3c2C1 10.1021/jm00038a007
6761 67799 None 19 Rat Binding pIC50 = 5.5 5.5 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 None 19 Rat Binding pIC50 = 5.5 5.5 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
10409556 162372 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
CHEMBL416523 162372 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 414 8 1 5 3.3 COc1cccc2c1CC(CNCCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
10614906 110505 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL324931 110505 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
11796807 165543 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 428 9 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL424154 165543 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 428 9 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1)c1ccccc1 10.1021/jm9805687
9949172 10873 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL117249 10873 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
11794853 203075 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3ccsc3n2c1 10.1021/jm950543x
CHEMBL63790 203075 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3ccsc3n2c1 10.1021/jm950543x
10499348 201364 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 369 4 1 6 2.7 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4O)CC3)ccc21 10.1021/jm970298c
CHEMBL60447 201364 None 0 Rat Binding pIC50 = 7.5 7.5 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 369 4 1 6 2.7 Cn1c(=O)sc2cc(CCN3CCN(c4ccccc4O)CC3)ccc21 10.1021/jm970298c
15951272 125386 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 338 4 2 3 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12 nan
CHEMBL3645475 125386 None 0 Rat Binding pIC50 = 6.5 6.5 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 338 4 2 3 3.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(/N=C(\N)c3cccs3)cc12 nan
10614906 110505 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
CHEMBL324931 110505 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
10600213 203109 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
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 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
3066250 70286 None 2 Rat Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
CHEMBL194305 70286 None 2 Rat Binding pIC50 = 6.5 6.5 - 0
Inhibitory activity against 5-hydroxytryptamine 1B receptor in ratInhibitory activity against 5-hydroxytryptamine 1B receptor in rat
ChEMBL 242 2 2 2 2.9 COc1ccc2[nH]c(C)c(C3=CCNCC3)c2c1 10.1016/j.bmcl.2005.06.067
9911120 9623 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 9623 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
10617665 52762 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 347 5 2 2 3.9 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(=O)NCc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL159470 52762 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 347 5 2 2 3.9 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(=O)NCc4ccccc4)cc32)C1 10.1021/jm000956k
44267852 11195 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2c(ccc3ccccc23)O1 10.1021/jm00401a007
CHEMBL11787 11195 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2c(ccc3ccccc23)O1 10.1021/jm00401a007
10714457 101716 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 374 4 0 4 3.9 Fc1ccc(CN2CCN(Cc3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL299524 101716 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 374 4 0 4 3.9 Fc1ccc(CN2CCN(Cc3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
1971 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543.0 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 None 38 Rat Binding pIC50 = 5.5 5.5 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
11668825 9591 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 415 7 2 5 3.8 OC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL112507 9591 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 415 7 2 5 3.8 OC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
10501944 11037 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL117579 11037 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
18691566 89271 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 299 4 3 3 2.3 CN[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2368256 89271 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 299 4 3 3 2.3 CN[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10571716 40494 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 378 8 1 5 3.3 C=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL148286 40494 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 378 8 1 5 3.3 C=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
969502 98111 None 4 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm00401a007
CHEMBL1314789 98111 None 4 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm00401a007
CHEMBL273490 98111 None 4 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 356 2 0 4 4.4 CSc1ccc2c(c1)[C@H](N1CCN(C)CC1)Cc1ccccc1S2 10.1021/jm00401a007
10689227 55817 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 350 8 2 5 2.4 C=CCNC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL162296 55817 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 350 8 2 5 2.4 C=CCNC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10501944 11037 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
CHEMBL117579 11037 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
10693206 55162 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 415 9 1 5 4.2 c1ccc(COC[C@@H]2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL161735 55162 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 415 9 1 5 4.2 c1ccc(COC[C@@H]2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
109 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm950543x
2689 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm950543x
CHEMBL27403 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm950543x
109 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm960501o
2689 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm960501o
CHEMBL27403 902 None 31 Rat Binding pIC50 = 6.5 6.5 - 7
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm960501o
11796209 203388 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1Cl 10.1021/jm950543x
CHEMBL65413 203388 None 0 Rat Binding pIC50 = 4.5 4.5 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1Cl 10.1021/jm950543x
10766320 38293 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.7 OC[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146265 38293 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.7 OC[C@@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
44341783 10099 None 1 Human Binding pIC50 = 6.5 6.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 454 7 3 7 3.0 CC(C)(C)OC(=O)NCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL115496 10099 None 1 Human Binding pIC50 = 6.5 6.5 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 454 7 3 7 3.0 CC(C)(C)OC(=O)NCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
49836386 18550 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
CHEMBL1275709 18550 None 0 Human Binding pIC50 = 6.5 6.5 - 0
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 253 2 1 2 3.2 CN(C)[C@@H]1CC[C@H](c2c[nH]c3ccc(C#N)cc23)C1 10.1021/jm100515z
31703 194717 None 63 Rat Binding pIC50 = 4.5 4.5 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL359744 194717 None 63 Rat Binding pIC50 = 4.5 4.5 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL53463 194717 None 63 Rat Binding pIC50 = 4.5 4.5 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
10764998 113489 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
CHEMBL331970 113489 None 0 Human Binding pIC50 = 7.5 7.5 - 0
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 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
10502988 38012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 434 8 1 6 4.3 CN(Cc1ccsc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146024 38012 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 434 8 1 6 4.3 CN(Cc1ccsc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10764998 113489 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL331970 113489 None 0 Human Binding pIC50 = 7.5 7.5 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10838622 38164 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 485 9 3 6 4.5 CC(=O)Nc1ccc([C@@H](C)NC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146150 38164 None 0 Human Binding pIC50 = 6.5 6.5 - 0
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 485 9 3 6 4.5 CC(=O)Nc1ccc([C@@H](C)NC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
44296810 161994 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 404 7 0 7 3.3 COc1ccc2c(c1)nc(N1CCN(CCCCn3cccn3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL415933 161994 None 0 Rat Binding pIC50 = 5.5 5.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 404 7 0 7 3.3 COc1ccc2c(c1)nc(N1CCN(CCCCn3cccn3)CC1)c1cccn12 10.1021/jm960501o
44267205 98409 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 366 5 0 4 3.6 CCCN1CCN(Cc2ccccc2)CC12COc1cccc(OC)c1C2 10.1016/0960-894X(96)00174-6
CHEMBL275481 98409 None 0 Human Binding pIC50 = 4.5 4.5 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 366 5 0 4 3.6 CCCN1CCN(Cc2ccccc2)CC12COc1cccc(OC)c1C2 10.1016/0960-894X(96)00174-6
11005810 10466 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
CHEMBL116463 10466 None 0 Human Binding pIC50 = 5.5 5.5 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 517 10 1 4 6.2 N#Cc1ccc(CCOC(=O)NC2CCN(CCCC(c3ccc(F)cc3)c3ccc(F)cc3)CC2)cc1 10.1021/jm010878g
26987 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
26987.0 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 None 33 Rat Binding pIC50 = 6.5 6.5 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
10548444 56913 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 390 7 2 6 2.2 c1c[nH]c(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)n1 10.1021/jm980569z
CHEMBL164413 56913 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 390 7 2 6 2.2 c1c[nH]c(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)n1 10.1021/jm980569z
10644514 101057 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 397 6 0 6 3.4 COc1ccccc1N1CCN(CCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
CHEMBL294730 101057 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 397 6 0 6 3.4 COc1ccccc1N1CCN(CCCc2ccc3c(c2)sc(=O)n3C)CC1 10.1021/jm970298c
18975338 102617 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 416 7 2 6 2.5 OC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(Cc2ccccc2)CC1 10.1021/jm981133m
CHEMBL304197 102617 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 416 7 2 6 2.5 OC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(Cc2ccccc2)CC1 10.1021/jm981133m
10386282 164100 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm980569z
CHEMBL420965 164100 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm980569z
376254 118504 None 2 Rat Binding pIC50 = 6.4 6.4 - 1
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 284 1 0 4 2.4 CN1CCN(c2nc3cc(F)ccc3n3cccc23)CC1 10.1021/jm970376w
CHEMBL341474 118504 None 2 Rat Binding pIC50 = 6.4 6.4 - 1
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 284 1 0 4 2.4 CN1CCN(c2nc3cc(F)ccc3n3cccc23)CC1 10.1021/jm970376w
180 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160.0 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 None 56 Rat Binding pIC50 = 5.4 5.4 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
10600212 102713 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1F 10.1021/jm981133m
CHEMBL304833 102713 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1F 10.1021/jm981133m
173 3262 None 95 Rat Binding pIC50 = 6.4 6.4 -2 23
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970376w
5011 3262 None 95 Rat Binding pIC50 = 6.4 6.4 -2 23
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970376w
CHEMBL18772 3262 None 95 Rat Binding pIC50 = 6.4 6.4 -2 23
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970376w
9911120 9623 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
CHEMBL11265 9623 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1021/jm950861w
10835403 26416 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 410 5 0 4 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCCC12COc1ccccc1C2 10.1021/jm950861w
CHEMBL135952 26416 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 410 5 0 4 3.9 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCCC12COc1ccccc1C2 10.1021/jm950861w
1220 187 None 55 Rat Binding pIC50 = 5.4 5.4 -7413 44
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00401a007
31 187 None 55 Rat Binding pIC50 = 5.4 5.4 -7413 44
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00401a007
7 187 None 55 Rat Binding pIC50 = 5.4 5.4 -7413 44
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00401a007
CHEMBL56 187 None 55 Rat Binding pIC50 = 5.4 5.4 -7413 44
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00401a007
10665840 89275 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 354 4 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)NC(C)(C)C4=O)cc32)C1 10.1021/jm000956k
CHEMBL2368260 89275 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 354 4 2 3 2.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)NC(C)(C)C4=O)cc32)C1 10.1021/jm000956k
9911120 9623 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
CHEMBL11265 9623 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
10546440 194915 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 360 3 0 4 3.9 Fc1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL54125 194915 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 360 3 0 4 3.9 Fc1ccc(CN2CCN(c3nc4ccccc4n4cccc34)CC2)cc1 10.1021/jm960501o
10852406 52840 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 309 4 2 3 3.0 Cc1nc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n[nH]1 10.1021/jm000956k
CHEMBL159536 52840 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 309 4 2 3 3.0 Cc1nc(Cc2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n[nH]1 10.1021/jm000956k
10502669 56561 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 428 8 2 5 4.1 CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL164046 56561 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 428 8 2 5 4.1 CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10764284 55434 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 414 7 1 5 3.0 O=C1CN(Cc2ccccc2)CCN1CCCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
CHEMBL161969 55434 None 0 Human Binding pIC50 = 5.4 5.4 - 0
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 414 7 1 5 3.0 O=C1CN(Cc2ccccc2)CCN1CCCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
13673326 16414 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccc3ccccc3c2O1 10.1021/jm00401a007
CHEMBL12311 16414 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 436 7 1 5 4.1 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccc3ccccc3c2O1 10.1021/jm00401a007
23374587 54572 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 267 4 1 4 2.0 c1cc2[nH]cc(CCN3CCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL161045 54572 None 0 Human Binding pIC50 = 8.4 8.4 - 0
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 267 4 1 4 2.0 c1cc2[nH]cc(CCN3CCC3)c2cc1-n1cnnc1 10.1021/jm9805687
5 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
5202 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
CHEMBL39 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
DB08839 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptorInhibition of radiolabeled [3H]-5-HT ligand binding to 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970376w
5 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternolDisplacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5202 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternolDisplacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
CHEMBL39 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternolDisplacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
DB08839 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternolDisplacement of [125I]CYP from rat cerebral cortex 5-HT1B receptor in the presence of isoproternol
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.03.006
5 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting methodDisplacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
5202 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting methodDisplacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
CHEMBL39 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting methodDisplacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
DB08839 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Displacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting methodDisplacement of [125I]CYP from rat cerebral cortex 5HT1B receptor measured after 120 mins by scintillation counting method
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.bmc.2016.11.014
10768115 119725 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 513 9 2 6 4.1 CC(=O)Nc1ccc(C(=O)N(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL347570 119725 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 513 9 2 6 4.1 CC(=O)Nc1ccc(C(=O)N(C)CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10789000 203318 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
CHEMBL64845 203318 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 435 6 1 5 5.2 Oc1nc2ccc(CCCCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
10251673 99490 None 0 Rat Binding pIC50 = 6.4 6.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283207 99490 None 0 Rat Binding pIC50 = 6.4 6.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL52396 99490 None 0 Rat Binding pIC50 = 6.4 6.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 422 9 0 5 3.8 CCCN(CCCCN1C(=O)c2ccccc2C1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10646959 40115 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL147961 40115 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10321248 99426 None 0 Rat Binding pIC50 = 4.4 4.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL28287 99426 None 0 Rat Binding pIC50 = 4.4 4.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL50722 99426 None 0 Rat Binding pIC50 = 4.4 4.4 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 444 9 0 6 3.7 CCCN(CCCON1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
2726 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Rat Binding pIC50 = 5.4 5.4 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
10719857 202943 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 363 3 0 4 4.0 C[N+]1(Cc2ccccc2)CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL62911 202943 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 363 3 0 4 4.0 C[N+]1(Cc2ccccc2)CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
2393 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
5078 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
5078.0 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
51 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
CHEMBL905 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
DB00953 3334 None 82 Human Binding pIC50 = 7.4 7.4 -1 5
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 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
10693140 53079 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 414 8 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL159759 53079 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 414 8 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
11795644 40433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 406 8 1 5 4.0 CC(C)=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL148233 40433 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 406 8 1 5 4.0 CC(C)=CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10552243 39969 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 468 7 1 5 5.4 c1ccc(C2CCCCN2C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL147838 39969 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 468 7 1 5 5.4 c1ccc(C2CCCCN2C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10756517 189173 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL51118 189173 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1 10.1021/jm950543x
10756517 189173 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1 10.1021/jm960501o
CHEMBL51118 189173 None 0 Rat Binding pIC50 = 6.4 6.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3sccc3n3cccc23)CC1 10.1021/jm960501o
10550488 35655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL144002 35655 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cncn4)cc23)CC1)c1ccccc1 10.1021/jm9910021
161 754 None 6 Rat Binding pIC50 = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 754 None 6 Rat Binding pIC50 = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 754 None 6 Rat Binding pIC50 = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
10811876 102128 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1Cl 10.1021/jm950543x
CHEMBL302431 102128 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)cc1Cl 10.1021/jm950543x
9949172 10873 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
CHEMBL117249 10873 None 0 Human Binding pIC50 = 6.4 6.4 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704560
10498554 194945 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 357 3 0 5 3.5 Cc1ccnc2c1nc(N1CCN(Cc3ccccc3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL54246 194945 None 0 Rat Binding pIC50 = 4.4 4.4 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 357 3 0 5 3.5 Cc1ccnc2c1nc(N1CCN(Cc3ccccc3)CC1)c1cccn12 10.1021/jm960501o
10539089 51958 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 257 3 2 2 2.1 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(N)=O)cc32)C1 10.1021/jm000956k
CHEMBL158638 51958 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 257 3 2 2 2.1 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(C(N)=O)cc32)C1 10.1021/jm000956k
15222791 28560 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 219 1 1 3 1.8 COc1cccc2c1CC1(CCCN1)CO2 10.1021/jm950861w
CHEMBL137643 28560 None 0 Rat Binding pIC50 = 5.4 5.4 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 219 1 1 3 1.8 COc1cccc2c1CC1(CCCN1)CO2 10.1021/jm950861w
10574570 56232 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 428 8 1 5 4.1 CC(CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm980569z
CHEMBL162722 56232 None 0 Human Binding pIC50 = 7.4 7.4 - 0
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 428 8 1 5 4.1 CC(CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm980569z
10719203 38379 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 9 3 6 3.9 CC(=O)Nc1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146335 38379 None 0 Human Binding pIC50 = 7.4 7.4 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 9 3 6 3.9 CC(=O)Nc1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10505438 56355 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 496 9 1 8 3.9 Cc1noc(-c2ccc(CCN3CCN(CCCc4c[nH]c5ccc(-n6cnnc6)cc45)CC3)cc2)n1 10.1021/jm980569z
CHEMBL163114 56355 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 496 9 1 8 3.9 Cc1noc(-c2ccc(CCN3CCN(CCCc4c[nH]c5ccc(-n6cnnc6)cc45)CC3)cc2)n1 10.1021/jm980569z
10788207 200767 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 419 4 0 4 3.4 CN1C(=O)COc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL60047 200767 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 419 4 0 4 3.4 CN1C(=O)COc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
10552573 38141 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 476 10 4 5 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCCN4CCC(N[C@@H](CO)c5ccccc5)CC4)c3c2)CO1 10.1021/jm9910021
CHEMBL146129 38141 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 476 10 4 5 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCCN4CCC(N[C@@H](CO)c5ccccc5)CC4)c3c2)CO1 10.1021/jm9910021
10764757 44027 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 423 6 4 5 3.0 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(O)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15139 44027 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 423 6 4 5 3.0 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(O)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
10645615 101001 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)c(Cl)c1 10.1021/jm950543x
CHEMBL294368 101001 None 0 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4ccsc4n4cccc34)CC2)c(Cl)c1 10.1021/jm950543x
11647963 110898 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 444 9 3 6 3.3 OC1(CNCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL326125 110898 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 444 9 3 6 3.3 OC1(CNCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
10386282 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL420965 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10386282 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420965 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
10811007 53145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL159819 53145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10386282 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL420965 164100 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10503731 10289 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.8 Fc1cc(F)cc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9704560
CHEMBL116153 10289 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.8 Fc1cc(F)cc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm9704560
3117 207841 None 103 Rat Binding pIC50 = 5.3 5.3 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 None 103 Rat Binding pIC50 = 5.3 5.3 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
10644749 119984 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 401 8 2 6 2.8 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)nc1 10.1021/jm9805687
CHEMBL349893 119984 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 401 8 2 6 2.8 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)nc1 10.1021/jm9805687
10527882 35593 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 9 3 6 3.9 C[C@@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL143947 35593 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 9 3 6 3.9 C[C@@H](O)[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
21138 98451 None 39 Rat Binding pIC50 = 6.3 6.3 -162 7
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 10.1021/jm00401a007
CHEMBL275742 98451 None 39 Rat Binding pIC50 = 6.3 6.3 -162 7
Binding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligandBinding affinity against 5-HT1B receptor in rat frontal cortex using [3H]-5-HT in presence of 0.1 uM [3H]-8-OH-DPAT as a radioligand
ChEMBL 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 10.1021/jm00401a007
10548259 188223 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 387 3 0 7 2.9 c1cnc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12 10.1021/jm960501o
CHEMBL49932 188223 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 387 3 0 7 2.9 c1cnc2c(c1)nc(N1CCN(Cc3ccc4c(c3)OCO4)CC1)c1cccn12 10.1021/jm960501o
10252256 52777 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
CHEMBL159483 52777 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
10252256 52777 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
CHEMBL159483 52777 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
11797644 53423 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL160070 53423 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1 10.1021/jm9805687
10812592 100884 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 431 8 1 4 5.1 FC1(CCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL293678 100884 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 431 8 1 4 5.1 FC1(CCc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
15951342 125388 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 324 3 2 3 3.7 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)C1 nan
CHEMBL3645479 125388 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).Binding Assay: 5-HT1D binding assays (agonist radioligand)were performed using bovine caudate membranes according to the methods of Heuring and Peroutka (J. Neurosci 1987, 7: 894-903). 5-HT1B (rat cerebral cortex) binding assays (agonist radioligand) were performed according to the method of Hoyer et. al. (Eur. J. Pharmacol. 1995, 118: 1-12).
ChEMBL 324 3 2 3 3.7 CN1CCC(c2c[nH]c3ccc(/N=C(\N)c4cccs4)cc23)C1 nan
5 139 None 72 Human Binding pIC50 = 8.3 8.3 -11 54
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
5202 139 None 72 Human Binding pIC50 = 8.3 8.3 -11 54
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
CHEMBL39 139 None 72 Human Binding pIC50 = 8.3 8.3 -11 54
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
DB08839 139 None 72 Human Binding pIC50 = 8.3 8.3 -11 54
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00101a032
5 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
5202 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL39 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
DB08839 139 None 72 Rat Binding pIC50 = 8.3 8.3 -13 54
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT as the radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
10670534 203436 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 Fc1cccc(CC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL65765 203436 None 0 Human Binding pIC50 = 8.3 8.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 435 7 1 4 4.9 Fc1cccc(CC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
11797644 53423 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL160070 53423 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 446 9 3 4 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4)cc23)C1)c1ccccc1 10.1021/jm9805687
10811007 53145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL159819 53145 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
9824884 51859 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 447 4 2 4 4.3 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15855 51859 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 447 4 2 4 4.3 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10412190 52918 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cccc(F)c34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15961 52918 None 0 Rat Binding pIC50 = 7.3 7.3 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cccc(F)c34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
49836496 18555 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
CHEMBL1275791 18555 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 246 2 1 1 3.5 CN(C)[C@H]1CC[C@@H](c2c[nH]c3ccc(F)cc23)C1 10.1021/jm100515z
121852 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5.3 5.3 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
4223 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
6918314.0 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
7427 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
CHEMBL439849 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
DB06684 3992 None 94 Rat Binding pIC50 = 5.3 5.3 - 3
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.1021/jm040793q
42 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
56971 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
CHEMBL8412 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00038a007
10338595 162499 None 0 Rat Binding pIC50 = 4.3 4.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL416747 162499 None 0 Rat Binding pIC50 = 4.3 4.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 360 9 0 4 4.0 CCCN(CCCCN1CCCCC1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
42 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
56971 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
CHEMBL8412 2063 None 57 Rat Binding pIC50 = 4.3 4.3 -1778 18
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm950861w
23786480 15263 None 2 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@@H]1COc2ccccc2O1 10.1021/jm00401a007
CHEMBL12124 15263 None 2 Rat Binding pIC50 = 5.3 5.3 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@@H]1COc2ccccc2O1 10.1021/jm00401a007
121852 10166 None 7 Human Binding pIC50 = 5.3 5.3 - 1
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL11592 10166 None 7 Human Binding pIC50 = 5.3 5.3 - 1
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL301060 10166 None 7 Human Binding pIC50 = 5.3 5.3 - 1
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
115 3791 None 80 Rat Binding pIC50 = 7.3 7.3 1 27
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00123a039
4296 3791 None 80 Rat Binding pIC50 = 7.3 7.3 1 27
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00123a039
CHEMBL274866 3791 None 80 Rat Binding pIC50 = 7.3 7.3 1 27
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00123a039
3082597 99559 None 8 Rat Binding pIC50 = 6.3 6.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL283606 99559 None 8 Rat Binding pIC50 = 6.3 6.3 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 263 6 0 3 3.1 CCCN(CCC)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10759465 164895 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 338 6 1 5 2.3 CN1CCN(CCCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL422191 164895 None 0 Human Binding pIC50 = 5.3 5.3 - 0
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 338 6 1 5 2.3 CN1CCN(CCCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10527884 28374 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
CHEMBL137486 28374 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 458 8 1 5 3.9 COc1cccc2c1CC1(CCCCN1CCCCNS(=O)(=O)c1ccc(C)cc1)CO2 10.1021/jm950861w
10551525 100670 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1ccccc1CCN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL292262 100670 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1ccccc1CCN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
10618751 35190 None 0 Human Binding pIC50 = 6.3 6.3 -4 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
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 None 0 Human Binding pIC50 = 6.3 6.3 -4 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10623434 102312 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1ccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL303514 102312 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1ccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
44341637 9601 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 445 9 3 7 2.7 OC1(CNCc2ccccn2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL112558 9601 None 0 Human Binding pIC50 = 7.3 7.3 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 445 9 3 7 2.7 OC1(CNCc2ccccn2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
44214559 56498 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163462 56498 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
145 140 None 49 Human Binding pIC50 = 6.3 6.3 -8 30
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00101a032
1832 140 None 49 Human Binding pIC50 = 6.3 6.3 -8 30
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00101a032
CHEMBL7257 140 None 49 Human Binding pIC50 = 6.3 6.3 -8 30
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00101a032
DB14010 140 None 49 Human Binding pIC50 = 6.3 6.3 -8 30
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00101a032
3081681 98514 None 4 Rat Binding pIC50 = 5.3 5.3 - 0
compound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissuecompound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
CHEMBL276175 98514 None 4 Rat Binding pIC50 = 5.3 5.3 - 0
compound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissuecompound was measured for affinity against 5-hydroxytryptamine 1B receptor labelled with [3H]5-HT radioligand in striatum tissue
ChEMBL 442 6 0 7 3.4 O=C1CC2(CCCC2)CC(=O)N1OCCCN1CCN(c2nsc3ccccc23)CC1 10.1021/jm00107a028
9890331 56367 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 457 8 2 6 3.5 CC(=O)Nc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL163127 56367 None 0 Human Binding pIC50 = 7.3 7.3 - 0
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 457 8 2 6 3.5 CC(=O)Nc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
18366015 78372 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2110300 78372 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 313 4 2 3 2.6 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10666301 193436 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 361 3 0 5 3.3 Fc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL52625 193436 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 361 3 0 5 3.3 Fc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)cc1 10.1021/jm960501o
10646633 51282 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 437 3 2 4 3.7 COc1ccc(NC(=O)N2CCc3[nH]c4ccc(F)cc4c3C2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15808 51282 None 0 Rat Binding pIC50 = 6.3 6.3 - 0
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 437 3 2 4 3.7 COc1ccc(NC(=O)N2CCc3[nH]c4ccc(F)cc4c3C2)cc1N1CCN(C)CC1 10.1021/jm9811054
44344504 112832 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL330803 112832 None 0 Human Binding pIC50 = 6.3 6.3 - 0
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 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
44341657 113057 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 408 9 3 6 2.5 OC1(CNCC2CC2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL331143 113057 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 408 9 3 6 2.5 OC1(CNCC2CC2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
73347307 89698 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376487 89698 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 257 2 2 3 2.8 Cc1[nH]c2ccc([N+](=O)[O-])cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
44344504 112832 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL330803 112832 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
10834908 52665 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 401 8 1 5 4.0 c1ccc(COC[C@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
CHEMBL159381 52665 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 401 8 1 5 4.0 c1ccc(COC[C@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
11796808 53053 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 428 9 1 5 3.8 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
CHEMBL159733 53053 None 0 Human Binding pIC50 = 6.2 6.2 - 0
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 428 9 1 5 3.8 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
10590206 202803 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL62274 202803 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 0 5 2.9 C=CCN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
10646873 38448 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 2 5 4.7 C[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146391 38448 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 9 2 5 4.7 C[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10105889 24183 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm00101a032
CHEMBL133939 24183 None 1 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@@H]3CCCN3C)c2c1 10.1021/jm00101a032
10694810 203767 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(CCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL68019 203767 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 449 8 1 4 5.3 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(CCc2ccccc2)CC1 10.1021/jm981133m
11797241 194354 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 437 3 0 7 4.1 c1cnc2ccc3nc(N4CCN(Cc5ccc6c(c5)OCO6)CC4)c4cccn4c3c2c1 10.1021/jm960501o
CHEMBL52867 194354 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 437 3 0 7 4.1 c1cnc2ccc3nc(N4CCN(Cc5ccc6c(c5)OCO6)CC4)c4cccn4c3c2c1 10.1021/jm960501o
10741528 55111 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 434 7 1 5 4.2 Clc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL161696 55111 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 434 7 1 5 4.2 Clc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10836301 52964 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 428 9 1 5 4.1 CN(Cc1ccccc1)C[C@@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL159650 52964 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 428 9 1 5 4.1 CN(Cc1ccccc1)C[C@@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
108029 3414 None 57 Rat Binding pIC50 = 8.2 8.2 -3 13
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.ejmech.2013.03.006
23 3414 None 57 Rat Binding pIC50 = 8.2 8.2 -3 13
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL18785 3414 None 57 Rat Binding pIC50 = 8.2 8.2 -3 13
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1016/j.ejmech.2013.03.006
2869 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
60 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
60857 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
60857.0 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
CHEMBL1185 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
DB00315 4152 None 89 Human Binding pIC50 = 8.2 8.2 -8 7
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 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
10528410 39382 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 8 2 5 4.6 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
CHEMBL147148 39382 None 0 Human Binding pIC50 = 8.2 8.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 471 8 2 5 4.6 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
10624680 122018 None 17 Rat Binding pIC50 = 8.2 8.2 - 0
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 483 5 2 7 4.7 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1 10.1021/jm990397l
CHEMBL359447 122018 None 17 Rat Binding pIC50 = 8.2 8.2 - 0
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 483 5 2 7 4.7 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1 10.1021/jm990397l
5 139 None 72 Human Binding pIC50 = 8.2 8.2 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 None 72 Human Binding pIC50 = 8.2 8.2 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 None 72 Human Binding pIC50 = 8.2 8.2 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 None 72 Human Binding pIC50 = 8.2 8.2 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
10719448 35603 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 478 9 2 6 3.4 O=S(=O)(NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL143952 35603 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 478 9 2 6 3.4 O=S(=O)(NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10673854 44452 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 533 7 1 8 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL151894 44452 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 533 7 1 8 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
10645076 200310 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 407 4 1 5 4.4 Oc1nc2ccc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
CHEMBL59741 200310 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 407 4 1 5 4.4 Oc1nc2ccc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)cc2s1 10.1021/jm970298c
121852 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
121852 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL11592 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
CHEMBL301060 10166 None 7 Rat Binding pIC50 = 5.2 5.2 - 1
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 442 9 0 5 4.2 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)C1COc2cccc(OC)c2C1 10.1021/jm950861w
10040815 97060 None 0 Rat Binding pIC50 = 4.2 4.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL264027 97060 None 0 Rat Binding pIC50 = 4.2 4.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26715 97060 None 0 Rat Binding pIC50 = 4.2 4.2 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 306 7 1 4 1.8 CCCN(CCNC(C)=O)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
15516683 10072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 438 8 2 6 3.5 CN(CC(C)(C)C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL115352 10072 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 438 8 2 6 3.5 CN(CC(C)(C)C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
10691383 100775 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
CHEMBL292935 100775 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 383 6 1 6 3.8 COc1ccccc1N1CCN(CCCc2ccc3nc(O)sc3c2)CC1 10.1021/jm970298c
25070577 111666 None 4 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
CHEMBL3286557 111666 None 4 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 304 3 2 4 2.3 CNc1nc(C(F)(F)c2ccccc2)nc2c1CCNCC2 10.1021/jm5003292
9867902 55219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
CHEMBL161780 55219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Affinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding techniqueAffinity of compound towards 5-hydroxytryptamine 1B receptor was evaluated using radioligand binding technique
ChEMBL 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
9867902 55219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
CHEMBL161780 55219 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
10525100 119521 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 401 8 2 6 2.8 c1cncc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
CHEMBL345657 119521 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 401 8 2 6 2.8 c1cncc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
10341917 168049 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
CHEMBL432332 168049 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
10502495 53715 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 425 6 3 4 3.4 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL16035 53715 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
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 425 6 3 4 3.4 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
10592083 35601 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 324 5 2 5 2.1 NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL143951 35601 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 324 5 2 5 2.1 NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
182585 15447 None 15 Rat Binding pIC50 = 6.2 6.2 -1 4
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 10.1021/jm00401a007
CHEMBL12152 15447 None 15 Rat Binding pIC50 = 6.2 6.2 -1 4
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 10.1021/jm00401a007
10782381 89273 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 326 4 2 3 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)CNC4=O)cc32)C1 10.1021/jm000956k
CHEMBL2368258 89273 None 0 Human Binding pIC50 = 5.2 5.2 - 0
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 326 4 2 3 2.0 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(CN4C(=O)CNC4=O)cc32)C1 10.1021/jm000956k
10598044 203294 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)c(Cl)c1 10.1021/jm950543x
CHEMBL64727 203294 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 416 3 0 5 5.2 Clc1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)c(Cl)c1 10.1021/jm950543x
10551680 99044 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
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 454 7 2 4 4.7 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
CHEMBL280314 99044 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
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 454 7 2 4 4.7 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
10833258 96418 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 374 4 0 5 4.4 C(=C/c1ccccc1)\CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL261977 96418 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 374 4 0 5 4.4 C(=C/c1ccccc1)\CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
1524 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
197 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
3822 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
3822.0 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
88 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
CHEMBL51 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
DB12465 2181 None 96 Human Binding pIC50 = 5.2 5.2 -2511 52
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 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
10839082 39713 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 2 6 4.3 CC(=O)Nc1ccc(CCN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL147546 39713 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 2 6 4.3 CC(=O)Nc1ccc(CCN(C)C2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10602052 119265 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 520 10 1 7 3.9 CN(Cc1ccc(S(C)(=O)=O)cc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL343667 119265 None 0 Human Binding pIC50 = 7.2 7.2 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 520 10 1 7 3.9 CN(Cc1ccc(S(C)(=O)=O)cc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10691904 35620 None 0 Human Binding pIC50 = 6.2 6.2 -6 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
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 None 0 Human Binding pIC50 = 6.2 6.2 -6 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
9911120 9623 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
CHEMBL11265 9623 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.Compound was evaluated for the binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]ketanserin.
ChEMBL 440 6 0 5 4.0 COc1cccc2c1CC1(CCCN1CCCCN1C(=O)CC3(CCCC3)CC1=O)CO2 10.1016/0960-894X(96)00174-6
10569470 100912 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 344 4 0 7 2.2 CCOC(=O)CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
CHEMBL293879 100912 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 344 4 0 7 2.2 CCOC(=O)CN1CCN(c2nc3ccsc3n3cccc23)CC1 10.1021/jm950543x
10789717 79526 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(C[C@@H](F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL2114036 79526 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(C[C@@H](F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10600063 120011 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 460 9 1 4 4.2 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4C)cc23)C1 10.1021/jm9805687
CHEMBL350153 120011 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 460 9 1 4 4.2 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(C[C@H]4COC(=O)N4C)cc23)C1 10.1021/jm9805687
10707563 28355 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
CHEMBL137478 28355 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSBBinding affinity to 5-HT1B receptors using rat cortex+striatum + globus pallidus,[3H]-5-OH-tryptamine, and serotonin for NSB
ChEMBL 275 3 0 3 3.3 CCCN1CCCCC12COc1cccc(OC)c1C2 10.1021/jm950861w
10091430 9881 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
CHEMBL11425 9881 None 0 Human Binding pIC50 = 5.2 5.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 384 7 1 4 3.3 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2C1 10.1016/0960-894X(96)00174-6
10452995 194746 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 390 4 0 5 4.0 COc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL53662 194746 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 390 4 0 5 4.0 COc1ccc2c(c1)nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
10600871 164950 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 483 5 2 7 4.7 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
CHEMBL422504 164950 None 0 Rat Binding pIC50 = 8.1 8.1 - 0
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 483 5 2 7 4.7 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
10733823 56280 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 311 5 1 5 2.0 c1cc2[nH]cc(CCCN3CCOCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL162930 56280 None 0 Human Binding pIC50 = 8.1 8.1 - 0
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 311 5 1 5 2.0 c1cc2[nH]cc(CCCN3CCOCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10717072 163243 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
CHEMBL418499 163243 None 0 Rat Binding pIC50 = 7.2 7.2 - 0
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
ChEMBL 421 4 0 5 4.0 Cn1c(=O)sc2cc(CCN3CCN(c4cccc(C(F)(F)F)c4)CC3)ccc21 10.1021/jm970298c
10530932 169678 None 15 Rat Binding pIC50 = 7.2 7.2 - 0
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 561 7 1 9 4.4 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(C)(=O)=O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1 10.1021/jm990397l
CHEMBL443762 169678 None 15 Rat Binding pIC50 = 7.2 7.2 - 0
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 561 7 1 9 4.4 Cc1nnc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(C)(=O)=O)c(N5CCN(C)CC5)c4)cc3)c(C)c2)o1 10.1021/jm990397l
9981671 14541 None 0 Rat Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
CHEMBL12028 14541 None 0 Rat Binding pIC50 = 6.2 6.2 - 1
In vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membraneIn vitro inhibitory concentration against radioligand [3H]5-HT binding to 5-hydroxytryptamine 1B receptor in rat striatal membrane
ChEMBL 459 7 1 9 3.1 COc1ccccc1N1CCN(CCCSc2nc3sc(C)c(C)c3c(=O)n2N)CC1 10.1021/jm950866t
10627612 44245 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
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 615 7 1 9 5.3 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(=O)(=O)C(F)(F)F)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
CHEMBL151695 44245 None 0 Rat Binding pIC50 = 6.2 6.2 - 0
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 615 7 1 9 5.3 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc(OS(=O)(=O)C(F)(F)F)c(N5CCN(C)CC5)c4)cc3)c(C)c2)no1 10.1021/jm990397l
10429859 12042 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL1183429 12042 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
CHEMBL296395 12042 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 380 7 1 5 2.7 COc1cccc2c1CC(NCCCCN1C(=O)c3ccccc3C1=O)CO2 10.1021/jm00038a007
135398745 2914 None 112 Rat Binding pIC50 = 6.2 6.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745.0 2914 None 112 Rat Binding pIC50 = 6.2 6.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 None 112 Rat Binding pIC50 = 6.2 6.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 None 112 Rat Binding pIC50 = 6.2 6.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 None 112 Rat Binding pIC50 = 6.2 6.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
173 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm950543x
5011 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm950543x
CHEMBL18772 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm950543x
10739272 100739 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3sccc3n2c1 10.1021/jm950543x
CHEMBL292725 100739 None 0 Rat Binding pIC50 = 5.2 5.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 392 3 0 7 3.6 c1cc2c(N3CCN(Cc4ccc5c(c4)OCO5)CC3)nc3sccc3n2c1 10.1021/jm950543x
173 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm960501o
5011 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm960501o
CHEMBL18772 3262 None 95 Rat Binding pIC50 = 5.2 5.2 -2 23
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm960501o
10689339 203091 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 352 2 0 5 4.0 Fc1ccc(N2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL63905 203091 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 352 2 0 5 4.0 Fc1ccc(N2CCN(c3nc4ccsc4n4cccc34)CC2)cc1 10.1021/jm950543x
10714509 101589 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 375 3 0 5 3.7 Cc1ccnc2c1nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
CHEMBL298649 101589 None 0 Rat Binding pIC50 = 4.2 4.2 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 375 3 0 5 3.7 Cc1ccnc2c1nc(N1CCN(Cc3ccc(F)cc3)CC1)c1cccn12 10.1021/jm960501o
11059058 10091 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
CHEMBL115444 10091 None 0 Human Binding pIC50 = 6.2 6.2 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 429 3 1 7 4.1 O=C(OCc1cc2c(cc1Cl)OCO2)N1CCC(n2c(O)nc3ccccc32)CC1 10.1021/jm010878g
10504096 118935 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](CO)c1ccccc1 10.1021/jm9910021
CHEMBL342330 118935 None 0 Human Binding pIC50 = 7.2 7.2 - 0
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 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](CO)c1ccccc1 10.1021/jm9910021
114 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
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 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
6426760 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
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 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
CHEMBL292779 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
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 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
114 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
6426760 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
CHEMBL292779 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
10694895 102445 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.7 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(COc2ccccc2)CC1 10.1021/jm981133m
CHEMBL303997 102445 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 451 8 1 5 4.7 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(COc2ccccc2)CC1 10.1021/jm981133m
10501945 54934 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 414 8 2 5 4.0 C[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL161410 54934 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 414 8 2 5 4.0 C[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10741826 39199 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 441 6 2 7 4.1 Oc1nc2ccccc2n1C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146991 39199 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 441 6 2 7 4.1 Oc1nc2ccccc2n1C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10573164 203084 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 402 2 0 5 4.9 FC(F)(F)c1cccc(N2CCN(c3nc4sccc4n4cccc34)CC2)c1 10.1021/jm950543x
CHEMBL63845 203084 None 0 Rat Binding pIC50 = 5.1 5.1 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 402 2 0 5 4.9 FC(F)(F)c1cccc(N2CCN(c3nc4sccc4n4cccc34)CC2)c1 10.1021/jm950543x
44267161 163042 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
CHEMBL417608 163042 None 0 Human Binding pIC50 = 5.1 5.1 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.Binding affinity towards 5-hydroxytryptamine 1B receptor by displacement of [3H]5-HT.
ChEMBL 456 10 0 5 4.4 CCCN(CCCCN1C(=O)CC2(CCCC2)CC1=O)CC1COc2cccc(OC)c2C1 10.1016/0960-894X(96)00174-6
114 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
6426760 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
CHEMBL292779 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Compound was evaluated for the affinity at 5-hydroxytryptamine 1B receptorCompound was evaluated for the affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
73354882 89693 None 1 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL2376482 89693 None 1 Rat Binding pIC50 = 7.1 7.1 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 290 1 2 1 3.6 Cc1[nH]c2ccc(Br)cc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
114 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
6426760 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
CHEMBL292779 2254 None 14 Human Binding pIC50 = 7.1 7.1 - 1
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704560
10693207 37981 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm9910021
CHEMBL145997 37981 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 8 2 6 3.3 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm9910021
10530035 51632 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 522 8 2 5 4.2 COc1ccc(NC(=O)N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15837 51632 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 522 8 2 5 4.2 COc1ccc(NC(=O)N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10645335 188713 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 411 3 0 5 4.5 Clc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c(Cl)c1 10.1021/jm960501o
CHEMBL50456 188713 None 0 Rat Binding pIC50 = 4.1 4.1 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 411 3 0 5 4.5 Clc1ccc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c(Cl)c1 10.1021/jm960501o
10768329 40248 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 521 11 3 7 3.0 CS(=O)(=O)NC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148071 40248 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 521 11 3 7 3.0 CS(=O)(=O)NC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10836290 55437 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 428 8 1 5 3.1 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1CCc1ccccc1 10.1021/jm980569z
CHEMBL161970 55437 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 428 8 1 5 3.1 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1CCc1ccccc1 10.1021/jm980569z
11795525 121116 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 404 8 2 6 3.5 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm9910021
CHEMBL357408 121116 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 404 8 2 6 3.5 c1cc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm9910021
10766321 40142 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.7 OC[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL147979 40142 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 458 10 3 6 3.7 OC[C@H](NCC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
6604720 15273 None 3 Rat Binding pIC50 = 6.1 6.1 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@H]1COc2ccccc2O1 10.1021/jm00401a007
CHEMBL12129 15273 None 3 Rat Binding pIC50 = 6.1 6.1 - 0
Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.Binding affinity against 5-HT1B receptor in rat brain membrane using [3H]8-OH-DPAT as a selective ligand.
ChEMBL 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNC[C@H]1COc2ccccc2O1 10.1021/jm00401a007
10621021 203384 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
CHEMBL65367 203384 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704560
134551 358 None 27 Rat Binding pIC50 = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 358 None 27 Rat Binding pIC50 = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 358 None 27 Rat Binding pIC50 = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 358 None 27 Rat Binding pIC50 = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
10505525 38382 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 3 6 4.7 CC(=O)Nc1ccc([C@@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146338 38382 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 3 6 4.7 CC(=O)Nc1ccc([C@@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10767244 40089 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 10 3 6 4.1 CC(=O)Nc1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL147940 40089 None 0 Human Binding pIC50 = 8.1 8.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 485 10 3 6 4.1 CC(=O)Nc1ccc(CNCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10096048 98855 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL278917 98855 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
9804849 67456 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
CHEMBL189118 67456 None 0 Human Binding pIC50 = 6.1 6.1 - 0
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 472 8 1 5 5.1 Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12 10.1021/jm050103y
9981024 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10786628 38455 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 390 7 1 5 3.1 CC#CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146396 38455 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 390 7 1 5 3.1 CC#CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
14450364 56003 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 247 1 0 3 2.6 COc1cc(C)cc2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
CHEMBL162449 56003 None 0 Rat Binding pIC50 = 6.1 6.1 - 0
Concentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uMConcentration necessary to achieve half maximal inhibition of [125I]- Iodocyanopindolol binding to 5-hydroxytryptamine 1B receptor at 1 uM
ChEMBL 247 1 0 3 2.6 COc1cc(C)cc2c1[C@H]1CCCN(C)[C@@H]1CO2 10.1021/jm00123a039
11626724 110476 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 458 9 3 6 3.6 Cc1ccccc1CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL324751 110476 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 458 9 3 6 3.6 Cc1ccccc1CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
6426761 13957 None 1 Human Binding pIC50 = 7.1 7.1 - 0
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 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
CHEMBL119668 13957 None 1 Human Binding pIC50 = 7.1 7.1 - 0
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 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
9881324 28372 None 3 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm00101a032
CHEMBL137485 28372 None 3 Human Binding pIC50 = 6.1 6.1 - 0
Binding affinity against 5-hydroxytryptamine 1B receptorBinding affinity against 5-hydroxytryptamine 1B receptor
ChEMBL 244 3 1 2 2.8 COc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1021/jm00101a032
10709057 120068 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 296 3 1 4 3.3 Cc1noc(-c2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1 10.1021/jm000956k
CHEMBL350637 120068 None 0 Human Binding pIC50 = 6.1 6.1 - 0
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 296 3 1 4 3.3 Cc1noc(-c2ccc3[nH]cc([C@H]4C[C@H](N(C)C)C4)c3c2)n1 10.1021/jm000956k
44341798 9816 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 424 8 3 6 3.1 CC(C)(C)CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL113831 9816 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 424 8 3 6 3.1 CC(C)(C)CNCC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
11798621 40299 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 471 9 3 6 3.8 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
CHEMBL148110 40299 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 471 9 3 6 3.8 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
10412189 77253 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL2079627 77253 None 0 Rat Binding pIC50 = 7.1 7.1 - 0
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 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10670211 120220 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 428 9 1 5 3.9 c1ccc(CCCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL352123 120220 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 428 9 1 5 3.9 c1ccc(CCCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10739818 111143 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL326371 111143 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10719245 37808 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 472 10 2 6 4.1 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
CHEMBL145849 37808 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 472 10 2 6 4.1 CN(CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
176 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Rat Binding pIC50 = 4.1 4.1 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2105 3054 None 37 Rat Binding pIC50 = 7.1 7.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3054 None 37 Rat Binding pIC50 = 7.1 7.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3054 None 37 Rat Binding pIC50 = 7.1 7.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3054 None 37 Rat Binding pIC50 = 7.1 7.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3054 None 37 Rat Binding pIC50 = 7.1 7.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
10500370 52790 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 386 7 2 5 3.7 c1ccc(NC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL159493 52790 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 386 7 2 5 3.7 c1ccc(NC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10670879 119868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 442 9 1 5 4.4 C[C@@H](c1ccccc1)N(C)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
CHEMBL348864 119868 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 442 9 1 5 4.4 C[C@@H](c1ccccc1)N(C)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
10739818 111143 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL326371 111143 None 0 Human Binding pIC50 = 7.1 7.1 - 0
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 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
44341609 9895 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 472 9 2 6 3.9 Cc1ccccc1CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL114303 9895 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 472 9 2 6 3.9 Cc1ccccc1CN(C)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
10600678 119197 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 476 10 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
CHEMBL343217 119197 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 476 10 2 6 4.3 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
10811964 168334 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 418 8 1 6 3.9 CN(Cc1ccco1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL434315 168334 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 418 8 1 6 3.9 CN(Cc1ccco1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
3245407 48105 None 25 Rat Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
CHEMBL1550957 48105 None 25 Rat Binding pIC50 = 6.1 6.1 - 0
Displacement of [125I]-iodocyanopindolol from rat 5HT1B receptorDisplacement of [125I]-iodocyanopindolol from rat 5HT1B receptor
ChEMBL 212 1 2 1 2.9 Cc1[nH]c2ccccc2c1C1=CCNCC1 10.1016/j.ejmech.2013.03.006
441383 20333 None 57 Rat Binding pIC50 = 4.1 4.1 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20333 None 57 Rat Binding pIC50 = 4.1 4.1 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10720175 38570 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 3 6 4.7 CC(=O)Nc1ccc([C@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146483 38570 None 0 Human Binding pIC50 = 8.0 8.0 - 0
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 499 10 3 6 4.7 CC(=O)Nc1ccc([C@H](C)NCC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
10788768 56495 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 430 8 2 6 3.0 OCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163386 56495 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 430 8 2 6 3.0 OCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10588665 89269 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 278 3 2 2 4.2 N[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL2368254 89269 None 0 Human Binding pIC50 = 8.0 8.0 - 0
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 278 3 2 2 4.2 N[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
9981024 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL26018 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
CHEMBL300735 96097 None 0 Rat Binding pIC50 = 5.1 5.1 - 1
Binding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidusBinding affinity for 5-hydroxytryptamine 1B receptor in rat cortex, striatum and globus pallidus
ChEMBL 446 11 1 5 3.8 CCCN(CCCCNS(=O)(=O)c1ccc(C)cc1)C1COc2cccc(OC)c2C1 10.1021/jm00038a007
10247171 203427 None 0 Rat Binding pIC50 = 4.0 4.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1 10.1021/jm950543x
CHEMBL65710 203427 None 0 Rat Binding pIC50 = 4.0 4.0 - 0
Binding affinity for 5-hydroxytryptamine 1B receptorBinding affinity for 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 0 5 3.9 c1ccc(CN2CCN(c3nc4sccc4n4cccc34)CC2)cc1 10.1021/jm950543x
10811801 120144 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 415 8 1 6 2.9 c1cncc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL351311 120144 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 415 8 1 6 2.9 c1cncc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10519108 52944 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 311 5 2 5 1.6 OC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL159627 52944 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 311 5 2 5 1.6 OC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10780344 119936 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 297 4 2 5 1.4 O[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL349528 119936 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 297 4 2 5 1.4 O[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10526737 102742 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.5 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(CCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL304993 102742 None 0 Human Binding pIC50 = 6.0 6.0 - 0
Displacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of specific [3H]5-HT binding to cloned human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 8 1 5 3.5 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCN(CCc2ccccc2)CC1 10.1021/jm981133m
10526567 40268 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 428 8 2 5 4.5 C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148087 40268 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 428 8 2 5 4.5 C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10456869 9992 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 458 9 2 6 3.6 CN(Cc1ccccc1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
CHEMBL114877 9992 None 0 Human Binding pIC50 = 7.0 7.0 - 0
Ability to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitroAbility to displace [3H]5-HT from recombinant human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells determined in vitro
ChEMBL 458 9 2 6 3.6 CN(Cc1ccccc1)CC1(O)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1016/s0960-894x(99)00614-9
10494885 89268 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 306 4 1 2 4.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL2368253 89268 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 306 4 1 2 4.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
18691565 89272 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
CHEMBL2368257 89272 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 327 4 1 3 3.0 CN1C(=O)OCC1Cc1ccc2[nH]cc([C@H]3C[C@H](N(C)C)C3)c2c1 10.1021/jm000956k
10834414 188894 None 0 Rat Binding pIC50 = 4.0 4.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 393 3 0 5 4.4 c1ccc(CN2CCN(c3nc4ccc5ncccc5c4n4cccc34)CC2)cc1 10.1021/jm960501o
CHEMBL50740 188894 None 0 Rat Binding pIC50 = 4.0 4.0 - 0
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 393 3 0 5 4.4 c1ccc(CN2CCN(c3nc4ccc5ncccc5c4n4cccc34)CC2)cc1 10.1021/jm960501o
10504097 40393 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 458 9 3 6 3.6 CC(CO)(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148194 40393 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 458 9 3 6 3.6 CC(CO)(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
9802530 35386 None 1 Human Binding pIC50 = 7.0 7.0 -2 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
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 None 1 Human Binding pIC50 = 7.0 7.0 -2 4
Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.Compound was tested for binding affinity against human 5-hydroxytryptamine 1D receptor beta clones expressed in human embryonic kidney (HEK 293) cells line.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10526736 10222 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL116031 10222 None 0 Human Binding pIC50 = 7.0 7.0 - 0
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 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
6426761 13957 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm9704560
CHEMBL119668 13957 None 1 Human Binding pIC50 = 7.0 7.0 - 0
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm9704560
23533297 193025 None 2 Guinea pig Binding pKd = 9.4 9.4 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
CHEMBL5209320 193025 None 2 Guinea pig Binding pKd = 9.4 9.4 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
CHEMBL5222828 193025 None 2 Guinea pig Binding pKd = 9.4 9.4 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as dissociation constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
2869 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60857 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
60857.0 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
CHEMBL1185 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
DB00315 4152 None 89 Human Binding pKd = 8.8 8.8 -8 7
Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.Binding affinity against 5-hydroxytryptamine 1D receptor beta using rabbit saphenous vein assay.
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm00018a016
23533297 193025 None 2 Guinea pig Binding pKi = 11 11.0 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
CHEMBL5209320 193025 None 2 Guinea pig Binding pKi = 11 11.0 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
CHEMBL5222828 193025 None 2 Guinea pig Binding pKi = 11 11.0 - 1
Binding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysisBinding affinity to guinea pig 5-HT1B receptor assessed as inhibition constant by autoradiographic analysis
ChEMBL 462 4 1 7 2.9 Cc1ccc(N2CCN(C)CC2)c2oc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c12 10.1021/acs.jmedchem.2c00633
1043 1582 None 14 Rat Binding pKi = 10.0 10.0 4 28
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 None 14 Rat Binding pKi = 10.0 10.0 4 28
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 None 14 Rat Binding pKi = 10.0 10.0 4 28
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
8223.0 1582 None 14 Rat Binding pKi = 10.0 10.0 4 28
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 None 14 Rat Binding pKi = 10.0 10.0 4 28
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 None 14 Rat Binding pKi = 10.0 10.0 4 28
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
11797998 35692 None 0 Human Binding pKi = 10 10.0 1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm7011722
CHEMBL144030 35692 None 0 Human Binding pKi = 10 10.0 1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm7011722
24881753 137202 None 0 Human Binding pKi = 10 10.0 14 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL374973 137202 None 0 Human Binding pKi = 10 10.0 14 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
107780 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
14 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
CHEMBL15928 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
107780 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity towards cloned human 5-hydroxytryptamine 1B receptorAffinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
14 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity towards cloned human 5-hydroxytryptamine 1B receptorAffinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
CHEMBL15928 1844 None 54 Human Binding pKi = 9.9 9.9 1 17
Affinity towards cloned human 5-hydroxytryptamine 1B receptorAffinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
44351656 117098 None 0 Human Binding pKi = 9.9 9.9 5 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 499 6 2 7 4.3 COc1ccc(NC(=O)c2ccc(-c3ccc(C4=NC(C)ON4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm9703552
CHEMBL339308 117098 None 0 Human Binding pKi = 9.9 9.9 5 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 499 6 2 7 4.3 COc1ccc(NC(=O)c2ccc(-c3ccc(C4=NC(C)ON4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm9703552
44443130 93769 None 0 Human Binding pKi = 9.7 9.7 1 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 464 6 0 6 3.2 Cc1ccc2c(OCCN3CCN(Cc4cc(F)c5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL247428 93769 None 0 Human Binding pKi = 9.7 9.7 1 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 464 6 0 6 3.2 Cc1ccc2c(OCCN3CCN(Cc4cc(F)c5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
9909089 186968 None 0 Human Binding pKi = 9.7 9.7 -23 7
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL490417 186968 None 0 Human Binding pKi = 9.7 9.7 -23 7
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
6160690 119321 None 37 Human Binding pKi = 9.7 9.7 6 3
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 377 8 2 3 3.6 COc1ccc(CNC(=O)/C=C/c2ccc3[nH]cc(CCN(C)C)c3c2)cc1 10.1021/jm9604890
CHEMBL344127 119321 None 37 Human Binding pKi = 9.7 9.7 6 3
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 377 8 2 3 3.6 COc1ccc(CNC(=O)/C=C/c2ccc3[nH]cc(CCN(C)C)c3c2)cc1 10.1021/jm9604890
71461632 78778 None 0 Human Binding pKi = 9.7 9.7 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 472 6 0 5 3.6 Cc1ccccc1CN1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1 10.1021/jm9703552
CHEMBL2112662 78778 None 0 Human Binding pKi = 9.7 9.7 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 472 6 0 5 3.6 Cc1ccccc1CN1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1 10.1021/jm9703552
44404240 72527 None 0 Human Binding pKi = 9.6 9.6 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 441 2 0 5 3.6 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C(F)(F)F)nc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL199088 72527 None 0 Human Binding pKi = 9.6 9.6 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 441 2 0 5 3.6 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C(F)(F)F)nc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
59636728 125684 None 0 Chinese hamster Binding pKi = 9.6 9.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 544 7 1 7 4.6 O=C(NC1CCN(c2ncccc2Cl)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647266 125684 None 0 Chinese hamster Binding pKi = 9.6 9.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 544 7 1 7 4.6 O=C(NC1CCN(c2ncccc2Cl)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
124 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
2032 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
4636 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
4636.0 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
CHEMBL762 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
DB00935 2981 None 47 Human Binding pKi = 9.5 9.5 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm970513p
9955819 118144 None 0 Human Binding pKi = 9.5 9.5 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 458 5 0 5 3.6 Cc1ccccc1N1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1 10.1021/jm9703552
CHEMBL340786 118144 None 0 Human Binding pKi = 9.5 9.5 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 458 5 0 5 3.6 Cc1ccccc1N1CCN(C(=O)COc2ccc3cccc(N4CCN(C)CC4)c3c2)CC1 10.1021/jm9703552
188 3391 None 80 Human Binding pKi = 9.5 9.5 1 6
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2015.07.012
196968 3391 None 80 Human Binding pKi = 9.5 9.5 1 6
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2015.07.012
CHEMBL473186 3391 None 80 Human Binding pKi = 9.5 9.5 1 6
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 281 2 1 3 4.1 Nc1nc(cc(n1)c1ccc(c2c1cccc2)F)C(C)C 10.1016/j.bmcl.2015.07.012
10073139 184296 None 0 Human Binding pKi = 9.5 9.5 1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 464 5 1 5 4.6 O=C1COc2ccc(CCN3CCN(c4cccc5nc(-c6ccccc6)ccc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
CHEMBL484059 184296 None 0 Human Binding pKi = 9.5 9.5 1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 464 5 1 5 4.6 O=C1COc2ccc(CCN3CCN(c4cccc5nc(-c6ccccc6)ccc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
44404225 133533 None 0 Human Binding pKi = 9.5 9.5 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 406 2 0 4 3.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(Cl)cc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL370852 133533 None 0 Human Binding pKi = 9.5 9.5 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 406 2 0 4 3.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(Cl)cc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
10838063 78776 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL2112660 78776 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
10531 1420 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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
10531.0 1420 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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 None 21 Rat Binding pKi = 9.4 9.4 -5 23
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
9977716 170130 None 0 Human Binding pKi = 9.4 9.4 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 390 4 2 4 3.2 Cc1cc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2[nH]1 10.1016/j.bmcl.2008.08.084
CHEMBL444398 170130 None 0 Human Binding pKi = 9.4 9.4 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 390 4 2 4 3.2 Cc1cc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2[nH]1 10.1016/j.bmcl.2008.08.084
10454806 187885 None 0 Human Binding pKi = 9.4 9.4 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL496520 187885 None 0 Human Binding pKi = 9.4 9.4 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
45104767 201610 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1 10.1021/jm901200t
CHEMBL605785 201610 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1 10.1021/jm901200t
45104767 201610 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1 10.1021/jm901200t
CHEMBL605785 201610 None 0 Human Binding pKi = 9.4 9.4 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 506 5 1 8 4.2 COC1(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(-c5c(C)nn(C)c5C)c4o3)cn2)CCOCC1 10.1021/jm901200t
10649124 19470 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL129813 19470 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
10672840 78777 None 0 Human Binding pKi = 9.4 9.4 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 494 5 0 5 4.5 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6ccccc56)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL2112661 78777 None 0 Human Binding pKi = 9.4 9.4 2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 494 5 0 5 4.5 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6ccccc56)CC4)cc23)CC1 10.1021/jm9703552
10601619 116836 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
CHEMBL338015 116836 None 0 Human Binding pKi = 9.4 9.4 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
59636724 126208 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 483 7 0 7 3.5 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CC(Oc2cccnc2)C1 nan
CHEMBL3650029 126208 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 483 7 0 7 3.5 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CC(Oc2cccnc2)C1 nan
10434550 12099 None 0 Human Binding pKi = 9.3 9.3 52 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1183948 12099 None 0 Human Binding pKi = 9.3 9.3 52 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL325359 12099 None 0 Human Binding pKi = 9.3 9.3 52 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
24881204 188422 None 0 Human Binding pKi = 9.3 9.3 3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL502138 188422 None 0 Human Binding pKi = 9.3 9.3 3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
10673329 99332 None 0 Human Binding pKi = 9.3 9.3 10 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 512 8 0 7 5.2 COc1cc2c(cc1OCCN(C)C)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1021/jm970457s
CHEMBL282229 99332 None 0 Human Binding pKi = 9.3 9.3 10 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 512 8 0 7 5.2 COc1cc2c(cc1OCCN(C)C)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1021/jm970457s
49850672 56386 None 0 Human Binding pKi = 9.3 9.3 -1 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631532 56386 None 0 Human Binding pKi = 9.3 9.3 -1 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 404 5 1 5 4.1 COC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49850872 56458 None 0 Human Binding pKi = 9.3 9.3 -1 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632206 56458 None 0 Human Binding pKi = 9.3 9.3 -1 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 388 5 1 4 3.9 CC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
9909089 186968 None 0 Human Binding pKi = 9.3 9.3 -23 7
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100714c
CHEMBL490417 186968 None 0 Human Binding pKi = 9.3 9.3 -23 7
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100714c
10478217 188087 None 0 Human Binding pKi = 9.3 9.3 -2 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)ccc(Cl)c2n1 10.1016/j.bmcl.2008.08.084
CHEMBL497980 188087 None 0 Human Binding pKi = 9.3 9.3 -2 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)ccc(Cl)c2n1 10.1016/j.bmcl.2008.08.084
10071738 192599 None 0 Human Binding pKi = 9.3 9.3 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL521506 192599 None 0 Human Binding pKi = 9.3 9.3 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 4 1 5 3.9 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2008.08.084
9979309 192982 None 0 Human Binding pKi = 9.3 9.3 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL522257 192982 None 0 Human Binding pKi = 9.3 9.3 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
9909089 186968 None 0 Human Binding pKi = 9.3 9.3 -23 7
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL490417 186968 None 0 Human Binding pKi = 9.3 9.3 -23 7
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
44404229 70486 None 0 Human Binding pKi = 9.3 9.3 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 397 2 0 5 3.1 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C#N)cc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL194647 70486 None 0 Human Binding pKi = 9.3 9.3 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 397 2 0 5 3.1 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccc(C#N)cc2)CC4)CC1 10.1016/j.bmcl.2005.06.042
59636723 125679 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 509 7 1 6 4.6 O=C(NC1CCN(c2ccccc2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647261 125679 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 509 7 1 6 4.6 O=C(NC1CCN(c2ccccc2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
59636782 125700 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 540 8 1 8 4.0 COc1cccnc1N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
CHEMBL3647282 125700 None 0 Chinese hamster Binding pKi = 9.3 9.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 540 8 1 8 4.0 COc1cccnc1N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
24881754 188292 None 0 Human Binding pKi = 9.2 9.2 3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL500284 188292 None 0 Human Binding pKi = 9.2 9.2 3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
44402885 71814 None 0 Human Binding pKi = 9.2 9.2 25 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 469 4 0 4 5.4 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccccc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196848 71814 None 0 Human Binding pKi = 9.2 9.2 25 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 469 4 0 4 5.4 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccccc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
10001971 184324 None 0 Human Binding pKi = 9.2 9.2 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.5 Cc1cc(N2CCN(CCc3ccc4c(c3)NC(=O)CO4)CC2)c2ccc(C)nc2c1 10.1016/j.bmcl.2008.08.084
CHEMBL484260 184324 None 0 Human Binding pKi = 9.2 9.2 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.5 Cc1cc(N2CCN(CCc3ccc4c(c3)NC(=O)CO4)CC2)c2ccc(C)nc2c1 10.1016/j.bmcl.2008.08.084
10341129 186798 None 0 Human Binding pKi = 9.2 9.2 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 403 4 1 6 2.6 Cc1ncc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL489195 186798 None 0 Human Binding pKi = 9.2 9.2 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 403 4 1 6 2.6 Cc1ncc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
10319235 187137 None 0 Human Binding pKi = 9.2 9.2 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 407 4 1 5 3.1 CC1(C)Cc2cccc(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)c2O1 10.1016/j.bmcl.2008.08.084
CHEMBL491839 187137 None 0 Human Binding pKi = 9.2 9.2 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 407 4 1 5 3.1 CC1(C)Cc2cccc(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)c2O1 10.1016/j.bmcl.2008.08.084
9955522 72489 None 0 Human Binding pKi = 9.2 9.2 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 452 3 0 6 3.7 Cc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)cnn1-c1ccccc1 10.1016/j.bmcl.2005.06.042
CHEMBL198975 72489 None 0 Human Binding pKi = 9.2 9.2 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 452 3 0 6 3.7 Cc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)cnn1-c1ccccc1 10.1016/j.bmcl.2005.06.042
9832057 52315 None 0 Human Binding pKi = 9.2 9.2 1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
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 10.1021/jm7011722
CHEMBL158941 52315 None 0 Human Binding pKi = 9.2 9.2 1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
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 10.1021/jm7011722
9832057 52315 None 0 Human Binding pKi = 9.2 9.2 1 3
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 0 Human Binding pKi = 9.2 9.2 1 3
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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
44279549 99440 None 0 Human Binding pKi = 9.2 9.2 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 606 11 4 7 4.6 CN1CCN(c2cccc3ccc(OCC(=O)Nc4ccc(NC(=O)COc5ccc6[nH]cc(CCN)c6c5)cc4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL282950 99440 None 0 Human Binding pKi = 9.2 9.2 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 606 11 4 7 4.6 CN1CCN(c2cccc3ccc(OCC(=O)Nc4ccc(NC(=O)COc5ccc6[nH]cc(CCN)c6c5)cc4)cc23)CC1 10.1016/s0960-894x(98)00222-4
59636764 125694 None 0 Chinese hamster Binding pKi = 9.2 9.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 484 9 1 6 4.2 COc1cccc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647276 125694 None 0 Chinese hamster Binding pKi = 9.2 9.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 484 9 1 6 4.2 COc1cccc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
44279525 105512 None 0 Human Binding pKi = 9.1 9.1 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL31217 105512 None 0 Human Binding pKi = 9.1 9.1 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
44279525 105512 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL31217 105512 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 10.1021/jm7011722
24881689 170132 None 0 Human Binding pKi = 9.1 9.1 1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL444404 170132 None 0 Human Binding pKi = 9.1 9.1 1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
24881203 173231 None 0 Human Binding pKi = 9.1 9.1 1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL452387 173231 None 0 Human Binding pKi = 9.1 9.1 1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
11655728 16644 None 8 Human Binding pKi = 9.1 9.1 -16 6
Displacement of [3H]-5-HT from human recombinant 5HT1B receptor expressed in CHO cells after 45 mins by scintillation countingDisplacement of [3H]-5-HT from human recombinant 5HT1B receptor expressed in CHO cells after 45 mins by scintillation counting
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16644 None 8 Human Binding pKi = 9.1 9.1 -16 6
Displacement of [3H]-5-HT from human recombinant 5HT1B receptor expressed in CHO cells after 45 mins by scintillation countingDisplacement of [3H]-5-HT from human recombinant 5HT1B receptor expressed in CHO cells after 45 mins by scintillation counting
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
10275633 91954 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241463 91954 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
49850870 56389 None 0 Human Binding pKi = 9.1 9.1 -6 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631535 56389 None 0 Human Binding pKi = 9.1 9.1 -6 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 424 6 1 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
10048342 186832 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2ccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2008.08.084
CHEMBL489393 186832 None 0 Human Binding pKi = 9.1 9.1 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2ccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2008.08.084
10023176 186946 None 0 Human Binding pKi = 9.1 9.1 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4nccc5ccccc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
CHEMBL490211 186946 None 0 Human Binding pKi = 9.1 9.1 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4nccc5ccccc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
44580783 193160 None 0 Human Binding pKi = 9.1 9.1 31 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 414 4 1 5 3.4 Cc1ccc2c(N3C[C@H]4C[C@@H]3CN4CCc3ccc4c(c3)NC(=O)CO4)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL523064 193160 None 0 Human Binding pKi = 9.1 9.1 31 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 414 4 1 5 3.4 Cc1ccc2c(N3C[C@H]4C[C@@H]3CN4CCc3ccc4c(c3)NC(=O)CO4)cccc2n1 10.1016/j.bmcl.2008.08.084
44404241 133444 None 1 Human Binding pKi = 9.1 9.1 5 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 423 2 0 5 3.7 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cccc3ncccc23)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL370625 133444 None 1 Human Binding pKi = 9.1 9.1 5 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 423 2 0 5 3.7 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cccc3ncccc23)CC4)CC1 10.1016/j.bmcl.2005.06.042
10385855 14425 None 0 Human Binding pKi = 9.1 9.1 1 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 9.1 9.1 1 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 9.1 9.1 1 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
24881264 188307 None 0 Human Binding pKi = 9.1 9.1 13 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL500488 188307 None 0 Human Binding pKi = 9.1 9.1 13 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
59636727 125688 None 0 Chinese hamster Binding pKi = 9.1 9.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 364 5 1 5 2.6 CNC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647270 125688 None 0 Chinese hamster Binding pKi = 9.1 9.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 364 5 1 5 2.6 CNC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
59636707 125686 None 0 Chinese hamster Binding pKi = 9.1 9.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 484 7 1 7 3.9 O=C(NCc1ccc2c(c1)OCO2)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647268 125686 None 0 Chinese hamster Binding pKi = 9.1 9.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 484 7 1 7 3.9 O=C(NCc1ccc2c(c1)OCO2)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
22184652 85052 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 5 2 7 2.8 COc1cc(N2CCCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL224195 85052 None 0 Human Binding pKi = 9.1 9.1 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 5 2 7 2.8 COc1cc(N2CCCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
124 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636.0 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 2981 None 47 Rat Binding pKi = 9.0 9.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
45104862 200835 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 494 5 1 7 4.2 COC1(c2ccc(NC(=O)C3CCc4cc(F)cc(-c5c(C)nn(C)c5C)c4O3)cn2)CCOCC1 10.1021/jm901200t
CHEMBL601013 200835 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 494 5 1 7 4.2 COC1(c2ccc(NC(=O)C3CCc4cc(F)cc(-c5c(C)nn(C)c5C)c4O3)cn2)CCOCC1 10.1021/jm901200t
45104862 200835 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 494 5 1 7 4.2 COC1(c2ccc(NC(=O)C3CCc4cc(F)cc(-c5c(C)nn(C)c5C)c4O3)cn2)CCOCC1 10.1021/jm901200t
CHEMBL601013 200835 None 0 Human Binding pKi = 9.0 9.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 494 5 1 7 4.2 COC1(c2ccc(NC(=O)C3CCc4cc(F)cc(-c5c(C)nn(C)c5C)c4O3)cn2)CCOCC1 10.1021/jm901200t
107780 1844 None 54 Human Binding pKi = 9 9.0 1 17
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
14 1844 None 54 Human Binding pKi = 9 9.0 1 17
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
CHEMBL15928 1844 None 54 Human Binding pKi = 9 9.0 1 17
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
28 3496 None 46 Human Binding pKi = 9 9.0 13 10
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
3292447 3496 None 46 Human Binding pKi = 9 9.0 13 10
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
CHEMBL20963 3496 None 46 Human Binding pKi = 9 9.0 13 10
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
10802304 108536 None 1 Human Binding pKi = 9 9.0 4 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 9 2 2 4.0 CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL320079 108536 None 1 Human Binding pKi = 9 9.0 4 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 9 2 2 4.0 CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
10613373 111305 None 1 Human Binding pKi = 9 9.0 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 10 2 2 4.4 CCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL326667 111305 None 1 Human Binding pKi = 9 9.0 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 10 2 2 4.4 CCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
49850669 56387 None 0 Human Binding pKi = 9 9.0 -5 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631533 56387 None 0 Human Binding pKi = 9 9.0 -5 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
10454807 186833 None 0 Human Binding pKi = 9 9.0 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4cc(F)c5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL489394 186833 None 0 Human Binding pKi = 9 9.0 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4cc(F)c5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
59636767 125704 None 0 Chinese hamster Binding pKi = 9 9.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
CHEMBL3647286 125704 None 0 Chinese hamster Binding pKi = 9 9.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
44404268 72153 None 0 Human Binding pKi = 9 9.0 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 517 4 0 7 4.3 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN6CCC[C@@H]6C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL197947 72153 None 0 Human Binding pKi = 9 9.0 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 517 4 0 7 4.3 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN6CCC[C@@H]6C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
9957274 135301 None 0 Human Binding pKi = 9 9.0 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 491 4 0 7 3.8 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL372743 135301 None 0 Human Binding pKi = 9 9.0 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 491 4 0 7 3.8 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
44404249 140361 None 0 Human Binding pKi = 9 9.0 -3 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 412 2 0 6 2.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn3ccccc23)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL380812 140361 None 0 Human Binding pKi = 9 9.0 -3 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 412 2 0 6 2.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn3ccccc23)CC4)CC1 10.1016/j.bmcl.2005.06.042
5 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970645i
5202 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970645i
CHEMBL39 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970645i
DB08839 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm970645i
5 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm981112s
5202 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm981112s
CHEMBL39 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm981112s
DB08839 139 None 72 Rat Binding pKi = 9.0 9.0 -13 54
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm981112s
10665156 108979 None 0 Human Binding pKi = 9.0 9.0 8 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 344 11 1 3 4.9 CCCCCCCCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL321190 108979 None 0 Human Binding pKi = 9.0 9.0 8 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 344 11 1 3 4.9 CCCCCCCCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
5 139 None 72 Human Binding pKi = 9.0 9.0 -11 54
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm7011722
5202 139 None 72 Human Binding pKi = 9.0 9.0 -11 54
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm7011722
CHEMBL39 139 None 72 Human Binding pKi = 9.0 9.0 -11 54
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm7011722
DB08839 139 None 72 Human Binding pKi = 9.0 9.0 -11 54
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm7011722
59636758 125678 None 0 Chinese hamster Binding pKi = 9.0 9.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 511 7 1 7 4.3 O=C(Nc1ccc(N2CCOCC2)cc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647260 125678 None 0 Chinese hamster Binding pKi = 9.0 9.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 511 7 1 7 4.3 O=C(Nc1ccc(N2CCOCC2)cc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
106 148 None 26 Human Binding pKi = 8.9 8.9 4 6
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
1797 148 None 26 Human Binding pKi = 8.9 8.9 4 6
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
CHEMBL97450 148 None 26 Human Binding pKi = 8.9 8.9 4 6
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
1809 134 None 32 Human Binding pKi = 8.9 8.9 -15 36
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cellsBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
4 134 None 32 Human Binding pKi = 8.9 8.9 -15 36
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cellsBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
CHEMBL18840 134 None 32 Human Binding pKi = 8.9 8.9 -15 36
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cellsBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm0341204
49850673 56392 None 0 Human Binding pKi = 8.9 8.9 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.5 CCOC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631538 56392 None 0 Human Binding pKi = 8.9 8.9 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 418 6 1 5 4.5 CCOC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49852001 56459 None 0 Human Binding pKi = 8.9 8.9 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 6 1 4 4.3 CCC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632207 56459 None 0 Human Binding pKi = 8.9 8.9 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 6 1 4 4.3 CCC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49850567 56469 None 0 Human Binding pKi = 8.9 8.9 -6 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632217 56469 None 0 Human Binding pKi = 8.9 8.9 -6 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 452 6 1 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cnccn5)c4)CC3)cccc2n1 10.1021/jm100714c
49850570 56472 None 0 Human Binding pKi = 8.9 8.9 -7 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632220 56472 None 0 Human Binding pKi = 8.9 8.9 -7 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 417 6 2 4 4.0 CCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
44580740 187762 None 0 Human Binding pKi = 8.9 8.9 1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL495703 187762 None 0 Human Binding pKi = 8.9 8.9 1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
10174199 187693 None 0 Human Binding pKi = 8.9 8.9 -3 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 481 9 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(=O)(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL495213 187693 None 0 Human Binding pKi = 8.9 8.9 -3 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 481 9 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(=O)(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
44404236 70556 None 0 Human Binding pKi = 8.9 8.9 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 406 2 0 4 3.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccccc2Cl)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL194809 70556 None 0 Human Binding pKi = 8.9 8.9 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 406 2 0 4 3.8 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccccc2Cl)CC4)CC1 10.1016/j.bmcl.2005.06.042
1042 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
148 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
443884.0 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
CHEMBL119443 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
DB01253 1581 None 23 Rat Binding pKi = 8.9 8.9 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C nan
19066163 11386 None 0 Human Binding pKi = 8.9 8.9 28 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 8.9 8.9 28 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 8.9 8.9 28 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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
24881752 171759 None 0 Human Binding pKi = 8.9 8.9 -1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL446745 171759 None 0 Human Binding pKi = 8.9 8.9 -1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
24881202 172586 None 0 Human Binding pKi = 8.9 8.9 -1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL448902 172586 None 0 Human Binding pKi = 8.9 8.9 -1 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
59636755 126212 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 392 5 0 5 3.2 Cc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
CHEMBL3650033 126212 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 392 5 0 5 3.2 Cc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
196129 67798 None 17 Rat Binding pKi = 8.9 8.9 -1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
CHEMBL1909065 67798 None 17 Rat Binding pKi = 8.9 8.9 -1 15
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 917 13 4 16 4.3 CO[C@H]1C[C@@H](O[C@H]2C[C@H]([C@H]3O[C@](C)(O)[C@H](C)C[C@@H]3C)O[C@H]2[C@]2(C)CC[C@H]([C@]3(C)CC[C@]4(C[C@H](O)[C@@H](C)[C@@H]([C@@H](C)[C@@H]5O[C@](O)(CC(=O)O)[C@@H](C)[C@H](OC)[C@H]5OC)O4)O3)O2)O[C@@H](C)[C@@H]1OC nan
59636746 125699 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 502 6 0 8 3.6 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCN(c2nccs2)CC1 nan
CHEMBL3647281 125699 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 502 6 0 8 3.6 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCN(c2nccs2)CC1 nan
59636781 126218 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)n1 nan
CHEMBL3650039 126218 None 0 Chinese hamster Binding pKi = 8.9 8.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)n1 nan
10791125 18961 None 0 Human Binding pKi = 8.9 8.9 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
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 None 0 Human Binding pKi = 8.9 8.9 1 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
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
44342784 9827 None 0 Human Binding pKi = 8.8 8.8 -3 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 4 2 2 5.8 Cc1ccc(/N=C(\S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL113950 9827 None 0 Human Binding pKi = 8.8 8.8 -3 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 4 2 2 5.8 Cc1ccc(/N=C(\S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
44342506 10125 None 0 Human Binding pKi = 8.8 8.8 -2 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL115663 10125 None 0 Human Binding pKi = 8.8 8.8 -2 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.2 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
44402887 71734 None 0 Human Binding pKi = 8.8 8.8 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196600 71734 None 0 Human Binding pKi = 8.8 8.8 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
10577268 82389 None 0 Human Binding pKi = 8.8 8.8 15 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 498 8 1 7 5.1 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4cc5c(c(OCCN(C)C)c4)OCC5)cc3)c(C)c2)no1 10.1021/jm970457s
CHEMBL21724 82389 None 0 Human Binding pKi = 8.8 8.8 15 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 498 8 1 7 5.1 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4cc5c(c(OCCN(C)C)c4)OCC5)cc3)c(C)c2)no1 10.1021/jm970457s
49850772 56399 None 0 Human Binding pKi = 8.8 8.8 -10 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631545 56399 None 0 Human Binding pKi = 8.8 8.8 -10 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 397 5 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc(-n5cccn5)c4)CC3)cccc2n1 10.1021/jm100714c
49852002 56460 None 0 Human Binding pKi = 8.8 8.8 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 416 6 1 4 4.5 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632208 56460 None 0 Human Binding pKi = 8.8 8.8 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 416 6 1 4 4.5 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
49850984 56467 None 0 Human Binding pKi = 8.8 8.8 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1cccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)c1 10.1021/jm100714c
CHEMBL1632215 56467 None 0 Human Binding pKi = 8.8 8.8 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1cccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)c1 10.1021/jm100714c
44443131 93810 None 0 Human Binding pKi = 8.8 8.8 -3 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 464 6 0 6 3.2 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4F)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL247609 93810 None 0 Human Binding pKi = 8.8 8.8 -3 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 464 6 0 6 3.2 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4F)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
44443132 169484 None 0 Human Binding pKi = 8.8 8.8 -1 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 478 7 0 6 3.6 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)c(F)c21 10.1016/j.bmcl.2007.06.078
CHEMBL443060 169484 None 0 Human Binding pKi = 8.8 8.8 -1 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 478 7 0 6 3.6 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)c(F)c21 10.1016/j.bmcl.2007.06.078
10387420 187854 None 0 Human Binding pKi = 8.8 8.8 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL496317 187854 None 0 Human Binding pKi = 8.8 8.8 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
44404258 166159 None 0 Human Binding pKi = 8.8 8.8 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 5 0 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(CC)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL426285 166159 None 0 Human Binding pKi = 8.8 8.8 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 5 0 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(CC)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
10848041 9374 None 1 Human Binding pKi = 8.8 8.8 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 246 7 2 2 3.2 CCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111376 9374 None 1 Human Binding pKi = 8.8 8.8 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 246 7 2 2 3.2 CCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
49836002 126210 None 0 Chinese hamster Binding pKi = 8.8 8.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 460 5 0 5 3.4 CC(=O)N1CCc2cc(CCN3CCN(c4cccc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
CHEMBL3650031 126210 None 0 Chinese hamster Binding pKi = 8.8 8.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 460 5 0 5 3.4 CC(=O)N1CCc2cc(CCN3CCN(c4cccc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
9830790 201060 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 521 5 1 7 3.0 CCC(=O)N1CCN(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(N5CCN(C)CC5)c4o3)cc2)CC1 10.1021/jm901200t
CHEMBL602674 201060 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 521 5 1 7 3.0 CCC(=O)N1CCN(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(N5CCN(C)CC5)c4o3)cc2)CC1 10.1021/jm901200t
9830790 201060 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 521 5 1 7 3.0 CCC(=O)N1CCN(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(N5CCN(C)CC5)c4o3)cc2)CC1 10.1021/jm901200t
CHEMBL602674 201060 None 1 Human Binding pKi = 8.8 8.8 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 521 5 1 7 3.0 CCC(=O)N1CCN(c2ccc(NC(=O)c3cc(=O)c4cc(F)cc(N5CCN(C)CC5)c4o3)cc2)CC1 10.1021/jm901200t
19066203 12089 None 0 Human Binding pKi = 8.7 8.7 47 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 8.7 8.7 47 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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 None 0 Human Binding pKi = 8.7 8.7 47 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
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
59636750 125680 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 518 8 1 7 3.5 CS(=O)(=O)c1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
CHEMBL3647262 125680 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 518 8 1 7 3.5 CS(=O)(=O)c1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
59636703 125685 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
CHEMBL3647267 125685 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
44403095 135234 None 0 Human Binding pKi = 8.7 8.7 3 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL372453 135234 None 0 Human Binding pKi = 8.7 8.7 3 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(Cl)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10376578 121079 None 3 Human Binding pKi = 8.7 8.7 -4 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 230 3 2 1 3.2 CNCCc1c[nH]c2ccc(C(C)(C)C)cc12 10.1021/jm9805945
CHEMBL357034 121079 None 3 Human Binding pKi = 8.7 8.7 -4 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 230 3 2 1 3.2 CNCCc1c[nH]c2ccc(C(C)(C)C)cc12 10.1021/jm9805945
44402876 70888 None 0 Human Binding pKi = 8.7 8.7 6 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 492 4 0 5 5.2 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195114 70888 None 0 Human Binding pKi = 8.7 8.7 6 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 492 4 0 5 5.2 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
44402879 71408 None 0 Human Binding pKi = 8.7 8.7 50 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 445 4 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195898 71408 None 0 Human Binding pKi = 8.7 8.7 50 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 445 4 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
11304596 56396 None 0 Human Binding pKi = 8.7 8.7 -12 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631542 56396 None 0 Human Binding pKi = 8.7 8.7 -12 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 416 5 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc(N5CCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
49852000 56400 None 0 Human Binding pKi = 8.7 8.7 -3 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 452 8 1 5 4.1 CCCS(=O)(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631548 56400 None 0 Human Binding pKi = 8.7 8.7 -3 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 452 8 1 5 4.1 CCCS(=O)(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49852003 56461 None 0 Human Binding pKi = 8.7 8.7 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 1 4 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)C(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632209 56461 None 0 Human Binding pKi = 8.7 8.7 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 1 4 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)C(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
49850569 56471 None 0 Human Binding pKi = 8.7 8.7 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5scnc5C)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632219 56471 None 0 Human Binding pKi = 8.7 8.7 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5scnc5C)c4)CC3)cccc2n1 10.1021/jm100714c
49850571 56473 None 0 Human Binding pKi = 8.7 8.7 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 431 7 2 4 4.4 CCCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632221 56473 None 0 Human Binding pKi = 8.7 8.7 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 431 7 2 4 4.4 CCCNC(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
24865725 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL497963 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm100714c
10127424 176055 None 0 Human Binding pKi = 8.7 8.7 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL459061 176055 None 0 Human Binding pKi = 8.7 8.7 -1 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10319737 187763 None 0 Human Binding pKi = 8.7 8.7 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3C)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL495705 187763 None 0 Human Binding pKi = 8.7 8.7 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3C)cccc2n1 10.1016/j.bmcl.2008.08.084
24865725 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL497963 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10238566 190028 None 0 Human Binding pKi = 8.7 8.7 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 1 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL517170 190028 None 0 Human Binding pKi = 8.7 8.7 -3 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 1 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
24865725 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL497963 188084 None 0 Human Binding pKi = 8.7 8.7 -3 12
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 453 8 1 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(NS(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
44404244 72551 None 0 Human Binding pKi = 8.7 8.7 2 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 5 4.1 Cc1cc(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)c(C(F)(F)F)o1 10.1016/j.bmcl.2005.06.042
CHEMBL199175 72551 None 0 Human Binding pKi = 8.7 8.7 2 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 5 4.1 Cc1cc(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)c(C(F)(F)F)o1 10.1016/j.bmcl.2005.06.042
44404272 140891 None 0 Human Binding pKi = 8.7 8.7 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 517 4 0 7 4.3 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN6CCC[C@H]6C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL382078 140891 None 0 Human Binding pKi = 8.7 8.7 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 517 4 0 7 4.3 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN6CCC[C@H]6C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
130 3500 None 47 Human Binding pKi = 8 8.0 -1 13
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
3378093 3500 None 47 Human Binding pKi = 8 8.0 -1 13
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
CHEMBL281350 3500 None 47 Human Binding pKi = 8 8.0 -1 13
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/S0960-894X(97)10164-0
2389 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
5073.0 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
96 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
CHEMBL85 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
DB00734 3331 None 118 Human Binding pKi = 8 8.0 -93 67
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1039/C2MD00311B
2543 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
5358 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
5358.0 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
54 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
CHEMBL128 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
DB00669 3707 None 68 Human Binding pKi = 8 8.0 -3 32
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm950498t
127036 9360 None 12 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 229 1 3 2 1.1 NC(=O)c1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL111316 9360 None 12 Human Binding pKi = 8 8.0 - 1
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 229 1 3 2 1.1 NC(=O)c1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
10296414 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm049039v
76 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm049039v
CHEMBL183460 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm049039v
10296414 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
76 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
CHEMBL183460 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2006.11.031
10296414 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2007.06.078
76 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2007.06.078
CHEMBL183460 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2007.06.078
10296414 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2008.08.110
76 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2008.08.110
CHEMBL183460 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1016/j.bmcl.2008.08.110
10296414 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm8001444
76 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm8001444
CHEMBL183460 3531 None 15 Human Binding pKi = 8 8.0 -7 9
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 10.1021/jm8001444
130 3500 None 47 Human Binding pKi = 8 8.0 -1 13
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
3378093 3500 None 47 Human Binding pKi = 8 8.0 -1 13
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
CHEMBL281350 3500 None 47 Human Binding pKi = 8 8.0 -1 13
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
59636719 125695 None 0 Chinese hamster Binding pKi = 8 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 8 0 7 3.9 CN(Cc1cccc(S(C)(=O)=O)c1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647277 125695 None 0 Chinese hamster Binding pKi = 8 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 8 0 7 3.9 CN(Cc1cccc(S(C)(=O)=O)c1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
2393 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
5078 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
5078.0 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
51 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
CHEMBL905 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
DB00953 3334 None 82 Human Binding pKi = 8 8.0 -1 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9805945
1342 35 None 49 Human Binding pKi = 8 8.0 -4 19
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm9703552
3 35 None 49 Human Binding pKi = 8 8.0 -4 19
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm9703552
CHEMBL277120 35 None 49 Human Binding pKi = 8 8.0 -4 19
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm9703552
1251 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
7191 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
77992 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
77992.0 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
CHEMBL1279 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
DB00998 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 10.1021/jm9805945
44292375 169174 None 0 Human Binding pKi = 8.0 8.0 -36 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 3 1 1 3.9 CC(C)c1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL44054 169174 None 0 Human Binding pKi = 8.0 8.0 -36 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 3 1 1 3.9 CC(C)c1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
1342 35 None 49 Human Binding pKi = 8.0 8.0 -4 19
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/s0960-894x(98)00222-4
3 35 None 49 Human Binding pKi = 8.0 8.0 -4 19
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/s0960-894x(98)00222-4
CHEMBL277120 35 None 49 Human Binding pKi = 8.0 8.0 -4 19
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1016/s0960-894x(98)00222-4
11071135 208008 None 0 Human Binding pKi = 7 7.0 -45 7
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
CHEMBL97333 208008 None 0 Human Binding pKi = 7 7.0 -45 7
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 500 6 0 6 4.6 CN1CCC(CCN2CCC(c3cn(-c4ccc(F)cc4)c4ccc(-c5ncn(C)n5)cc34)CC2)C1=O 10.1021/jm020938y
22132503 101980 None 0 Human Binding pKi = 7 7.0 -25 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 521 9 2 5 4.4 O=C(/C=C/c1c[nH]c2ccccc12)NCCCCN1CCc2ccc(OS(=O)(=O)C(F)(F)F)cc2C1 10.1021/jm000090i
CHEMBL301475 101980 None 0 Human Binding pKi = 7 7.0 -25 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 521 9 2 5 4.4 O=C(/C=C/c1c[nH]c2ccccc12)NCCCCN1CCc2ccc(OS(=O)(=O)C(F)(F)F)cc2C1 10.1021/jm000090i
CHEMBL552599 101980 None 0 Human Binding pKi = 7 7.0 -25 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 521 9 2 5 4.4 O=C(/C=C/c1c[nH]c2ccccc12)NCCCCN1CCc2ccc(OS(=O)(=O)C(F)(F)F)cc2C1 10.1021/jm000090i
44400359 68685 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 6 0 7 3.0 Cc1ccc2c(OCCN3CCN(CN4C=CC5=CC(=O)CC=C5O4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL192176 68685 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 432 6 0 7 3.0 Cc1ccc2c(OCCN3CCN(CN4C=CC5=CC(=O)CC=C5O4)CC3)cccc2n1 10.1021/jm049039v
10159927 93970 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 432 6 1 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248457 93970 None 0 Human Binding pKi = 7 7.0 -10 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 432 6 1 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
24881617 188326 None 0 Human Binding pKi = 7 7.0 -165 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL500737 188326 None 0 Human Binding pKi = 7 7.0 -165 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
44593711 184323 None 0 Human Binding pKi = 7 7.0 1 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OCC(C)N3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484216 184323 None 0 Human Binding pKi = 7 7.0 1 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OCC(C)N3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
24865724 187964 None 0 Human Binding pKi = 7 7.0 -63 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 0 4 5.3 CCN(C(C)=O)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL497127 187964 None 0 Human Binding pKi = 7 7.0 -63 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 0 4 5.3 CCN(C(C)=O)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
181743 178572 None 5 Human Binding pKi = 7 7.0 -50 22
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL467094 178572 None 5 Human Binding pKi = 7 7.0 -50 22
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2015.07.012
181743 178572 None 5 Human Binding pKi = 7 7.0 -50 22
Displacement of [3H]GR127543 from human 5HT1B receptorDisplacement of [3H]GR127543 from human 5HT1B receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
CHEMBL467094 178572 None 5 Human Binding pKi = 7 7.0 -50 22
Displacement of [3H]GR127543 from human 5HT1B receptorDisplacement of [3H]GR127543 from human 5HT1B receptor
ChEMBL 339 2 0 5 3.2 COc1cc2c3c(c1OC)-c1cc4c(cc1CC3N(C)CC2)OCO4 10.1016/j.bmcl.2009.11.053
15124074 119697 None 0 Rat Binding pKi = 7 7.0 -14 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 394 6 0 4 3.4 CCc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL347334 119697 None 0 Rat Binding pKi = 7 7.0 -14 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 394 6 0 4 3.4 CCc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
10811696 102482 None 0 Human Binding pKi = 6 6.0 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)C2 10.1021/jm000090i
CHEMBL2368612 102482 None 0 Human Binding pKi = 6 6.0 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)C2 10.1021/jm000090i
CHEMBL3040263 102482 None 0 Human Binding pKi = 6 6.0 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CCN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)C2 10.1021/jm000090i
152 364 None 29 Rat Binding pKi = 6 6.0 -57 18
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00384a001
2107 364 None 29 Rat Binding pKi = 6 6.0 -57 18
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00384a001
CHEMBL275854 364 None 29 Rat Binding pKi = 6 6.0 -57 18
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00384a001
5475158 67213 None 25 Rat Binding pKi = 6 6.0 -1023 14
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 10.1021/jm00384a001
CHEMBL18786 67213 None 25 Rat Binding pKi = 6 6.0 -1023 14
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 10.1021/jm00384a001
10257042 204361 None 0 Human Binding pKi = 6 6.0 -25 7
Binding affinity for 5-hydroxytryptamine 1B receptor was determinedBinding affinity for 5-hydroxytryptamine 1B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
CHEMBL71707 204361 None 0 Human Binding pKi = 6 6.0 -25 7
Binding affinity for 5-hydroxytryptamine 1B receptor was determinedBinding affinity for 5-hydroxytryptamine 1B receptor was determined
ChEMBL 551 6 3 3 7.3 O=C(/C=C/c1ccc(Cl)c(Cl)c1)N[C@H]1CC[C@@H](CN2[C@H]3CC[C@@H]2C[C@@H](c2c[nH]c4ccc(O)cc24)C3)CC1 10.1016/s0960-894x(01)00397-3
242 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
34 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
60795.0 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
CHEMBL1112 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
DB01238 470 None 124 Human Binding pKi = 6 6.0 -380 51
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1039/C2MD00311B
135398737 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398737.0 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
38 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
722 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
CHEMBL42 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
DB00363 958 None 93 Human Binding pKi = 6 6.0 -151 89
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1039/C2MD00311B
135398745 2914 None 112 Human Binding pKi = 6 6.0 -199 65
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
135398745.0 2914 None 112 Human Binding pKi = 6 6.0 -199 65
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
47 2914 None 112 Human Binding pKi = 6 6.0 -199 65
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
CHEMBL715 2914 None 112 Human Binding pKi = 6 6.0 -199 65
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
DB00334 2914 None 112 Human Binding pKi = 6 6.0 -199 65
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1039/C2MD00311B
3233 3512 None 44 Human Binding pKi = 6 6.0 -741 12
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
3247 3512 None 44 Human Binding pKi = 6 6.0 -741 12
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
6604889 3512 None 44 Human Binding pKi = 6 6.0 -741 12
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
CHEMBL282199 3512 None 44 Human Binding pKi = 6 6.0 -741 12
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
DB13988 3512 None 44 Human Binding pKi = 6 6.0 -741 12
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.1021/jm991151j
10573876 10462 None 0 Human Binding pKi = 6 6.0 -501 7
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
CHEMBL116448 10462 None 0 Human Binding pKi = 6 6.0 -501 7
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 414 5 0 3 3.7 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc(Br)c2)CC1 10.1021/jm991151j
9934284 90296 None 0 Human Binding pKi = 6 6.0 -2511 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238520 90296 None 0 Human Binding pKi = 6 6.0 -2511 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
22326660 90771 None 0 Human Binding pKi = 6 6.0 -50 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 456 6 1 6 4.1 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cc(C#N)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL239167 90771 None 0 Human Binding pKi = 6 6.0 -50 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 456 6 1 6 4.1 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cc(C#N)cc2n1 10.1016/j.bmcl.2006.11.031
11046087 4947 None 0 Human Binding pKi = 6 6.0 -134 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccsc4)nc23)CC1 10.1021/jm030020m
CHEMBL104753 4947 None 0 Human Binding pKi = 6 6.0 -134 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccsc4)nc23)CC1 10.1021/jm030020m
11110452 5130 None 0 Human Binding pKi = 6 6.0 -158 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccn4)nc23)CC1 10.1021/jm030020m
CHEMBL105722 5130 None 0 Human Binding pKi = 6 6.0 -158 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccn4)nc23)CC1 10.1021/jm030020m
13520547 27004 None 1 Rat Binding pKi = 6 6.0 -2 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL136470 27004 None 1 Rat Binding pKi = 6 6.0 -2 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm00124a021
23274477 29121 None 1 Rat Binding pKi = 6 6.0 -3 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL138136 29121 None 1 Rat Binding pKi = 6 6.0 -3 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm00124a021
3198 205513 None 76 Rat Binding pKi = 5 5.0 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 205513 None 76 Rat Binding pKi = 5 5.0 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 205513 None 76 Rat Binding pKi = 5 5.0 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
117209971 186485 None 1 Human Binding pKi = 6.0 6.0 -20 5
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4877051 186485 None 1 Human Binding pKi = 6.0 6.0 -20 5
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 258 3 2 4 1.5 COc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
1150 3878 None 121 Rat Binding pKi = 5.0 5.0 -204 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00384a001
125 3878 None 121 Rat Binding pKi = 5.0 5.0 -204 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00384a001
CHEMBL6640 3878 None 121 Rat Binding pKi = 5.0 5.0 -204 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00384a001
DB08653 3878 None 121 Rat Binding pKi = 5.0 5.0 -204 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm00384a001
20255884 66063 None 0 Human Binding pKi = 5.0 5.0 -30 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 234 2 2 5 1.6 Cc1cc([N+](=O)[O-])cc(C)c1NC1=NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL183704 66063 None 0 Human Binding pKi = 5.0 5.0 -30 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 234 2 2 5 1.6 Cc1cc([N+](=O)[O-])cc(C)c1NC1=NCCN1 10.1016/j.bmcl.2004.06.085
24881550 172746 None 0 Human Binding pKi = 7.0 7.0 -4 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 726 10 4 4 9.0 O=C(Nc1ccc2[nH]cc(C3CCN(C/C=C/CN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL450852 172746 None 0 Human Binding pKi = 7.0 7.0 -4 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 726 10 4 4 9.0 O=C(Nc1ccc2[nH]cc(C3CCN(C/C=C/CN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
44431532 145237 None 0 Human Binding pKi = 7.0 7.0 -14 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL391271 145237 None 0 Human Binding pKi = 7.0 7.0 -14 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
11297 67345 None 18 Rat Binding pKi = 6.0 6.0 -26 6
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 10.1021/jm00384a001
CHEMBL18855 67345 None 18 Rat Binding pKi = 6.0 6.0 -26 6
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 10.1021/jm00384a001
44352308 117487 None 0 Human Binding pKi = 6.0 6.0 -131 12
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
CHEMBL339980 117487 None 0 Human Binding pKi = 6.0 6.0 -131 12
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT radioligand
ChEMBL 339 5 2 2 4.0 Cc1[nH]c2cccc(NC(=O)c3ccc(F)cc3)c2c1CCN(C)C 10.1021/jm0155190
44383729 59927 None 0 Human Binding pKi = 7.0 7.0 -23 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 294 4 1 2 4.3 C1=CCN(CCc2c[nH]c3ccc(-c4cccs4)cc23)C1 10.1016/s0960-894x(00)00133-5
CHEMBL173162 59927 None 0 Human Binding pKi = 7.0 7.0 -23 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 294 4 1 2 4.3 C1=CCN(CCc2c[nH]c3ccc(-c4cccs4)cc23)C1 10.1016/s0960-894x(00)00133-5
4431 2729 None 25 Rat Binding pKi = 6.0 6.0 -3090 12
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1021/jm00020a020
73 2729 None 25 Rat Binding pKi = 6.0 6.0 -3090 12
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1021/jm00020a020
CHEMBL8618 2729 None 25 Rat Binding pKi = 6.0 6.0 -3090 12
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 393 7 0 5 2.9 COc1ccccc1N1CCN(CC1)CCCCN1C(=O)c2c(C1=O)cccc2 10.1021/jm00020a020
134 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
1775 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
9681.0 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
CHEMBL1065 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
DB00247 2514 None 24 Rat Binding pKi = 7.0 7.0 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO nan
10015980 204317 None 0 Human Binding pKi = 7.0 7.0 -154 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 4 1 2 3.2 CCCN(C)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL71469 204317 None 0 Human Binding pKi = 7.0 7.0 -154 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 4 1 2 3.2 CCCN(C)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10065919 103090 None 0 Human Binding pKi = 6.0 6.0 -22 3
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
CHEMBL307521 103090 None 0 Human Binding pKi = 6.0 6.0 -22 3
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
10250307 22607 None 0 Rat Binding pKi = 6.0 6.0 -295 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 398 5 0 4 4.4 Clc1cccc2c1CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL132657 22607 None 0 Rat Binding pKi = 6.0 6.0 -295 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 398 5 0 4 4.4 Clc1cccc2c1CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
10896220 107530 None 0 Human Binding pKi = 8.0 8.0 -3 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1ccnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL318735 107530 None 0 Human Binding pKi = 8.0 8.0 -3 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1ccnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
44337731 11379 None 0 Human Binding pKi = 8.0 8.0 21 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 442 5 0 5 3.1 Cc1ccccc1N1CCN(C(=O)COc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL106807 11379 None 0 Human Binding pKi = 8.0 8.0 21 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 442 5 0 5 3.1 Cc1ccccc1N1CCN(C(=O)COc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1179968 11379 None 0 Human Binding pKi = 8.0 8.0 21 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 442 5 0 5 3.1 Cc1ccccc1N1CCN(C(=O)COc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
9862256 207120 None 0 Human Binding pKi = 8.0 8.0 -7 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL92139 207120 None 0 Human Binding pKi = 8.0 8.0 -7 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
44342823 113809 None 0 Human Binding pKi = 8.0 8.0 -2 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 4 2 2 5.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)NC45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL332484 113809 None 0 Human Binding pKi = 8.0 8.0 -2 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 4 2 2 5.6 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)NC45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
133 2496 None 52 Rat Binding pKi = 8.0 8.0 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
1723 2496 None 52 Rat Binding pKi = 8.0 8.0 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
28693 2496 None 52 Rat Binding pKi = 8.0 8.0 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
CHEMBL19215 2496 None 52 Rat Binding pKi = 8.0 8.0 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
DB13520 2496 None 52 Rat Binding pKi = 8.0 8.0 -40 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C nan
107715 200945 None 22 Rat Binding pKi = 8.0 8.0 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL1255837 200945 None 22 Rat Binding pKi = 8.0 8.0 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
CHEMBL601773 200945 None 22 Rat Binding pKi = 8.0 8.0 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O nan
10069802 102878 None 0 Human Binding pKi = 8.0 8.0 -9 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 404 9 1 3 5.2 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL305837 102878 None 0 Human Binding pKi = 8.0 8.0 -9 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 404 9 1 3 5.2 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10044965 204168 None 0 Human Binding pKi = 8.0 8.0 -18 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 374 8 1 2 5.2 CCCN(CCCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL70680 204168 None 0 Human Binding pKi = 8.0 8.0 -18 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 374 8 1 2 5.2 CCCN(CCCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
59636718 126226 None 0 Chinese hamster Binding pKi = 8.0 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 5 0 5 3.7 CN(C)C(=O)c1cc2c(Br)ccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650046 126226 None 0 Chinese hamster Binding pKi = 8.0 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 5 0 5 3.7 CN(C)C(=O)c1cc2c(Br)ccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44404394 132815 None 0 Human Binding pKi = 8.0 8.0 3 7
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL370128 132815 None 0 Human Binding pKi = 8.0 8.0 3 7
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 443 4 1 5 3.5 COc1ccc(NC(=O)N2CCN(c3ccccc3Cl)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
415628 208192 None 95 Rat Binding pKi = 7.9 7.9 2 5
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9841 208192 None 95 Rat Binding pKi = 7.9 7.9 2 5
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1ccccc1N1CCNCC1 10.1021/jm00125a020
11049209 207405 None 0 Human Binding pKi = 7.0 7.0 -223 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL93923 207405 None 0 Human Binding pKi = 7.0 7.0 -223 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1ccc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
44376492 119986 None 0 Human Binding pKi = 7.0 7.0 -11 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 469 6 1 3 4.9 O=S(=O)(c1ccc(Cl)cc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
CHEMBL349903 119986 None 0 Human Binding pKi = 7.0 7.0 -11 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 469 6 1 3 4.9 O=S(=O)(c1ccc(Cl)cc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
10198756 4870 None 1 Human Binding pKi = 7.0 7.0 -4 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 245 2 1 3 2.4 COc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL104374 4870 None 1 Human Binding pKi = 7.0 7.0 -4 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 245 2 1 3 2.4 COc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
10925382 5016 None 0 Human Binding pKi = 6.0 6.0 -85 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccco4)nc23)CC1 10.1021/jm030020m
CHEMBL105091 5016 None 0 Human Binding pKi = 6.0 6.0 -85 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccco4)nc23)CC1 10.1021/jm030020m
6422277 30036 None 5 Rat Binding pKi = 6.0 6.0 -28 4
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL138907 30036 None 5 Rat Binding pKi = 6.0 6.0 -28 4
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm00124a021
44383738 60266 None 0 Human Binding pKi = 7.0 7.0 -13 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 326 5 2 3 3.9 OC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL174141 60266 None 0 Human Binding pKi = 7.0 7.0 -13 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 326 5 2 3 3.9 OC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
122197403 133474 None 0 Human Binding pKi = 6.9 6.9 -8 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 433 5 1 4 4.3 C[C@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL3706923 133474 None 0 Human Binding pKi = 6.9 6.9 -8 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 433 5 1 4 4.3 C[C@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
9981270 165274 None 0 Human Binding pKi = 6.9 6.9 -40 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL423127 165274 None 0 Human Binding pKi = 6.9 6.9 -40 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
115 3791 None 80 Rat Binding pKi = 6.9 6.9 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
4296 3791 None 80 Rat Binding pKi = 6.9 6.9 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
CHEMBL274866 3791 None 80 Rat Binding pKi = 6.9 6.9 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
11662592 72344 None 0 Rat Binding pKi = 6.9 6.9 -97 9
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
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 None 0 Rat Binding pKi = 6.9 6.9 -97 9
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44292367 101869 None 0 Human Binding pKi = 6.9 6.9 -33 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 228 2 1 1 3.1 Cc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL300686 101869 None 0 Human Binding pKi = 6.9 6.9 -33 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 228 2 1 1 3.1 Cc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
10003971 63033 None 0 Human Binding pKi = 6.9 6.9 -199 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL1788198 63033 None 0 Human Binding pKi = 6.9 6.9 -199 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL5083607 214873 None 0 Human Binding pKi = 7.9 7.9 1 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCN(C)C2)ccc1Cl 10.1021/acs.jmedchem.1c00110
25067561 201092 None 4 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 466 5 1 7 2.6 COc1cc2c(c(N3CCN(C)CC3)c1)O[C@@H](C(=O)Nc1ccc(N3CCOCC3)cc1)CC2 10.1021/jm901200t
CHEMBL602875 201092 None 4 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 466 5 1 7 2.6 COc1cc2c(c(N3CCN(C)CC3)c1)O[C@@H](C(=O)Nc1ccc(N3CCOCC3)cc1)CC2 10.1021/jm901200t
44394222 127554 None 0 Human Binding pKi = 7.9 7.9 -39 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 245 1 2 3 3.0 Cc1cc(C(C)(C)C)cc(C)c1NC1=NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL366322 127554 None 0 Human Binding pKi = 7.9 7.9 -39 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 245 1 2 3 3.0 Cc1cc(C(C)(C)C)cc(C)c1NC1=NCCN1 10.1016/j.bmcl.2004.06.085
113 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
128018 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
CHEMBL119264 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
25067561 201092 None 4 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 466 5 1 7 2.6 COc1cc2c(c(N3CCN(C)CC3)c1)O[C@@H](C(=O)Nc1ccc(N3CCOCC3)cc1)CC2 10.1021/jm901200t
CHEMBL602875 201092 None 4 Human Binding pKi = 7.9 7.9 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 466 5 1 7 2.6 COc1cc2c(c(N3CCN(C)CC3)c1)O[C@@H](C(=O)Nc1ccc(N3CCOCC3)cc1)CC2 10.1021/jm901200t
10478367 71670 None 0 Human Binding pKi = 7.9 7.9 19 7
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196370 71670 None 0 Human Binding pKi = 7.9 7.9 19 7
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL430500 71670 None 0 Human Binding pKi = 7.9 7.9 19 7
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
44402874 133546 None 0 Human Binding pKi = 7.9 7.9 19 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 447 3 0 4 4.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL370896 133546 None 0 Human Binding pKi = 7.9 7.9 19 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 447 3 0 4 4.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
44444556 94402 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
CHEMBL250973 94402 None 0 Human Binding pKi = 7.9 7.9 - 1
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 471 6 0 5 4.4 CCOc1ccc(CC(=O)N2CCc3cc(OC)c(N4C[C@H](C)N(C)[C@H](C)C4)cc32)cc1Cl 10.1016/j.bmcl.2007.09.067
10436045 3516 None 4 Human Binding pKi = 7.9 7.9 -3 13
Binding affinity for 5-hydroxytryptamine 1B receptor was determinedBinding affinity for 5-hydroxytryptamine 1B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
782 3516 None 4 Human Binding pKi = 7.9 7.9 -3 13
Binding affinity for 5-hydroxytryptamine 1B receptor was determinedBinding affinity for 5-hydroxytryptamine 1B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
CHEMBL432713 3516 None 4 Human Binding pKi = 7.9 7.9 -3 13
Binding affinity for 5-hydroxytryptamine 1B receptor was determinedBinding affinity for 5-hydroxytryptamine 1B receptor was determined
ChEMBL 499 9 3 3 6.4 O=C(/C=C/c1ccc(c(c1)Cl)Cl)NCCCCCN1CCC(CC1)c1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(01)00397-3
10597210 77131 None 0 Human Binding pKi = 7.9 7.9 3 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 401 3 1 3 4.1 Cc1cc(C(=O)Nc2ccc(C)c(N3CCN(C)CC3)c2)ccc1Br 10.1021/jm970457s
CHEMBL20771 77131 None 0 Human Binding pKi = 7.9 7.9 3 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 401 3 1 3 4.1 Cc1cc(C(=O)Nc2ccc(C)c(N3CCN(C)CC3)c2)ccc1Br 10.1021/jm970457s
49850768 56393 None 0 Human Binding pKi = 7.9 7.9 -39 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 5 0 4 3.9 CC(=O)N(C)c1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1631539 56393 None 0 Human Binding pKi = 7.9 7.9 -39 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 402 5 0 4 3.9 CC(=O)N(C)c1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
10310285 189925 None 0 Human Binding pKi = 7.9 7.9 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5cccnc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL516997 189925 None 0 Human Binding pKi = 7.9 7.9 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5cccnc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
24865726 187656 None 0 Human Binding pKi = 7.9 7.9 -7 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 467 8 0 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(N(C)S(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL495046 187656 None 0 Human Binding pKi = 7.9 7.9 -7 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 467 8 0 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(N(C)S(C)(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
24865727 193113 None 0 Human Binding pKi = 7.9 7.9 -7 11
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL522708 193113 None 0 Human Binding pKi = 7.9 7.9 -7 11
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 479 7 0 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCS5(=O)=O)c4)CC3)cccc2n1 10.1021/jm8001444
56935645 67917 None 0 Human Binding pKi = 6.9 6.9 -2 2
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 553 5 1 6 5.1 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)CN3c2ccc(Cl)c(Cl)c2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2011.09.046
CHEMBL1910792 67917 None 0 Human Binding pKi = 6.9 6.9 -2 2
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 553 5 1 6 5.1 COc1ccc(NC(=O)c2ccc3c(c2)N(C)C(=O)CN3c2ccc(Cl)c(Cl)c2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2011.09.046
14083218 63051 None 7 Rat Binding pKi = 6.9 6.9 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
CHEMBL1788239 63051 None 7 Rat Binding pKi = 6.9 6.9 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
92042876 151336 None 0 Human Binding pKi = 5.9 5.9 -229 10
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL3961059 151336 None 0 Human Binding pKi = 5.9 5.9 -229 10
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 261 4 1 2 3.7 CNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
10020895 4705 None 0 Human Binding pKi = 5.9 5.9 -158 8
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL103479 4705 None 0 Human Binding pKi = 5.9 5.9 -158 8
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
10926112 172631 None 0 Human Binding pKi = 5.9 5.9 -208 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 2 3 3.9 Cc1cccc(C(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3n2)c1 10.1021/jm030020m
CHEMBL449406 172631 None 0 Human Binding pKi = 5.9 5.9 -208 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 2 3 3.9 Cc1cccc(C(=O)Nc2ccc3[nH]cc(C4CCN(C)CC4)c3n2)c1 10.1021/jm030020m
2274 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
4917.0 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
7279 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
CHEMBL728 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
DB00433 3173 None 58 Rat Binding pKi = 5.9 5.9 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 nan
145990586 166843 None 0 Human Binding pKi = 5.9 5.9 -93 11
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
CHEMBL4285281 166843 None 0 Human Binding pKi = 5.9 5.9 -93 11
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assayBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition of radioligand binding by radioligand competition binding assay
ChEMBL 297 2 2 4 2.6 COc1cc2c3c(c1OC)-c1ccccc1[C@@H](O)[C@@H]3NCC2 10.1039/C7MD00656J
10358224 204320 None 0 Human Binding pKi = 6.9 6.9 -52 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 313 5 1 2 4.2 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL71474 204320 None 0 Human Binding pKi = 6.9 6.9 -52 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 313 5 1 2 4.2 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
53248361 62082 None 0 Human Binding pKi = 6.9 6.9 -77 7
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
CHEMBL1774991 62082 None 0 Human Binding pKi = 6.9 6.9 -77 7
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 568 7 0 5 3.2 COc1ccccc1N1CCN(CCN(C(=O)C23C4C5C2C2C3C4C52I)c2ccccn2)CC1 10.1021/jm1009956
73213196 104460 None 4 Human Binding pKi = 5.9 5.9 -11 13
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104460 None 4 Human Binding pKi = 5.9 5.9 -11 13
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
73213196 104460 None 4 Human Binding pKi = 5.9 5.9 -11 13
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104093 104460 None 4 Human Binding pKi = 5.9 5.9 -11 13
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.9 CN1CCc2c(c3cccc4c3n2CCc2ccccc2-4)C1 10.1016/j.bmcl.2013.12.024
2812 4779 None 101 Rat Binding pKi = 4.9 4.9 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
CHEMBL104 4779 None 101 Rat Binding pKi = 4.9 4.9 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
62597539 106212 None 2 Human Binding pKi = 5.9 5.9 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 307 4 1 2 2.8 CNCCOc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL2260923 106212 None 2 Human Binding pKi = 5.9 5.9 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 307 4 1 2 2.8 CNCCOc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL3138772 106212 None 2 Human Binding pKi = 5.9 5.9 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 307 4 1 2 2.8 CNCCOc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
11794624 80212 None 1 Human Binding pKi = 6.9 6.9 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 387 3 1 3 3.8 Cc1cc(C(=O)Nc2cccc(N3CCN(C)CC3)c2)ccc1Br 10.1021/jm970457s
CHEMBL21369 80212 None 1 Human Binding pKi = 6.9 6.9 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 387 3 1 3 3.8 Cc1cc(C(=O)Nc2cccc(N3CCN(C)CC3)c2)ccc1Br 10.1021/jm970457s
10310423 175496 None 0 Human Binding pKi = 6.9 6.9 -50 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 445 7 0 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCOCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL457765 175496 None 0 Human Binding pKi = 6.9 6.9 -50 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 445 7 0 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCOCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10238763 175694 None 0 Human Binding pKi = 6.9 6.9 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)C(=O)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL458200 175694 None 0 Human Binding pKi = 6.9 6.9 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)C(=O)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44580784 188086 None 0 Human Binding pKi = 6.9 6.9 -501 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2008.08.084
CHEMBL497979 188086 None 0 Human Binding pKi = 6.9 6.9 -501 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2008.08.084
9891617 207982 None 0 Human Binding pKi = 5.9 5.9 -1000 5
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
CHEMBL97211 207982 None 0 Human Binding pKi = 5.9 5.9 -1000 5
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 4.9 Cc1cc(N2CCNCC2)c2cc(NS(=O)(=O)c3sc4ccc(Cl)cc4c3C)ccc2n1 10.1016/s0960-894x(01)00558-3
10413595 161841 None 0 Human Binding pKi = 5.9 5.9 -3981 11
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
CHEMBL414628 161841 None 0 Human Binding pKi = 5.9 5.9 -3981 11
Compound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as the radioligandCompound was evaluated for binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as the radioligand
ChEMBL 499 4 1 5 2.5 COc1ccc(S(=O)(=O)N2CCc3ccc(I)cc32)cc1N1CCNCC1 10.1016/s0960-894x(00)00597-7
10115848 90770 None 0 Human Binding pKi = 5.9 5.9 -794 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 465 6 1 5 4.9 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL239166 90770 None 0 Human Binding pKi = 5.9 5.9 -794 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 465 6 1 5 4.9 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
24865540 187676 None 0 Human Binding pKi = 5.9 5.9 -7 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
CHEMBL495160 187676 None 0 Human Binding pKi = 5.9 5.9 -7 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
24881618 188787 None 0 Human Binding pKi = 6.9 6.9 -125 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL505750 188787 None 0 Human Binding pKi = 6.9 6.9 -125 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
24881619 189038 None 0 Human Binding pKi = 6.9 6.9 -9 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL509314 189038 None 0 Human Binding pKi = 6.9 6.9 -9 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
277 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
2913.0 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
765 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
CHEMBL516 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
DB00434 1301 None 62 Rat Binding pKi = 5.9 5.9 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
50878551 90745 None 61 Human Binding pKi = 6.9 6.9 -7 18
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 None 61 Human Binding pKi = 6.9 6.9 -7 18
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
50878551 90745 None 61 Human Binding pKi = 6.9 6.9 -7 18
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
CHEMBL2391541 90745 None 61 Human Binding pKi = 6.9 6.9 -7 18
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2013.03.066
44342783 9819 None 0 Human Binding pKi = 7.9 7.9 -6 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C4CCCCC4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL113868 9819 None 0 Human Binding pKi = 7.9 7.9 -6 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C4CCCCC4)CC3)cc12 10.1016/s0960-894x(03)00779-0
3658 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
517 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
5709 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
5709.0 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
CHEMBL312448 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
DB06694 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1016/j.bmcl.2004.06.085
106 148 None 26 Rat Binding pKi = 7.9 7.9 -4 6
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
1797 148 None 26 Rat Binding pKi = 7.9 7.9 -4 6
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
CHEMBL97450 148 None 26 Rat Binding pKi = 7.9 7.9 -4 6
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10.1021/jm00044a001
52942395 17921 None 0 Human Binding pKi = 7.9 7.9 -24 5
Displacement of [3H]CT from human 5-HT1B receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]CT from human 5-HT1B receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
CHEMBL1259203 17921 None 0 Human Binding pKi = 7.9 7.9 -24 5
Displacement of [3H]CT from human 5-HT1B receptor expressed in human HeLa cells after 60 mins by scintillation counting analysisDisplacement of [3H]CT from human 5-HT1B receptor expressed in human HeLa cells after 60 mins by scintillation counting analysis
ChEMBL 386 3 0 4 5.0 CN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1016/j.bmc.2012.10.049
10643939 14111 None 0 Human Binding pKi = 7.9 7.9 35 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
CHEMBL119800 14111 None 0 Human Binding pKi = 7.9 7.9 35 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
44403101 71997 None 0 Human Binding pKi = 7.9 7.9 -2 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL197408 71997 None 0 Human Binding pKi = 7.9 7.9 -2 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 485 5 1 5 4.5 COc1ccc(NC(=O)N2CCN(c3ccc(-c4ccccc4)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
83357 98172 None 69 Rat Binding pKi = 7.9 7.9 -1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 206 3 1 3 1.5 CCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL273923 98172 None 69 Rat Binding pKi = 7.9 7.9 -1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 206 3 1 3 1.5 CCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
44376494 56262 None 0 Human Binding pKi = 6.9 6.9 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 420 6 2 3 4.5 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
CHEMBL162771 56262 None 0 Human Binding pKi = 6.9 6.9 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 420 6 2 3 4.5 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
10163458 85182 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 490 6 2 8 3.1 CNc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(OC)cc12 10.1016/j.bmc.2006.10.037
CHEMBL225364 85182 None 0 Human Binding pKi = 5.9 5.9 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 490 6 2 8 3.1 CNc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(OC)cc12 10.1016/j.bmc.2006.10.037
10089261 102474 None 0 Rat Binding pKi = 5.9 5.9 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 350 4 0 4 4.5 CN(C)CCSc1nc2ccccc2c2c1CCOc1ccccc1-2 10.1021/jm00014a021
CHEMBL304016 102474 None 0 Rat Binding pKi = 5.9 5.9 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 350 4 0 4 4.5 CN(C)CCSc1nc2ccccc2c2c1CCOc1ccccc1-2 10.1021/jm00014a021
206 2493 None 16 Rat Binding pKi = 4.9 4.9 -7585 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm00384a001
68848 2493 None 16 Rat Binding pKi = 4.9 4.9 -7585 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm00384a001
CHEMBL12314 2493 None 16 Rat Binding pKi = 4.9 4.9 -7585 25
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C 10.1021/jm00384a001
72550642 114078 None 0 Human Binding pKi = 6.9 6.9 -15 8
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326982 114078 None 0 Human Binding pKi = 6.9 6.9 -15 8
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 491 10 1 4 5.6 COc1ccccc1N1CCN(CCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
44461249 205351 None 0 Human Binding pKi = 6.9 6.9 -15 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 421 5 2 3 4.3 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL79674 205351 None 0 Human Binding pKi = 6.9 6.9 -15 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 421 5 2 3 4.3 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44269026 33744 None 0 Rat Binding pKi = 5.9 5.9 -363 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 458 6 0 4 3.7 COc1cccc2c1C1CCN(CCCCN3C(=O)C4C5C=CC(C6C=CC65)C4C3=O)CC1C2 10.1021/jm00027a013
CHEMBL14224 33744 None 0 Rat Binding pKi = 5.9 5.9 -363 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 458 6 0 4 3.7 COc1cccc2c1C1CCN(CCCCN3C(=O)C4C5C=CC(C6C=CC65)C4C3=O)CC1C2 10.1021/jm00027a013
CHEMBL1743629 33744 None 0 Rat Binding pKi = 5.9 5.9 -363 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 458 6 0 4 3.7 COc1cccc2c1C1CCN(CCCCN3C(=O)C4C5C=CC(C6C=CC65)C4C3=O)CC1C2 10.1021/jm00027a013
10016747 60298 None 0 Human Binding pKi = 6.9 6.9 -40 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 284 4 1 2 4.3 Cc1ccc(-c2ccc3[nH]cc(CCN(C)C)c3c2)s1 10.1016/s0960-894x(00)00133-5
CHEMBL174355 60298 None 0 Human Binding pKi = 6.9 6.9 -40 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 284 4 1 2 4.3 Cc1ccc(-c2ccc3[nH]cc(CCN(C)C)c3c2)s1 10.1016/s0960-894x(00)00133-5
127036186 137414 None 0 Human Binding pKi = 5.9 5.9 -42 19
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3753318 137414 None 0 Human Binding pKi = 5.9 5.9 -42 19
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 254 7 1 1 3.7 C=CCN(CC=C)CCc1c[nH]c2ccc(C)cc12 10.1016/j.bmcl.2015.12.053
21509921 104458 None 0 Human Binding pKi = 5.9 5.9 -131 24
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 None 0 Human Binding pKi = 5.9 5.9 -131 24
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
10498633 163303 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 358 15 2 2 6.2 CCCCCCCCCOc1ccc2[nH]cc(CCNCCCC)c2c1 10.1021/jm950498t
CHEMBL418823 163303 None 0 Human Binding pKi = 6.9 6.9 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 358 15 2 2 6.2 CCCCCCCCCOc1ccc2[nH]cc(CCNCCCC)c2c1 10.1021/jm950498t
CHEMBL1200558 208599 None 21 Rat Binding pKi = 5.9 5.9 - 1
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL None None None CC[C@H](C)[C@H](N)C1=N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](C(=O)N[C@H]2CCCCNC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](Cc3cnc[nH]3)NC(=O)[C@@H](Cc3ccccc3)NC(=O)[C@H]([C@@H](C)CC)NC(=O)[C@@H](CCCN)NC2=O)[C@@H](C)CC)CS1 nan
125957 120160 None 8 Rat Binding pKi = 6.9 6.9 -1 2
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
CHEMBL351530 120160 None 8 Rat Binding pKi = 6.9 6.9 -1 2
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
14975319 77234 None 0 Rat Binding pKi = 4.9 4.9 -245 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
CHEMBL2079545 77234 None 0 Rat Binding pKi = 4.9 4.9 -245 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
21509921 104458 None 0 Human Binding pKi = 5.9 5.9 -131 24
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104091 104458 None 0 Human Binding pKi = 5.9 5.9 -131 24
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
6761 67799 None 19 Rat Binding pKi = 5.9 5.9 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
CHEMBL1909072 67799 None 19 Rat Binding pKi = 5.9 5.9 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 nan
117209962 184869 None 1 Human Binding pKi = 5.9 5.9 -52 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4852622 184869 None 1 Human Binding pKi = 5.9 5.9 -52 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 242 2 2 3 1.8 Cc1ccc(-c2n[nH]cc2N2CCNCC2)cc1 10.1021/acs.jmedchem.1c01093
448779 63068 None 35 Rat Binding pKi = 5.9 5.9 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 174 2 2 1 2.1 C[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00402a026
CHEMBL1788285 63068 None 35 Rat Binding pKi = 5.9 5.9 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 174 2 2 1 2.1 C[C@@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00402a026
10858566 102087 None 1 Human Binding pKi = 6.9 6.9 -22 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL302172 102087 None 1 Human Binding pKi = 6.9 6.9 -22 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
10858566 102087 None 1 Human Binding pKi = 6.9 6.9 -22 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL302172 102087 None 1 Human Binding pKi = 6.9 6.9 -22 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
11826976 207528 None 1 Human Binding pKi = 7.9 7.9 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 483 6 1 4 5.0 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cccnc4)cc23)CC1 10.1021/jm020938y
CHEMBL94612 207528 None 1 Human Binding pKi = 7.9 7.9 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 483 6 1 4 5.0 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cccnc4)cc23)CC1 10.1021/jm020938y
113 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
128018 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
CHEMBL119264 1852 None 14 Human Binding pKi = 7.9 7.9 39 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10.1021/jm9702948
44342727 10171 None 0 Human Binding pKi = 7.9 7.9 -18 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 465 6 1 4 4.3 COc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL115941 10171 None 0 Human Binding pKi = 7.9 7.9 -18 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 465 6 1 4 4.3 COc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
44342705 110114 None 0 Human Binding pKi = 7.9 7.9 -4 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 420 4 2 2 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)NC4CCCCC4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL323603 110114 None 0 Human Binding pKi = 7.9 7.9 -4 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 420 4 2 2 4.9 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)NC4CCCCC4)CC3)cc12 10.1016/s0960-894x(03)00779-0
3658 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
517 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
5709 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
5709.0 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
CHEMBL312448 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
DB06694 4107 None 53 Human Binding pKi = 7.9 7.9 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1021/jm970513p
10518850 35193 None 0 Human Binding pKi = 7.9 7.9 -2 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143512 35193 None 0 Human Binding pKi = 7.9 7.9 -2 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
5 139 None 72 Human Binding pKi = 7.9 7.9 -11 54
Displacement of [125I]CYP from human 5HT1B receptorDisplacement of [125I]CYP from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
5202 139 None 72 Human Binding pKi = 7.9 7.9 -11 54
Displacement of [125I]CYP from human 5HT1B receptorDisplacement of [125I]CYP from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
CHEMBL39 139 None 72 Human Binding pKi = 7.9 7.9 -11 54
Displacement of [125I]CYP from human 5HT1B receptorDisplacement of [125I]CYP from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
DB08839 139 None 72 Human Binding pKi = 7.9 7.9 -11 54
Displacement of [125I]CYP from human 5HT1B receptorDisplacement of [125I]CYP from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm2006782
10828231 9354 None 2 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 302 10 2 2 4.7 CC(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111283 9354 None 2 Human Binding pKi = 7.9 7.9 2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 302 10 2 2 4.7 CC(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
11740144 63032 None 0 Human Binding pKi = 7.9 7.9 -15 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 374 8 1 2 5.2 CCCN(CCCc1ccccc1)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL1788197 63032 None 0 Human Binding pKi = 7.9 7.9 -15 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 374 8 1 2 5.2 CCCN(CCCc1ccccc1)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
11098166 109787 None 0 Human Binding pKi = 7.9 7.9 -5 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 287 2 3 3 2.1 CNC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL323264 109787 None 0 Human Binding pKi = 7.9 7.9 -5 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 287 2 3 3 2.1 CNC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
59636721 126222 None 0 Chinese hamster Binding pKi = 7.9 7.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 472 5 0 5 3.6 CC(=O)N1CCc2cc(CCN3CCN(c4cccc5cc(C(=O)N6CCC6)oc45)CC3)ccc21 nan
CHEMBL3650042 126222 None 0 Chinese hamster Binding pKi = 7.9 7.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 472 5 0 5 3.6 CC(=O)N1CCc2cc(CCN3CCN(c4cccc5cc(C(=O)N6CCC6)oc45)CC3)ccc21 nan
2762737 101850 None 20 Human Binding pKi = 7.9 7.9 -35 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 230 4 1 1 3.4 CC(C)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL300519 101850 None 20 Human Binding pKi = 7.9 7.9 -35 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 230 4 1 1 3.4 CC(C)c1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
44376280 119903 None 0 Human Binding pKi = 6.9 6.9 -11 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 449 6 1 3 4.6 Cc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL349174 119903 None 0 Human Binding pKi = 6.9 6.9 -11 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 449 6 1 3 4.6 Cc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
44376588 119952 None 0 Human Binding pKi = 6.9 6.9 -12 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 465 7 1 4 4.3 COc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL349675 119952 None 0 Human Binding pKi = 6.9 6.9 -12 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 465 7 1 4 4.3 COc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
59636711 126225 None 0 Chinese hamster Binding pKi = 6.9 6.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cc(N2CCN(CCc3ccccn3)CC2)c2oc(C(=O)N(C)C)cc2c1 nan
CHEMBL3650045 126225 None 0 Chinese hamster Binding pKi = 6.9 6.9 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cc(N2CCN(CCc3ccccn3)CC2)c2oc(C(=O)N(C)C)cc2c1 nan
10683472 199387 None 0 Rat Binding pKi = 5.9 5.9 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 2.4 N#CC1=Cc2cccc(OCC3CCCNC3)c2OC1 10.1021/jm970806i
CHEMBL59102 199387 None 0 Rat Binding pKi = 5.9 5.9 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 2.4 N#CC1=Cc2cccc(OCC3CCCNC3)c2OC1 10.1021/jm970806i
10066481 18476 None 0 Rat Binding pKi = 5.9 5.9 -371 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 2 0 4 3.1 c1ccc2c(c1)CC(N1CCN(c3cccc4c3OCCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL127216 18476 None 0 Rat Binding pKi = 5.9 5.9 -371 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 2 0 4 3.1 c1ccc2c(c1)CC(N1CCN(c3cccc4c3OCCCO4)CC1)C2 10.1021/jm00020a020
10247055 116140 None 0 Rat Binding pKi = 5.9 5.9 -501 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 346 5 0 3 4.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
CHEMBL335752 116140 None 0 Rat Binding pKi = 5.9 5.9 -501 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 346 5 0 3 4.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
3191 102858 None 97 Rat Binding pKi = 5.9 5.9 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
3191.0 102858 None 97 Rat Binding pKi = 5.9 5.9 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
CHEMBL305660 102858 None 97 Rat Binding pKi = 5.9 5.9 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
DB11742 102858 None 97 Rat Binding pKi = 5.9 5.9 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 nan
10062659 204174 None 1 Human Binding pKi = 6.9 6.9 -93 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL70710 204174 None 1 Human Binding pKi = 6.9 6.9 -93 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
12406830 65272 None 2 Human Binding pKi = 5.8 5.8 -26 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 267 1 2 1 2.2 Cc1cc(Br)cc(C)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL182837 65272 None 2 Human Binding pKi = 5.8 5.8 -26 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 267 1 2 1 2.2 Cc1cc(Br)cc(C)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
132060743 162236 None 0 Human Binding pKi = 5.8 5.8 -5 13
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4163428 162236 None 0 Human Binding pKi = 5.8 5.8 -5 13
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 351 3 0 4 3.1 CN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)C3)CC1 10.1016/j.ejmech.2018.02.024
1971 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543.0 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 2866 None 38 Rat Binding pKi = 5.8 5.8 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
76326512 106250 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 376 4 0 3 2.8 CN1CCN(CCOc2ccc(Br)cc2Br)CC1 10.1007/s00044-009-9164-1
CHEMBL2260924 106250 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 376 4 0 3 2.8 CN1CCN(CCOc2ccc(Br)cc2Br)CC1 10.1007/s00044-009-9164-1
CHEMBL3138935 106250 None 0 Human Binding pKi = 5.8 5.8 - 1
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 376 4 0 3 2.8 CN1CCN(CCOc2ccc(Br)cc2Br)CC1 10.1007/s00044-009-9164-1
44438464 147140 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 508 7 1 7 4.9 OCC1(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CCCC1 10.1016/j.bmcl.2006.12.109
CHEMBL392770 147140 None 0 Human Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 508 7 1 7 4.9 OCC1(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CCCC1 10.1016/j.bmcl.2006.12.109
44431537 145241 None 0 Human Binding pKi = 7.8 7.8 -15 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 3.6 N#Cc1ccc2c(N3CCN(CC[C@@H]4OCCc5cc(C(N)=O)ccc54)CC3)cccc2c1 10.1016/j.bmcl.2007.03.101
CHEMBL391273 145241 None 0 Human Binding pKi = 7.8 7.8 -15 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 3.6 N#Cc1ccc2c(N3CCN(CC[C@@H]4OCCc5cc(C(N)=O)ccc54)CC3)cccc2c1 10.1016/j.bmcl.2007.03.101
11200511 201730 None 0 Human Binding pKi = 7.8 7.8 -15 8
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
CHEMBL606547 201730 None 0 Human Binding pKi = 7.8 7.8 -15 8
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3ccccc3Cl)cc12 10.1021/jm049243i
10068933 103801 None 0 Human Binding pKi = 7.8 7.8 -3 4
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
CHEMBL309021 103801 None 0 Human Binding pKi = 7.8 7.8 -3 4
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
44292365 188110 None 0 Human Binding pKi = 7.8 7.8 -61 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 2 1 1 4.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C(C)(C)C)cc12 10.1016/s0960-894x(00)00322-x
CHEMBL49826 188110 None 0 Human Binding pKi = 7.8 7.8 -61 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 2 1 1 4.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C(C)(C)C)cc12 10.1016/s0960-894x(00)00322-x
69836292 79018 None 0 Human Binding pKi = 7.8 7.8 15 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 438 5 0 6 3.3 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL2113098 79018 None 0 Human Binding pKi = 7.8 7.8 15 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 438 5 0 6 3.3 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
10238565 190926 None 0 Human Binding pKi = 7.8 7.8 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 1 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN[C@@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL518545 190926 None 0 Human Binding pKi = 7.8 7.8 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 1 5 4.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN[C@@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10194809 188126 None 0 Human Binding pKi = 7.8 7.8 -25 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 8 1 4 5.2 CCC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL498354 188126 None 0 Human Binding pKi = 7.8 7.8 -25 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 8 1 4 5.2 CCC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
44404230 70519 None 0 Human Binding pKi = 7.8 7.8 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 440 2 0 4 4.2 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccccc2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL194701 70519 None 0 Human Binding pKi = 7.8 7.8 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 440 2 0 4 4.2 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2ccccc2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
44404245 71908 None 0 Human Binding pKi = 7.8 7.8 -6 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 391 2 0 6 2.8 Cc1nc(C)c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)o1 10.1016/j.bmcl.2005.06.042
CHEMBL197169 71908 None 0 Human Binding pKi = 7.8 7.8 -6 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 391 2 0 6 2.8 Cc1nc(C)c(C(=O)N2CCc3cc4ccnc(N5CCN(C)CC5)c4cc32)o1 10.1016/j.bmcl.2005.06.042
10774576 208243 None 7 Rat Binding pKi = 7.8 7.8 1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 3 1 2 2.0 CCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9870 208243 None 7 Rat Binding pKi = 7.8 7.8 1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 3 1 2 2.0 CCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
10048252 11380 None 0 Human Binding pKi = 6.8 6.8 -41 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 428 3 0 5 3.7 Cc1ccccc1N1CCN(C(=O)Oc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL107772 11380 None 0 Human Binding pKi = 6.8 6.8 -41 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 428 3 0 5 3.7 Cc1ccccc1N1CCN(C(=O)Oc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1179973 11380 None 0 Human Binding pKi = 6.8 6.8 -41 2
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 428 3 0 5 3.7 Cc1ccccc1N1CCN(C(=O)Oc2ccc(Cl)c(N3CCN(C)CC3)c2)CC1 10.1016/S0960-894X(97)10164-0
11035452 5004 None 0 Human Binding pKi = 6.8 6.8 -12 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 2 3 3.9 Cc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105025 5004 None 0 Human Binding pKi = 6.8 6.8 -12 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 348 3 2 3 3.9 Cc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
10759257 100176 None 0 Rat Binding pKi = 5.8 5.8 7 2
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 335 1 0 4 3.8 CN1CCN(c2nc3ccccc3c3c2CCc2sccc2-3)CC1 10.1021/jm981112s
CHEMBL288069 100176 None 0 Rat Binding pKi = 5.8 5.8 7 2
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 335 1 0 4 3.8 CN1CCN(c2nc3ccccc3c3c2CCc2sccc2-3)CC1 10.1021/jm981112s
3604129 30264 None 5 Rat Binding pKi = 5.8 5.8 -19 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL139103 30264 None 5 Rat Binding pKi = 5.8 5.8 -19 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
10398118 102121 None 0 Human Binding pKi = 5.8 5.8 -11 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 207 3 1 1 2.7 CCCNC1CCc2cc(F)ccc2C1 10.1021/jm00012a021
CHEMBL302373 102121 None 0 Human Binding pKi = 5.8 5.8 -11 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 207 3 1 1 2.7 CCCNC1CCc2cc(F)ccc2C1 10.1021/jm00012a021
10088157 22879 None 0 Rat Binding pKi = 5.8 5.8 -1071 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 332 4 0 3 4.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
CHEMBL132878 22879 None 0 Rat Binding pKi = 5.8 5.8 -1071 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 332 4 0 3 4.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
854157 77864 None 15 Rat Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 174 2 2 1 2.1 C[C@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00402a026
CHEMBL2093087 77864 None 15 Rat Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 174 2 2 1 2.1 C[C@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00402a026
10070281 205561 None 0 Human Binding pKi = 6.8 6.8 -28 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 412 5 1 3 4.7 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL81191 205561 None 0 Human Binding pKi = 6.8 6.8 -28 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 412 5 1 3 4.7 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
752521 198737 None 8 Human Binding pKi = 5.8 5.8 -74 9
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
CHEMBL582877 198737 None 8 Human Binding pKi = 5.8 5.8 -74 9
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 295 1 3 5 1.9 CC1(C)N=C(N)N=C(Nc2cccc(Br)c2)N1 10.1021/acs.jmedchem.5b01631
14083215 63067 None 2 Rat Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
CHEMBL1788284 63067 None 2 Rat Binding pKi = 5.8 5.8 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
44461149 205369 None 0 Human Binding pKi = 6.8 6.8 -4 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 421 5 1 5 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2noc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL79853 205369 None 0 Human Binding pKi = 6.8 6.8 -4 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 421 5 1 5 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2noc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44461298 205715 None 0 Human Binding pKi = 6.8 6.8 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 1 4 4.5 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2coc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL82488 205715 None 0 Human Binding pKi = 6.8 6.8 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 1 4 4.5 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2coc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
31703 194717 None 63 Rat Binding pKi = 4.8 4.8 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL359744 194717 None 63 Rat Binding pKi = 4.8 4.8 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
CHEMBL53463 194717 None 63 Rat Binding pKi = 4.8 4.8 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 nan
9795333 103075 None 0 Human Binding pKi = 5.8 5.8 -21 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 266 2 1 2 2.6 Cc1cc(Br)cc(C)c1CC1=NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL307408 103075 None 0 Human Binding pKi = 5.8 5.8 -21 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 266 2 1 2 2.6 Cc1cc(Br)cc(C)c1CC1=NCCN1 10.1016/j.bmcl.2004.06.085
9795333 103075 None 0 Human Binding pKi = 5.8 5.8 -21 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 266 2 1 2 2.6 Cc1cc(Br)cc(C)c1CC1=NCCN1 10.1021/jm970513p
CHEMBL307408 103075 None 0 Human Binding pKi = 5.8 5.8 -21 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 266 2 1 2 2.6 Cc1cc(Br)cc(C)c1CC1=NCCN1 10.1021/jm970513p
46945446 17762 None 0 Human Binding pKi = 5.8 5.8 5 2
Inhibition of 5-HT1B receptorInhibition of 5-HT1B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
CHEMBL1258723 17762 None 0 Human Binding pKi = 5.8 5.8 5 2
Inhibition of 5-HT1B receptorInhibition of 5-HT1B receptor
ChEMBL 408 9 0 5 4.6 CCCCOc1ccc(-c2nn3c(C)cc(C)nc3c2CC(=O)N(CC)CC)cc1 10.1016/j.bmcl.2010.07.135
22132555 13708 None 0 Human Binding pKi = 6.8 6.8 -12 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 398 7 2 3 4.0 N#Cc1ccc2c(c1)CN(CCCCNC(=O)/C=C/c1c[nH]c3ccccc13)CC2 10.1021/jm000090i
CHEMBL1194956 13708 None 0 Human Binding pKi = 6.8 6.8 -12 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 398 7 2 3 4.0 N#Cc1ccc2c(c1)CN(CCCCNC(=O)/C=C/c1c[nH]c3ccccc13)CC2 10.1021/jm000090i
CHEMBL553591 13708 None 0 Human Binding pKi = 6.8 6.8 -12 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 398 7 2 3 4.0 N#Cc1ccc2c(c1)CN(CCCCNC(=O)/C=C/c1c[nH]c3ccccc13)CC2 10.1021/jm000090i
10597855 84389 None 0 Human Binding pKi = 6.8 6.8 -125 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)CC2 10.1021/jm000090i
CHEMBL2113350 84389 None 0 Human Binding pKi = 6.8 6.8 -125 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)CC2 10.1021/jm000090i
CHEMBL2219579 84389 None 0 Human Binding pKi = 6.8 6.8 -125 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 413 6 1 3 4.7 N#Cc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccccc3)CC1)CC2 10.1021/jm000090i
10194297 78989 None 0 Human Binding pKi = 6.8 6.8 -50 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4ccc5[nH]ccc5c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL2113061 78989 None 0 Human Binding pKi = 6.8 6.8 -50 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4ccc5[nH]ccc5c4)CC3)cccc2n1 10.1021/jm049039v
10115847 91980 None 0 Human Binding pKi = 6.8 6.8 -3 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 465 6 1 5 4.9 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(Cl)c2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241500 91980 None 0 Human Binding pKi = 6.8 6.8 -3 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 465 6 1 5 4.9 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(Cl)c2n1 10.1016/j.bmcl.2006.11.031
44581604 176059 None 0 Human Binding pKi = 6.8 6.8 -39 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 485 7 0 4 5.6 CC(=O)N1CCC(c2cccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)c2)CC1 10.1016/j.bmcl.2008.11.052
CHEMBL459068 176059 None 0 Human Binding pKi = 6.8 6.8 -39 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 485 7 0 4 5.6 CC(=O)N1CCC(c2cccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)c2)CC1 10.1016/j.bmcl.2008.11.052
10174088 189498 None 0 Human Binding pKi = 6.8 6.8 -100 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)O[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL513955 189498 None 0 Human Binding pKi = 6.8 6.8 -100 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)O[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10172853 187646 None 0 Human Binding pKi = 6.8 6.8 -63 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL494992 187646 None 0 Human Binding pKi = 6.8 6.8 -63 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
9954121 96406 None 0 Human Binding pKi = 5.8 5.8 -2511 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL261917 96406 None 0 Human Binding pKi = 5.8 5.8 -2511 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 424 4 2 5 3.7 CC(C)(C)c1ccc(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)cc1 10.1016/s0960-894x(01)00558-3
9863250 17995 None 6 Human Binding pKi = 5.8 5.8 -512 7
Binding affinity towards 5-hydroxytryptamine 1B (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 350 5 0 3 3.3 Cc1cccc(S(=O)(=O)N2CCC[C@@H]2CCN2CCC(C)CC2)c1 10.1021/jm991151j
CHEMBL12624 17995 None 6 Human Binding pKi = 5.8 5.8 -512 7
Binding affinity towards 5-hydroxytryptamine 1B (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 350 5 0 3 3.3 Cc1cccc(S(=O)(=O)N2CCC[C@@H]2CCN2CCC(C)CC2)c1 10.1021/jm991151j
10835110 114588 None 0 Human Binding pKi = 5.8 5.8 -398 8
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 404 5 0 3 4.3 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm991151j
CHEMBL333784 114588 None 0 Human Binding pKi = 5.8 5.8 -398 8
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 404 5 0 3 4.3 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2ccc(Cl)c(Cl)c2)CC1 10.1021/jm991151j
11248705 90295 None 0 Human Binding pKi = 5.8 5.8 -630 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238519 90295 None 0 Human Binding pKi = 5.8 5.8 -630 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
24865541 187677 None 0 Human Binding pKi = 5.8 5.8 -316 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1ccccc1CN1CCN(CCOc2cccc3nc(C)ccc23)CC1 10.1021/jm8001444
CHEMBL495161 187677 None 0 Human Binding pKi = 5.8 5.8 -316 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1ccccc1CN1CCN(CCOc2cccc3nc(C)ccc23)CC1 10.1021/jm8001444
10543269 26587 None 0 Rat Binding pKi = 5.8 5.8 -3 3
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 314 3 1 5 1.7 OCCN1CCN(c2nc3cccc(F)c3n3cccc23)CC1 10.1021/jm990151g
CHEMBL136108 26587 None 0 Rat Binding pKi = 5.8 5.8 -3 3
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 314 3 1 5 1.7 OCCN1CCN(c2nc3cccc(F)c3n3cccc23)CC1 10.1021/jm990151g
24881201 186849 None 0 Human Binding pKi = 7.8 7.8 -4 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
CHEMBL489453 186849 None 0 Human Binding pKi = 7.8 7.8 -4 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 10.1021/jm7011722
59636729 125691 None 0 Chinese hamster Binding pKi = 7.8 7.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 5 0 5 3.0 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCC1 nan
CHEMBL3647273 125691 None 0 Chinese hamster Binding pKi = 7.8 7.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 5 0 5 3.0 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCC1 nan
10786335 12060 None 0 Human Binding pKi = 7.8 7.8 63 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
CHEMBL118360 12060 None 0 Human Binding pKi = 7.8 7.8 63 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
44403105 72108 None 0 Human Binding pKi = 7.8 7.8 19 5
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 455 5 1 6 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(SC)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL197796 72108 None 0 Human Binding pKi = 7.8 7.8 19 5
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 455 5 1 6 3.5 COc1ccc(NC(=O)N2CCN(c3ccc(SC)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL5084249 214905 None 0 Human Binding pKi = 6.8 6.8 -19 8
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCN(CC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5094493 215499 None 0 Human Binding pKi = 6.8 6.8 -7 7
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCN(CCC)CCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11810310 4718 None 0 Human Binding pKi = 5.8 5.8 -144 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(F)c4)nc23)CC1 10.1021/jm030020m
CHEMBL103550 4718 None 0 Human Binding pKi = 5.8 5.8 -144 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(F)c4)nc23)CC1 10.1021/jm030020m
122187375 123023 None 0 Human Binding pKi = 5.8 5.8 -5 2
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609140 123023 None 0 Human Binding pKi = 5.8 5.8 -5 2
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 443 5 0 5 5.6 CCCOc1c(OC)cc2c3c1-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
10049500 77821 None 0 Human Binding pKi = 5.8 5.8 -1071 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL2092864 77821 None 0 Human Binding pKi = 5.8 5.8 -1071 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL2112317 77821 None 0 Human Binding pKi = 5.8 5.8 -1071 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
15870567 186973 None 0 Human Binding pKi = 5.8 5.8 -36 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 4 1 1 3.4 CCc1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL49048 186973 None 0 Human Binding pKi = 5.8 5.8 -36 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 4 1 1 3.4 CCc1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
14639163 204198 None 4 Human Binding pKi = 5.8 5.8 - 1
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 190 3 1 3 1.2 COc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
CHEMBL70831 204198 None 4 Human Binding pKi = 5.8 5.8 - 1
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 190 3 1 3 1.2 COc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
168268877 189970 None 0 Human Binding pKi = 6.8 6.8 -35 12
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5170784 189970 None 0 Human Binding pKi = 6.8 6.8 -35 12
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 328 2 3 3 3.8 COc1ccc(C2NCCc3c2[nH]c2ccc(Cl)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
10425027 204212 None 0 Human Binding pKi = 5.8 5.8 -31 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 302 5 0 2 4.3 CCCN(CCC)C1CCc2cc(F)c3c(ccn3C)c2C1 10.1021/jm00012a021
CHEMBL70882 204212 None 0 Human Binding pKi = 5.8 5.8 -31 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 302 5 0 2 4.3 CCCN(CCC)C1CCc2cc(F)c3c(ccn3C)c2C1 10.1021/jm00012a021
16117151 60087 None 0 Human Binding pKi = 5.8 5.8 -1659 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1642882 60087 None 0 Human Binding pKi = 5.8 5.8 -1659 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
CHEMBL1739102 60087 None 0 Human Binding pKi = 5.8 5.8 -1659 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
14547415 100671 None 1 Human Binding pKi = 5.8 5.8 -10 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL292274 100671 None 1 Human Binding pKi = 5.8 5.8 -10 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
180 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160.0 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 401 None 56 Rat Binding pKi = 5.8 5.8 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
44214329 59439 None 0 Human Binding pKi = 7.8 7.8 -33 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3ccsc3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL171129 59439 None 0 Human Binding pKi = 7.8 7.8 -33 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3ccsc3)cc12 10.1016/s0960-894x(00)00133-5
44342969 10528 None 0 Human Binding pKi = 7.8 7.8 -21 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 449 5 1 3 4.6 Cc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL116876 10528 None 0 Human Binding pKi = 7.8 7.8 -21 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 449 5 1 3 4.6 Cc1ccc(S(=O)(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
59636726 125706 None 0 Chinese hamster Binding pKi = 7.8 7.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 8 1 7 2.9 Cn1cnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647288 125706 None 0 Chinese hamster Binding pKi = 7.8 7.8 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 8 1 7 2.9 Cn1cnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
2477 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
2477.0 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
36 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
437 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
CHEMBL49 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
DB00490 745 None 59 Rat Binding pKi = 7.8 7.8 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
2303 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
4946 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
564 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
63 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
91536 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL27 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL452861 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
DB00571 3187 None 68 Rat Binding pKi = 7.8 7.8 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
1346 83 None 117 Rat Binding pKi = 7.8 7.8 -40 9
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
280 83 None 117 Rat Binding pKi = 7.8 7.8 -40 9
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
9899402 83 None 117 Rat Binding pKi = 7.8 7.8 -40 9
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9666 83 None 117 Rat Binding pKi = 7.8 7.8 -40 9
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
44376283 56508 None 0 Human Binding pKi = 6.8 6.8 -5 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
CHEMBL163516 56508 None 0 Human Binding pKi = 6.8 6.8 -5 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
11465618 102398 None 23 Rat Binding pKi = 6.8 6.8 -630 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 102398 None 23 Rat Binding pKi = 6.8 6.8 -630 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 102398 None 23 Rat Binding pKi = 6.8 6.8 -630 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
22184640 85177 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 519 8 2 7 3.5 CCN1CCC(N(CC)c2cc(OC)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)C1 10.1016/j.bmc.2006.10.037
CHEMBL225310 85177 None 0 Human Binding pKi = 6.8 6.8 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 519 8 2 7 3.5 CCN1CCC(N(CC)c2cc(OC)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)C1 10.1016/j.bmc.2006.10.037
11011968 4941 None 0 Human Binding pKi = 5.8 5.8 -173 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 2 3 2.7 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CC4)nc23)CC1 10.1021/jm030020m
CHEMBL104720 4941 None 0 Human Binding pKi = 5.8 5.8 -173 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 2 3 2.7 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CC4)nc23)CC1 10.1021/jm030020m
10618751 35190 None 0 Human Binding pKi = 6.8 6.8 -4 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.
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 None 0 Human Binding pKi = 6.8 6.8 -4 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10496545 9327 None 0 Human Binding pKi = 6.8 6.8 13 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 328 9 2 2 5.1 CCCCCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL111107 9327 None 0 Human Binding pKi = 6.8 6.8 13 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 328 9 2 2 5.1 CCCCCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL4520788 213975 None 10 Human Binding pKi = 5.8 5.8 -83 25
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR1BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR1B
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
10088038 204356 None 0 Human Binding pKi = 6.8 6.8 -30 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 7 1 1 5.2 CCCc1c[nH]c2c(F)cc3c(c12)CC(N(CCC)CCC)CC3 10.1021/jm00012a021
CHEMBL71663 204356 None 0 Human Binding pKi = 6.8 6.8 -30 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 7 1 1 5.2 CCCc1c[nH]c2c(F)cc3c(c12)CC(N(CCC)CCC)CC3 10.1021/jm00012a021
132787 3430 None 45 Rat Binding pKi = 5.8 5.8 -1000 6
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
26 3430 None 45 Rat Binding pKi = 5.8 5.8 -1000 6
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
32 3430 None 45 Rat Binding pKi = 5.8 5.8 -1000 6
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
CHEMBL49247 3430 None 45 Rat Binding pKi = 5.8 5.8 -1000 6
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
127026052 137553 None 0 Human Binding pKi = 5.8 5.8 -107 19
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 137553 None 0 Human Binding pKi = 5.8 5.8 -107 19
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
107992 2553 None 49 Rat Binding pKi = 6.8 6.8 -12 10
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
165 2553 None 49 Rat Binding pKi = 6.8 6.8 -12 10
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
CHEMBL269521 2553 None 49 Rat Binding pKi = 6.8 6.8 -12 10
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
DB12111 2553 None 49 Rat Binding pKi = 6.8 6.8 -12 10
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
10064361 204164 None 0 Human Binding pKi = 6.8 6.8 -223 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL70652 204164 None 0 Human Binding pKi = 6.8 6.8 -223 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
19066188 12098 None 0 Human Binding pKi = 7.8 7.8 19 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1183944 12098 None 0 Human Binding pKi = 7.8 7.8 19 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL325131 12098 None 0 Human Binding pKi = 7.8 7.8 19 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
24882268 172557 None 0 Human Binding pKi = 7.8 7.8 -11 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL448555 172557 None 0 Human Binding pKi = 7.8 7.8 -11 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
5 139 None 72 Human Binding pKi = 7.8 7.8 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
5202 139 None 72 Human Binding pKi = 7.8 7.8 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
CHEMBL39 139 None 72 Human Binding pKi = 7.8 7.8 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
DB08839 139 None 72 Human Binding pKi = 7.8 7.8 -11 54
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
44404396 71457 None 0 Human Binding pKi = 7.7 7.7 5 5
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196169 71457 None 0 Human Binding pKi = 7.7 7.7 5 5
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10643939 14111 None 0 Human Binding pKi = 7.7 7.7 35 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
CHEMBL119800 14111 None 0 Human Binding pKi = 7.7 7.7 35 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
25263302 191984 None 0 Human Binding pKi = 5.8 5.8 -1380 5
Binding affinity to 5HT1b receptorBinding affinity to 5HT1b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 191984 None 0 Human Binding pKi = 5.8 5.8 -1380 5
Binding affinity to 5HT1b receptorBinding affinity to 5HT1b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
14011047 59029 None 22 Rat Binding pKi = 5.8 5.8 -446 2
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 274 8 1 2 3.8 CCCN(CCC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm00399a031
CHEMBL169328 59029 None 22 Rat Binding pKi = 5.8 5.8 -446 2
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 274 8 1 2 3.8 CCCN(CCC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm00399a031
14519865 31587 None 1 Rat Binding pKi = 5.8 5.8 -39 4
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL140417 31587 None 1 Rat Binding pKi = 5.8 5.8 -39 4
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
117209857 185138 None 1 Human Binding pKi = 5.7 5.7 -43 8
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 185138 None 1 Human Binding pKi = 5.7 5.7 -43 8
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
2726 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
2726.0 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 919 None 68 Rat Binding pKi = 5.7 5.7 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
44455426 155149 None 0 Human Binding pKi = 5.7 5.7 -26 12
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 155149 None 0 Human Binding pKi = 5.7 5.7 -26 12
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44460810 205623 None 0 Human Binding pKi = 6.7 6.7 -48 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 436 5 1 4 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2csc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL81703 205623 None 0 Human Binding pKi = 6.7 6.7 -48 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 436 5 1 4 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2csc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
9949568 123430 None 0 Human Binding pKi = 5.7 5.7 -61 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 334 4 0 2 5.1 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCN1Cc1ccccc1 10.1016/j.bmcl.2004.06.085
CHEMBL361729 123430 None 0 Human Binding pKi = 5.7 5.7 -61 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 334 4 0 2 5.1 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCN1Cc1ccccc1 10.1016/j.bmcl.2004.06.085
10068238 19719 None 0 Rat Binding pKi = 5.7 5.7 -1479 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 3.8 c1ccc2c(c1)CC(CCCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL130103 19719 None 0 Rat Binding pKi = 5.7 5.7 -1479 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 3.8 c1ccc2c(c1)CC(CCCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10432512 102389 None 0 Human Binding pKi = 6.7 6.7 -234 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 424 9 1 3 5.7 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL303921 102389 None 0 Human Binding pKi = 6.7 6.7 -234 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 424 9 1 3 5.7 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10517352 7628 None 0 Human Binding pKi = 6.7 6.7 5 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 286 6 2 2 3.9 CCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL108818 7628 None 0 Human Binding pKi = 6.7 6.7 5 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 286 6 2 2 3.9 CCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
10500422 78475 None 0 Human Binding pKi = 7.7 7.7 15 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
CHEMBL2111779 78475 None 0 Human Binding pKi = 7.7 7.7 15 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
73453 29616 None 24 Rat Binding pKi = 7.7 7.7 -26 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
CHEMBL1385840 29616 None 24 Rat Binding pKi = 7.7 7.7 -26 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
59636772 125676 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1ccccn1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647259 125676 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1ccccn1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
59636774 125705 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 7 3.3 Cc1ccnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)n1 nan
CHEMBL3647287 125705 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 7 3.3 Cc1ccnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)n1 nan
59636731 126220 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccc(F)cn4)CC3)c2o1 nan
CHEMBL3650040 126220 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccc(F)cn4)CC3)c2o1 nan
2543 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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
5358.0 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 68 Human Binding pKi = 7.7 7.7 -3 32
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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
44402875 70454 None 0 Human Binding pKi = 7.7 7.7 12 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 413 3 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL194610 70454 None 0 Human Binding pKi = 7.7 7.7 12 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 413 3 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.07.085
10161028 90772 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL239168 90772 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
10237964 187614 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL494806 187614 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
10216873 187800 None 0 Human Binding pKi = 7.7 7.7 -9 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 443 7 0 4 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL495895 187800 None 0 Human Binding pKi = 7.7 7.7 -9 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 443 7 0 4 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5=O)c4)CC3)cccc2n1 10.1021/jm8001444
10173263 193399 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 417 7 1 4 4.8 CC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL525712 193399 None 0 Human Binding pKi = 7.7 7.7 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 417 7 1 4 4.8 CC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
9867475 18013 None 0 Human Binding pKi = 6.7 6.7 -63 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 18013 None 0 Human Binding pKi = 6.7 6.7 -63 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
1524 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
197 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
3822 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
3822.0 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
88 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
CHEMBL51 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
DB12465 2181 None 96 Rat Binding pKi = 5.7 5.7 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
10016864 204248 None 0 Human Binding pKi = 6.7 6.7 -17 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 286 5 1 2 3.2 CCCN(CCC)C1CCc2ccc3c(c2C1)CC(=O)N3 10.1021/jm00012a021
CHEMBL71091 204248 None 0 Human Binding pKi = 6.7 6.7 -17 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 286 5 1 2 3.2 CCCN(CCC)C1CCc2ccc3c(c2C1)CC(=O)N3 10.1021/jm00012a021
10267412 204352 None 0 Human Binding pKi = 6.7 6.7 -323 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 310 6 1 2 4.0 CCCN(CC1CC1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL71640 204352 None 0 Human Binding pKi = 6.7 6.7 -323 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 310 6 1 2 4.0 CCCN(CC1CC1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
4656 122960 None 7 Human Binding pKi = 5.7 5.7 -39 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 355 1 2 1 2.8 Clc1cc(I)cc(Cl)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL360803 122960 None 7 Human Binding pKi = 5.7 5.7 -39 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 355 1 2 1 2.8 Clc1cc(I)cc(Cl)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
46905266 10174 None 0 Human Binding pKi = 6.7 6.7 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL1159649 10174 None 0 Human Binding pKi = 6.7 6.7 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
10427962 20828 None 0 Rat Binding pKi = 6.7 6.7 -114 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.3 c1ccc2c(c1)CCC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131011 20828 None 0 Rat Binding pKi = 6.7 6.7 -114 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.3 c1ccc2c(c1)CCC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
10287730 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
11259254 125169 None 0 Human Binding pKi = 6.7 6.7 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 440 7 0 6 4.3 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL364495 125169 None 0 Human Binding pKi = 6.7 6.7 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 440 7 0 6 4.3 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
44588720 184345 None 0 Human Binding pKi = 6.7 6.7 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OC(C)CN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484386 184345 None 0 Human Binding pKi = 6.7 6.7 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OC(C)CN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10287730 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
77 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
CHEMBL425190 3536 None 40 Human Binding pKi = 6.7 6.7 -251 12
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
173 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
5011 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
CHEMBL18772 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
10655811 204438 None 0 Human Binding pKi = 5.7 5.7 -1 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(CC2=NCCN2)c(C)c1O 10.1021/jm970513p
CHEMBL72167 204438 None 0 Human Binding pKi = 5.7 5.7 -1 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(CC2=NCCN2)c(C)c1O 10.1021/jm970513p
44444557 154686 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL399704 154686 None 0 Human Binding pKi = 5.7 5.7 - 1
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
6918603 207971 None 1 Human Binding pKi = 5.7 5.7 -999 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 207971 None 1 Human Binding pKi = 5.7 5.7 -999 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10127209 68658 None 0 Human Binding pKi = 5.7 5.7 1 2
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191980 68658 None 0 Human Binding pKi = 5.7 5.7 1 2
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)cccc2n1 10.1021/jm049039v
44439165 145753 None 0 Human Binding pKi = 5.7 5.7 -794 8
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391661 145753 None 0 Human Binding pKi = 5.7 5.7 -794 8
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL4576555 214017 None 5 Human Binding pKi = 5.7 5.7 -2 19
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
10478367 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL196370 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL430500 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
10478367 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196370 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL430500 71670 None 0 Human Binding pKi = 8.7 8.7 19 7
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10664203 5483 None 0 Human Binding pKi = 8.7 8.7 31 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 10 2 2 5.4 CC(C)(C)CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL107617 5483 None 0 Human Binding pKi = 8.7 8.7 31 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 10 2 2 5.4 CC(C)(C)CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636753 126215 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.1 CC(=O)c1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
CHEMBL3650036 126215 None 0 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.1 CC(=O)c1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
44351692 19456 None 6 Human Binding pKi = 8.7 8.7 -2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 242 2 1 3 2.3 COc1ccc2ccc(N3CCNCC3)cc2c1 10.1021/jm9703552
CHEMBL129661 19456 None 6 Human Binding pKi = 8.7 8.7 -2 3
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 242 2 1 3 2.3 COc1ccc2ccc(N3CCNCC3)cc2c1 10.1021/jm9703552
44279889 103194 None 0 Human Binding pKi = 8.7 8.7 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 510 7 0 6 5.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5cccc(N6CCN(C)CC6)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL30831 103194 None 0 Human Binding pKi = 8.7 8.7 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 510 7 0 6 5.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5cccc(N6CCN(C)CC6)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
1043 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
149 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
8223 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
8223.0 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
CHEMBL442 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
DB00696 1582 None 14 Human Binding pKi = 8.7 8.7 -29 28
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
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 10.1016/j.bmcl.2011.09.046
49848635 125687 None 3 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 378 5 0 5 2.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647269 125687 None 3 Chinese hamster Binding pKi = 8.7 8.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 378 5 0 5 2.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
115 3791 None 80 Rat Binding pKi = 8.7 8.7 1 27
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
4296 3791 None 80 Rat Binding pKi = 8.7 8.7 1 27
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
CHEMBL274866 3791 None 80 Rat Binding pKi = 8.7 8.7 1 27
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
10251722 11377 None 0 Human Binding pKi = 8.6 8.6 20 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL105970 11377 None 0 Human Binding pKi = 8.6 8.6 20 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1179958 11377 None 0 Human Binding pKi = 8.6 8.6 20 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
9928474 9333 None 0 Human Binding pKi = 8.6 8.6 6 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 9 2 2 5.0 CC(C)(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111150 9333 None 0 Human Binding pKi = 8.6 8.6 6 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 9 2 2 5.0 CC(C)(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636733 125702 None 0 Chinese hamster Binding pKi = 8.6 8.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647284 125702 None 0 Chinese hamster Binding pKi = 8.6 8.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
44342785 9835 None 0 Human Binding pKi = 8.6 8.6 -5 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 5 2 3 5.3 COc1ccc(NC(=S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL113994 9835 None 0 Human Binding pKi = 8.6 8.6 -5 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 5 2 3 5.3 COc1ccc(NC(=S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
59636730 126217 None 0 Chinese hamster Binding pKi = 8.6 8.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.0 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N5CCC5)oc34)CC2)n1 nan
CHEMBL3650038 126217 None 0 Chinese hamster Binding pKi = 8.6 8.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.0 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N5CCC5)oc34)CC2)n1 nan
5 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
5202 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
CHEMBL39 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
DB08839 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
44402883 72017 None 0 Human Binding pKi = 8.6 8.6 12 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 481 3 0 5 4.9 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL197505 72017 None 0 Human Binding pKi = 8.6 8.6 12 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 481 3 0 5 4.9 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402882 133009 None 0 Human Binding pKi = 8.6 8.6 19 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 496 3 1 4 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL370214 133009 None 0 Human Binding pKi = 8.6 8.6 19 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 496 3 1 4 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
44402884 135292 None 0 Human Binding pKi = 8.6 8.6 10 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 0 5 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL372731 135292 None 0 Human Binding pKi = 8.6 8.6 10 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 0 5 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
10791443 77194 None 0 Human Binding pKi = 8.6 8.6 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 7 1 7 5.0 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)N(CCN(C)C)CCO5)cc3)c(C)c2)no1 10.1021/jm970457s
CHEMBL20791 77194 None 0 Human Binding pKi = 8.6 8.6 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 7 1 7 5.0 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)N(CCN(C)C)CCO5)cc3)c(C)c2)no1 10.1021/jm970457s
10624768 99398 None 0 Human Binding pKi = 8.6 8.6 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 485 9 2 7 5.3 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1NCCN(C)C 10.1021/jm970457s
CHEMBL282693 99398 None 0 Human Binding pKi = 8.6 8.6 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 485 9 2 7 5.3 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1NCCN(C)C 10.1021/jm970457s
11328382 91983 None 0 Human Binding pKi = 8.6 8.6 -3 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241503 91983 None 0 Human Binding pKi = 8.6 8.6 -3 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
49850874 56462 None 0 Human Binding pKi = 8.6 8.6 -7 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632210 56462 None 0 Human Binding pKi = 8.6 8.6 -7 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
10477223 185017 None 0 Human Binding pKi = 8.6 8.6 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL485491 185017 None 0 Human Binding pKi = 8.6 8.6 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2008.08.084
44404253 135279 None 0 Human Binding pKi = 8.6 8.6 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 477 4 1 7 3.5 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCNCC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL372651 135279 None 0 Human Binding pKi = 8.6 8.6 -1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 477 4 1 7 3.5 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCNCC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
5 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
5202 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
CHEMBL39 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
DB08839 139 None 72 Rat Binding pKi = 8.6 8.6 -13 54
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
44279550 99805 None 0 Human Binding pKi = 8.6 8.6 -2 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 650 8 0 8 3.6 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(C(=O)COc5ccc6cccc(N7CCN(C)CC7)c6c5)CC4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL285402 99805 None 0 Human Binding pKi = 8.6 8.6 -2 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 650 8 0 8 3.6 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(C(=O)COc5ccc6cccc(N7CCN(C)CC7)c6c5)CC4)cc23)CC1 10.1016/s0960-894x(98)00222-4
11827039 207976 None 1 Human Binding pKi = 8.6 8.6 6 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1nncc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL97184 207976 None 1 Human Binding pKi = 8.6 8.6 6 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1nncc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
11038248 111475 None 0 Human Binding pKi = 7.7 7.7 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL327662 111475 None 0 Human Binding pKi = 7.7 7.7 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
11038263 112794 None 0 Human Binding pKi = 7.7 7.7 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL330603 112794 None 0 Human Binding pKi = 7.7 7.7 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
10060289 60315 None 1 Human Binding pKi = 7.7 7.7 -13 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 242 2 1 2 2.4 CN(C)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL1744040 60315 None 1 Human Binding pKi = 7.7 7.7 -13 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 242 2 1 2 2.4 CN(C)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
59636773 126216 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 435 6 1 6 2.9 CC(=O)Nc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
CHEMBL3650037 126216 None 0 Chinese hamster Binding pKi = 7.7 7.7 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 435 6 1 6 2.9 CC(=O)Nc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
10310103 107312 None 0 Human Binding pKi = 6.7 6.7 -51 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 107312 None 0 Human Binding pKi = 6.7 6.7 -51 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
44460826 170428 None 0 Human Binding pKi = 6.7 6.7 -5 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 439 5 1 5 4.4 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2nsc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL444843 170428 None 0 Human Binding pKi = 6.7 6.7 -5 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 439 5 1 5 4.4 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2nsc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44310169 204357 None 0 Human Binding pKi = 5.7 5.7 -26 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 264 5 1 2 3.4 CCCN(CCC)C1CCc2c(ccc(F)c2N)C1 10.1021/jm00012a021
CHEMBL71676 204357 None 0 Human Binding pKi = 5.7 5.7 -26 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 264 5 1 2 3.4 CCCN(CCC)C1CCc2c(ccc(F)c2N)C1 10.1021/jm00012a021
9802187 205848 None 0 Human Binding pKi = 6.7 6.7 -51 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2007.03.101
CHEMBL83617 205848 None 0 Human Binding pKi = 6.7 6.7 -51 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2007.03.101
137646281 157806 None 0 Human Binding pKi = 5.7 5.7 -4677 17
Displacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 157806 None 0 Human Binding pKi = 5.7 5.7 -4677 17
Displacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
10385009 20496 None 0 Rat Binding pKi = 6.7 6.7 -331 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CCC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130734 20496 None 0 Rat Binding pKi = 6.7 6.7 -331 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CCC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
164 1460 None 19 Rat Binding pKi = 5.7 5.7 -89 10
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
85875 1460 None 19 Rat Binding pKi = 5.7 5.7 -89 10
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
CHEMBL8600 1460 None 19 Rat Binding pKi = 5.7 5.7 -89 10
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
DB01528 1460 None 19 Rat Binding pKi = 5.7 5.7 -89 10
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
9827354 112590 None 0 Human Binding pKi = 6.7 6.7 -5 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL330171 112590 None 0 Human Binding pKi = 6.7 6.7 -5 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
173 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
5011 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
CHEMBL18772 3262 None 95 Rat Binding pKi = 6.7 6.7 -2 23
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
10640199 8995 None 0 Human Binding pKi = 7.7 7.7 3 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 13 2 2 5.6 CCCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL109839 8995 None 0 Human Binding pKi = 7.7 7.7 3 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 13 2 2 5.6 CCCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44431536 87321 None 0 Human Binding pKi = 7.7 7.7 -23 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 454 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL233210 87321 None 0 Human Binding pKi = 7.7 7.7 -23 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 454 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
2735875 98483 None 92 Rat Binding pKi = 7.7 7.7 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 187 1 1 3 1.0 N#Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL275943 98483 None 92 Rat Binding pKi = 7.7 7.7 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 187 1 1 3 1.0 N#Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
10870264 204348 None 1 Human Binding pKi = 6.7 6.7 -389 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL71625 204348 None 1 Human Binding pKi = 6.7 6.7 -389 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL5074880 214339 None 0 Human Binding pKi = 6.7 6.7 -21 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44461297 169266 None 0 Human Binding pKi = 6.7 6.7 -8 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 2 4 3.6 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2[nH]nc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL441259 169266 None 0 Human Binding pKi = 6.7 6.7 -8 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 2 4 3.6 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2[nH]nc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44461425 205859 None 0 Human Binding pKi = 6.7 6.7 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 430 5 1 3 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccc(F)cc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL83732 205859 None 0 Human Binding pKi = 6.7 6.7 -7 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 430 5 1 3 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccc(F)cc23)CC1 10.1016/j.bmcl.2004.03.003
9997154 21063 None 0 Rat Binding pKi = 6.7 6.7 -120 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 3 0 4 2.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131198 21063 None 0 Rat Binding pKi = 6.7 6.7 -120 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 3 0 4 2.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
899057 60323 None 7 Rat Binding pKi = 5.7 5.7 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@@H](C)N)c[nH]c2c1 10.1021/jm00402a026
CHEMBL1744073 60323 None 7 Rat Binding pKi = 5.7 5.7 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@@H](C)N)c[nH]c2c1 10.1021/jm00402a026
3117 207841 None 103 Rat Binding pKi = 5.7 5.7 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 207841 None 103 Rat Binding pKi = 5.7 5.7 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
10424220 102866 None 0 Human Binding pKi = 6.7 6.7 -151 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)C1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL305743 102866 None 0 Human Binding pKi = 6.7 6.7 -151 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)C1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL4576555 214017 None 5 Human Binding pKi = 5.7 5.7 -2 19
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
44582676 189779 None 0 Human Binding pKi = 5.7 5.7 -16 17
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 189779 None 0 Human Binding pKi = 5.7 5.7 -16 17
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
11778645 60316 None 0 Human Binding pKi = 6.7 6.7 -60 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 284 5 1 1 4.4 CCCN(CC(C)C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL1744041 60316 None 0 Human Binding pKi = 6.7 6.7 -60 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 284 5 1 1 4.4 CCCN(CC(C)C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
2543 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
5358 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
5358.0 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
54 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
CHEMBL128 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
DB00669 3707 None 68 Human Binding pKi = 7.7 7.7 -3 32
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta 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/jm9604890
10710400 9186 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 314 8 2 2 4.8 NCCc1c[nH]c2ccc(OCCCCC3CCCCC3)cc12 10.1021/jm950498t
CHEMBL110318 9186 None 0 Human Binding pKi = 7.7 7.7 2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 314 8 2 2 4.8 NCCc1c[nH]c2ccc(OCCCCC3CCCCC3)cc12 10.1021/jm950498t
10786335 12060 None 0 Human Binding pKi = 7.7 7.7 63 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
CHEMBL118360 12060 None 0 Human Binding pKi = 7.7 7.7 63 2
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
10917953 207988 None 0 Human Binding pKi = 6.7 6.7 -630 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 207988 None 0 Human Binding pKi = 6.7 6.7 -630 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
26987 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
26987.0 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 949 None 33 Rat Binding pKi = 6.7 6.7 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
24841480 183899 None 0 Human Binding pKi = 5.7 5.7 -1096 20
Antagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 183899 None 0 Human Binding pKi = 5.7 5.7 -1096 20
Antagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
6918542 204924 None 24 Human Binding pKi = 5.7 5.7 -2238 10
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL76237 204924 None 24 Human Binding pKi = 5.7 5.7 -2238 10
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
11743042 204050 None 0 Human Binding pKi = 6.7 6.7 -117 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 423 8 1 3 4.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL69943 204050 None 0 Human Binding pKi = 6.7 6.7 -117 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 423 8 1 3 4.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10400189 105655 None 0 Human Binding pKi = 6.6 6.6 -229 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 256 4 2 2 2.8 CCCNC1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL312525 105655 None 0 Human Binding pKi = 6.6 6.6 -229 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 256 4 2 2 2.8 CCCNC1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10468376 102086 None 1 Human Binding pKi = 5.6 5.6 -512 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL302171 102086 None 1 Human Binding pKi = 5.6 5.6 -512 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
10468376 102086 None 1 Human Binding pKi = 5.6 5.6 -512 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL302171 102086 None 1 Human Binding pKi = 5.6 5.6 -512 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
11948707 166167 None 0 Human Binding pKi = 6.6 6.6 -562 13
Binding affinity to 5HT1B receptor by radioligand binding assayBinding affinity to 5HT1B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 166167 None 0 Human Binding pKi = 6.6 6.6 -562 13
Binding affinity to 5HT1B receptor by radioligand binding assayBinding affinity to 5HT1B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
14547414 102284 None 1 Human Binding pKi = 6.6 6.6 -15 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL303339 102284 None 1 Human Binding pKi = 6.6 6.6 -15 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10245352 204233 None 0 Human Binding pKi = 6.6 6.6 -67 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 6 2 1 4.5 c1ccc(CCCNCC2CCc3ccc4[nH]ccc4c3C2)cc1 10.1021/jm00012a022
CHEMBL70980 204233 None 0 Human Binding pKi = 6.6 6.6 -67 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 6 2 1 4.5 c1ccc(CCCNCC2CCc3ccc4[nH]ccc4c3C2)cc1 10.1021/jm00012a022
25060119 104315 None 0 Rat Binding pKi = 5.6 5.6 -32359 7
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
CHEMBL3099899 104315 None 0 Rat Binding pKi = 5.6 5.6 -32359 7
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
10090960 21068 None 0 Rat Binding pKi = 6.6 6.6 -114 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 376 4 0 4 4.0 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CC1 10.1021/jm00020a020
CHEMBL131200 21068 None 0 Rat Binding pKi = 6.6 6.6 -114 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 376 4 0 4 4.0 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CC1 10.1021/jm00020a020
10775682 203192 None 1 Rat Binding pKi = 7.6 7.6 109 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1c2c(cc3ccccc13)CCC(N)C2 10.1016/S0960-894X(01)81009-X
CHEMBL64303 203192 None 1 Rat Binding pKi = 7.6 7.6 109 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1c2c(cc3ccccc13)CCC(N)C2 10.1016/S0960-894X(01)81009-X
11402988 59210 None 0 Human Binding pKi = 7.6 7.6 -32 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL170192 59210 None 0 Human Binding pKi = 7.6 7.6 -32 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
10096890 110156 None 0 Human Binding pKi = 7.6 7.6 -26 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 5 1 3 5.4 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(S(=O)(=O)c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL323666 110156 None 0 Human Binding pKi = 7.6 7.6 -26 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 5 1 3 5.4 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(S(=O)(=O)c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
2543 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358.0 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
54 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
CHEMBL128 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
DB00669 3707 None 68 Rat Binding pKi = 7.6 7.6 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
2543 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
5358 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
5358.0 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
54 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
CHEMBL128 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
DB00669 3707 None 68 Human Binding pKi = 7.6 7.6 -3 32
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
10447948 100171 None 0 Rat Binding pKi = 5.6 5.6 1 3
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 307 1 0 3 3.4 CN1CCN(c2nc3ccccc3c3c2CC2CCC3C2)CC1 10.1021/jm970645i
CHEMBL287987 100171 None 0 Rat Binding pKi = 5.6 5.6 1 3
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 307 1 0 3 3.4 CN1CCN(c2nc3ccccc3c3c2CC2CCC3C2)CC1 10.1021/jm970645i
9927441 207394 None 0 Human Binding pKi = 5.6 5.6 -676 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 207394 None 0 Human Binding pKi = 5.6 5.6 -676 9
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
9950390 66251 None 0 Human Binding pKi = 5.6 5.6 -588 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2n[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL184597 66251 None 0 Human Binding pKi = 5.6 5.6 -588 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2n[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2004.09.079
76319310 106322 None 0 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL2260928 106322 None 0 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL3139131 106322 None 0 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
3251 4072 None 58 Human Binding pKi = 7.6 7.6 -79 12
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 4072 None 58 Human Binding pKi = 7.6 7.6 -79 12
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 4072 None 58 Human Binding pKi = 7.6 7.6 -79 12
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 4072 None 58 Human Binding pKi = 7.6 7.6 -79 12
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
11792868 199187 None 0 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 360 4 1 6 0.7 O=C(C1=Cc2cccc(OCC3CNCCO3)c2OC1)N1CCOCC1 10.1021/jm970806i
CHEMBL58961 199187 None 0 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 360 4 1 6 0.7 O=C(C1=Cc2cccc(OCC3CNCCO3)c2OC1)N1CCOCC1 10.1021/jm970806i
151 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
20 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
5311258 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
CHEMBL101690 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
151 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
20 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
5311258 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
CHEMBL101690 2416 None 44 Human Binding pKi = 6.6 6.6 -89 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
44395787 126783 None 7 Human Binding pKi = 5.6 5.6 -588 3
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 1 4 3.7 CN1CCC(n2ncc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL365405 126783 None 7 Human Binding pKi = 5.6 5.6 -588 3
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 1 4 3.7 CN1CCC(n2ncc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
10475893 163931 None 0 Human Binding pKi = 6.6 6.6 -20 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 396 8 1 2 5.9 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL420748 163931 None 0 Human Binding pKi = 6.6 6.6 -20 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 396 8 1 2 5.9 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
132060770 162639 None 0 Human Binding pKi = 5.6 5.6 -39 10
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 162639 None 0 Human Binding pKi = 5.6 5.6 -39 10
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
10691904 35620 None 0 Human Binding pKi = 6.6 6.6 -6 4
Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.
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 None 0 Human Binding pKi = 6.6 6.6 -6 4
Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
122187378 123026 None 0 Human Binding pKi = 5.6 5.6 -8 2
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609143 123026 None 0 Human Binding pKi = 5.6 5.6 -8 2
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
76315631 106213 None 0 Human Binding pKi = 5.6 5.6 -4 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL2260925 106213 None 0 Human Binding pKi = 5.6 5.6 -4 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL3138773 106213 None 0 Human Binding pKi = 5.6 5.6 -4 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
10449461 204459 None 0 Human Binding pKi = 6.6 6.6 -354 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 332 6 1 1 5.0 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL72285 204459 None 0 Human Binding pKi = 6.6 6.6 -354 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 332 6 1 1 5.0 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
5 139 None 72 Rat Binding pKi = 7.6 7.6 -13 54
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
5202 139 None 72 Rat Binding pKi = 7.6 7.6 -13 54
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
CHEMBL39 139 None 72 Rat Binding pKi = 7.6 7.6 -13 54
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
DB08839 139 None 72 Rat Binding pKi = 7.6 7.6 -13 54
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
133 2496 None 52 Rat Binding pKi = 7.6 7.6 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
1723 2496 None 52 Rat Binding pKi = 7.6 7.6 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
28693 2496 None 52 Rat Binding pKi = 7.6 7.6 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
CHEMBL19215 2496 None 52 Rat Binding pKi = 7.6 7.6 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
DB13520 2496 None 52 Rat Binding pKi = 7.6 7.6 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
11809037 5093 None 0 Human Binding pKi = 7.6 7.6 -5 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 309 3 1 5 1.7 CN1CCC(c2c[nH]c3ccc(OS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
CHEMBL105556 5093 None 0 Human Binding pKi = 7.6 7.6 -5 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 309 3 1 5 1.7 CN1CCC(c2c[nH]c3ccc(OS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
44443101 93959 None 0 Human Binding pKi = 7.6 7.6 -12 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 536 9 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CCc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248407 93959 None 0 Human Binding pKi = 7.6 7.6 -12 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 536 9 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CCc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
44443094 93971 None 0 Human Binding pKi = 7.6 7.6 -25 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 460 7 0 6 3.5 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL248458 93971 None 0 Human Binding pKi = 7.6 7.6 -25 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 460 7 0 6 3.5 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44588745 184982 None 0 Human Binding pKi = 7.6 7.6 -3 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 417 5 1 5 4.0 Cc1ccc2c(OC3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485427 184982 None 0 Human Binding pKi = 7.6 7.6 -3 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 417 5 1 5 4.0 Cc1ccc2c(OC3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10151492 193382 None 0 Human Binding pKi = 7.6 7.6 -100 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 446 8 2 4 5.0 CCNC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL525362 193382 None 0 Human Binding pKi = 7.6 7.6 -100 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 446 8 2 4 5.0 CCNC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
10778246 165440 None 0 Rat Binding pKi = 7.6 7.6 -1 3
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandThe compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3ncccc3n3cccc23)CC1 10.1021/jm990151g
CHEMBL423899 165440 None 0 Rat Binding pKi = 7.6 7.6 -1 3
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandThe compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3ncccc3n3cccc23)CC1 10.1021/jm990151g
10802125 198071 None 1 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 272 3 1 5 1.4 N#CC1=Cc2cccc(OCC3CNCCO3)c2OC1 10.1021/jm970806i
CHEMBL57423 198071 None 1 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 272 3 1 5 1.4 N#CC1=Cc2cccc(OCC3CNCCO3)c2OC1 10.1021/jm970806i
CHEMBL5093342 215564 None 0 Human Binding pKi = 6.6 6.6 -29 7
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 215564 None 0 Human Binding pKi = 6.6 6.6 -29 7
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
152 364 None 29 Human Binding pKi = 6.6 6.6 -33 18
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
2107 364 None 29 Human Binding pKi = 6.6 6.6 -33 18
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
CHEMBL275854 364 None 29 Human Binding pKi = 6.6 6.6 -33 18
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
10451312 20671 None 0 Rat Binding pKi = 6.6 6.6 -316 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2C1 10.1021/jm00020a020
CHEMBL130870 20671 None 0 Rat Binding pKi = 6.6 6.6 -316 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2C1 10.1021/jm00020a020
10150658 68645 None 1 Human Binding pKi = 6.6 6.6 -158 2
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 392 6 2 6 3.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c(N)c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191895 68645 None 1 Human Binding pKi = 6.6 6.6 -158 2
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 392 6 2 6 3.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c(N)c4)CC3)cccc2n1 10.1021/jm049039v
10173169 68651 None 0 Human Binding pKi = 6.6 6.6 -100 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncccc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191921 68651 None 0 Human Binding pKi = 6.6 6.6 -100 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncccc45)CC3)cccc2n1 10.1021/jm049039v
11774585 69173 None 0 Human Binding pKi = 6.6 6.6 -31 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 424 7 0 6 3.8 Cc1ccc2c(OCCN3CCN(Cc4ccc(F)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL192536 69173 None 0 Human Binding pKi = 6.6 6.6 -31 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 424 7 0 6 3.8 Cc1ccc2c(OCCN3CCN(Cc4ccc(F)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
24865538 187579 None 0 Human Binding pKi = 6.6 6.6 -251 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 361 6 0 4 3.7 Cc1ccc2c(OCCN3CCN(Cc4ccccc4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL494631 187579 None 0 Human Binding pKi = 6.6 6.6 -251 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 361 6 0 4 3.7 Cc1ccc2c(OCCN3CCN(Cc4ccccc4)CC3)cccc2n1 10.1021/jm8001444
10683189 119082 None 0 Rat Binding pKi = 6.6 6.6 3 2
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 266 1 1 4 2.2 Cc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm990151g
CHEMBL342690 119082 None 0 Rat Binding pKi = 6.6 6.6 3 2
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 266 1 1 4 2.2 Cc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm990151g
9805456 207746 None 0 Human Binding pKi = 5.6 5.6 -1995 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 207746 None 0 Human Binding pKi = 5.6 5.6 -1995 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
1220 187 None 55 Rat Binding pKi = 5.6 5.6 -7413 44
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
31 187 None 55 Rat Binding pKi = 5.6 5.6 -7413 44
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
7 187 None 55 Rat Binding pKi = 5.6 5.6 -7413 44
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
CHEMBL56 187 None 55 Rat Binding pKi = 5.6 5.6 -7413 44
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
10402263 103199 None 1 Human Binding pKi = 7.6 7.6 -18 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL308347 103199 None 1 Human Binding pKi = 7.6 7.6 -18 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
44395832 123194 None 5 Human Binding pKi = 6.6 6.6 -120 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 1 3 4.3 CN1CCC(n2ccc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL361303 123194 None 5 Human Binding pKi = 6.6 6.6 -120 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 1 3 4.3 CN1CCC(n2ccc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
10692095 204392 None 0 Western lowland gorilla Binding pKi = 4.6 4.6 -120 4
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71907 204392 None 0 Western lowland gorilla Binding pKi = 4.6 4.6 -120 4
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
10326069 39296 None 1 Human Binding pKi = 5.6 5.6 -147 9
Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 39296 None 1 Human Binding pKi = 5.6 5.6 -147 9
Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
14083209 63064 None 2 Rat Binding pKi = 5.6 5.6 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@H](C)N)c12 10.1021/jm00402a026
CHEMBL1788280 63064 None 2 Rat Binding pKi = 5.6 5.6 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@H](C)N)c12 10.1021/jm00402a026
129503 161668 None 10 Human Binding pKi = 6.6 6.6 -22 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL413105 161668 None 10 Human Binding pKi = 6.6 6.6 -22 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10872581 4929 None 0 Human Binding pKi = 6.6 6.6 -34 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc([N+](=O)[O-])cc4)nc23)CC1 10.1021/jm030020m
CHEMBL104692 4929 None 0 Human Binding pKi = 6.6 6.6 -34 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc([N+](=O)[O-])cc4)nc23)CC1 10.1021/jm030020m
10445946 167863 None 4 Human Binding pKi = 6.6 6.6 -53 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 272 2 2 3 2.3 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL431041 167863 None 4 Human Binding pKi = 6.6 6.6 -53 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 272 2 2 3 2.3 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
53248365 62086 None 0 Human Binding pKi = 6.6 6.6 -281 7
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 62086 None 0 Human Binding pKi = 6.6 6.6 -281 7
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
16117279 60136 None 0 Human Binding pKi = 5.6 5.6 -2754 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 60136 None 0 Human Binding pKi = 5.6 5.6 -2754 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 60136 None 0 Human Binding pKi = 5.6 5.6 -2754 7
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
28338386 106225 None 2 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260921 106225 None 2 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138811 106225 None 2 Human Binding pKi = 5.6 5.6 -2 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
6604864 198818 None 1 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
CHEMBL1202783 198818 None 1 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
CHEMBL58353 198818 None 1 Rat Binding pKi = 6.6 6.6 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
10590370 161818 None 0 Human Binding pKi = 6.6 6.6 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 300 11 2 1 5.4 CCCCCCCCCCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL414420 161818 None 0 Human Binding pKi = 6.6 6.6 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 300 11 2 1 5.4 CCCCCCCCCCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
9837108 204658 None 3 Human Binding pKi = 5.6 5.6 -8 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 3 1 2 2.4 CC(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
CHEMBL73670 204658 None 3 Human Binding pKi = 5.6 5.6 -8 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 3 1 2 2.4 CC(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
11726413 102106 None 0 Human Binding pKi = 6.6 6.6 -14 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 366 6 1 2 4.9 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL302263 102106 None 0 Human Binding pKi = 6.6 6.6 -14 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 366 6 1 2 4.9 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(F)(F)F)c3c2C1 10.1021/jm00012a021
9848876 107445 None 0 Human Binding pKi = 7.6 7.6 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
CHEMBL318249 107445 None 0 Human Binding pKi = 7.6 7.6 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
44403102 71732 None 0 Human Binding pKi = 7.6 7.6 12 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196598 71732 None 0 Human Binding pKi = 7.6 7.6 12 6
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
70529 207470 None 110 Rat Binding pKi = 7.5 7.5 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9429 207470 None 110 Rat Binding pKi = 7.5 7.5 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL5090884 215577 None 0 Human Binding pKi = 6.6 6.6 -4 7
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 215577 None 0 Human Binding pKi = 6.6 6.6 -4 7
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
59636748 126204 None 0 Chinese hamster Binding pKi = 6.6 6.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 7 1 7 3.4 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccnn1C nan
CHEMBL3650025 126204 None 0 Chinese hamster Binding pKi = 6.6 6.6 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 7 1 7 3.4 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccnn1C nan
10063561 167801 None 1 Rat Binding pKi = 6.6 6.6 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 303 1 1 4 3.5 c1ccc2c(c1)nc(N1CCNCC1)c1oc3ccccc3c12 10.1021/jm00014a021
CHEMBL430566 167801 None 1 Rat Binding pKi = 6.6 6.6 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 303 1 1 4 3.5 c1ccc2c(c1)nc(N1CCNCC1)c1oc3ccccc3c12 10.1021/jm00014a021
9802187 205848 None 0 Human Binding pKi = 6.6 6.6 -51 4
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL83617 205848 None 0 Human Binding pKi = 6.6 6.6 -51 4
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44431531 88025 None 0 Human Binding pKi = 6.6 6.6 -60 3
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CCC1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL234447 88025 None 0 Human Binding pKi = 6.6 6.6 -60 3
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CCC1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
9802187 205848 None 0 Human Binding pKi = 6.6 6.6 -51 4
Inhibition constant against 5-HT 1B receptorInhibition constant against 5-HT 1B receptor
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm058225d
CHEMBL83617 205848 None 0 Human Binding pKi = 6.6 6.6 -51 4
Inhibition constant against 5-HT 1B receptorInhibition constant against 5-HT 1B receptor
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm058225d
10775128 188731 None 3 Human Binding pKi = 6.5 6.5 -2 3
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL50492 188731 None 3 Human Binding pKi = 6.5 6.5 -2 3
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
60820 4308 None 14 Human Binding pKi = 5.5 5.5 -144543 13
Binding affinity to 5HT1BBinding affinity to 5HT1B
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
CHEMBL10085 4308 None 14 Human Binding pKi = 5.5 5.5 -144543 13
Binding affinity to 5HT1BBinding affinity to 5HT1B
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
60820 4308 None 14 Rat Binding pKi = 5.5 5.5 -144543 13
Binding affinity towards 5-hydroxytryptamine 1B receptorBinding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
CHEMBL10085 4308 None 14 Rat Binding pKi = 5.5 5.5 -144543 13
Binding affinity towards 5-hydroxytryptamine 1B receptorBinding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
10891048 4811 None 0 Human Binding pKi = 5.5 5.5 -13 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 273 2 2 4 1.7 CC(=O)Nc1ncc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL104158 4811 None 0 Human Binding pKi = 5.5 5.5 -13 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 273 2 2 4 1.7 CC(=O)Nc1ncc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
23533329 85113 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 493 9 2 7 3.0 COc1cc(N(C)CCCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL224738 85113 None 0 Human Binding pKi = 6.5 6.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 493 9 2 7 3.0 COc1cc(N(C)CCCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
115 3791 None 80 Rat Binding pKi = 6.5 6.5 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
4296 3791 None 80 Rat Binding pKi = 6.5 6.5 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
CHEMBL274866 3791 None 80 Rat Binding pKi = 6.5 6.5 1 27
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
10342552 9936 None 0 Human Binding pKi = 8.5 8.5 -9 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 4 2 2 5.4 Cc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL114571 9936 None 0 Human Binding pKi = 8.5 8.5 -9 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 4 2 2 5.4 Cc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
10613373 111305 None 1 Human Binding pKi = 8.5 8.5 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 10 2 2 4.4 CCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL326667 111305 None 1 Human Binding pKi = 8.5 8.5 -1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 10 2 2 4.4 CCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
1043 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
149 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
8223 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
8223.0 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
CHEMBL442 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
DB00696 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
1043 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
149 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
8223 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
8223.0 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
CHEMBL442 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
DB00696 1582 None 14 Human Binding pKi = 8.5 8.5 -29 28
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
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 10.1016/j.bmcl.2013.12.024
44402877 71131 None 0 Human Binding pKi = 8.5 8.5 31 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 520 4 0 5 6.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195497 71131 None 0 Human Binding pKi = 8.5 8.5 31 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 520 4 0 5 6.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
44402880 71233 None 0 Human Binding pKi = 8.5 8.5 63 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(F)c1C(F)(F)F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195651 71233 None 0 Human Binding pKi = 8.5 8.5 63 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(F)c1C(F)(F)F)CC2 10.1016/j.bmcl.2005.07.085
11591924 71758 None 3 Human Binding pKi = 8.5 8.5 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 537 5 1 7 5.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196666 71758 None 3 Human Binding pKi = 8.5 8.5 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 537 5 1 7 5.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
44402886 71840 None 0 Human Binding pKi = 8.5 8.5 125 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 5 1 5 5.3 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(C(C)=O)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196951 71840 None 0 Human Binding pKi = 8.5 8.5 125 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 5 1 5 5.3 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(C(C)=O)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
11307899 78868 None 0 Human Binding pKi = 8.5 8.5 -50 7
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
CHEMBL2112882 78868 None 0 Human Binding pKi = 8.5 8.5 -50 7
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
10370874 82595 None 0 Human Binding pKi = 8.5 8.5 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 484 9 1 6 5.8 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1CCCN(C)C 10.1021/jm970457s
CHEMBL21790 82595 None 0 Human Binding pKi = 8.5 8.5 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 484 9 1 6 5.8 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1CCCN(C)C 10.1021/jm970457s
49850671 56391 None 0 Human Binding pKi = 8.5 8.5 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631537 56391 None 0 Human Binding pKi = 8.5 8.5 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
11292933 56394 None 45 Human Binding pKi = 8.5 8.5 -15 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631540 56394 None 45 Human Binding pKi = 8.5 8.5 -15 9
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
11419978 56463 None 0 Human Binding pKi = 8.5 8.5 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632211 56463 None 0 Human Binding pKi = 8.5 8.5 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
49850877 56464 None 0 Human Binding pKi = 8.5 8.5 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632212 56464 None 0 Human Binding pKi = 8.5 8.5 -10 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
49850568 56470 None 0 Human Binding pKi = 8.5 8.5 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5csc(C)n5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632218 56470 None 0 Human Binding pKi = 8.5 8.5 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5csc(C)n5)c4)CC3)cccc2n1 10.1021/jm100714c
11397149 56475 None 0 Human Binding pKi = 8.5 8.5 -10 7
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632223 56475 None 0 Human Binding pKi = 8.5 8.5 -10 7
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
107780 1844 None 54 Rat Binding pKi = 8.5 8.5 -4 17
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
14 1844 None 54 Rat Binding pKi = 8.5 8.5 -4 17
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
CHEMBL15928 1844 None 54 Rat Binding pKi = 8.5 8.5 -4 17
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
44342993 11010 None 0 Human Binding pKi = 8.5 8.5 -4 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 4 2 2 6.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL117397 11010 None 0 Human Binding pKi = 8.5 8.5 -4 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 4 2 2 6.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
10970604 5063 None 0 Human Binding pKi = 8.5 8.5 1 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 367 3 3 3 4.2 CN1CCC(c2c[nH]c3ccc(NC(=O)Nc4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL105369 5063 None 0 Human Binding pKi = 8.5 8.5 1 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 367 3 3 3 4.2 CN1CCC(c2c[nH]c3ccc(NC(=O)Nc4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
11655728 16644 None 8 Rat Binding pKi = 8.5 8.5 -46 6
Displacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometryDisplacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometry
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 16644 None 8 Rat Binding pKi = 8.5 8.5 -46 6
Displacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometryDisplacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometry
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
1884 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
4440 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
4440.0 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
45 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
CHEMBL1278 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
DB00952 2735 None 58 Human Binding pKi = 8.5 8.5 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
59636740 125693 None 0 Chinese hamster Binding pKi = 8.5 8.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 9 1 7 3.7 CS(=O)(=O)Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
CHEMBL3647275 125693 None 0 Chinese hamster Binding pKi = 8.5 8.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 9 1 7 3.7 CS(=O)(=O)Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
5 139 None 72 Rat Binding pKi = 8.5 8.5 -13 54
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
5202 139 None 72 Rat Binding pKi = 8.5 8.5 -13 54
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
CHEMBL39 139 None 72 Rat Binding pKi = 8.5 8.5 -13 54
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
DB08839 139 None 72 Rat Binding pKi = 8.5 8.5 -13 54
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
107 141 None 121 Human Binding pKi = 8.5 8.5 -16 30
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
1833 141 None 121 Human Binding pKi = 8.5 8.5 -16 30
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
CHEMBL8165 141 None 121 Human Binding pKi = 8.5 8.5 -16 30
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
23533322 85070 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 477 5 2 7 2.4 COc1cc(N2CCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL224399 85070 None 0 Human Binding pKi = 8.5 8.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 477 5 2 7 2.4 COc1cc(N2CCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
59636761 126209 None 0 Chinese hamster Binding pKi = 8.5 8.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 2 6 3.8 O=C(NCc1cccc(O)c1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650030 126209 None 0 Chinese hamster Binding pKi = 8.5 8.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 2 6 3.8 O=C(NCc1cccc(O)c1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44342508 9823 None 0 Human Binding pKi = 8.4 8.4 -8 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL113893 9823 None 0 Human Binding pKi = 8.4 8.4 -8 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
44342518 9974 None 0 Human Binding pKi = 8.4 8.4 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 4 2 2 5.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL114780 9974 None 0 Human Binding pKi = 8.4 8.4 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 4 2 2 5.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
3608822 98510 None 21 Rat Binding pKi = 8.4 8.4 3 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 2 1 2 2.2 CC(C)c1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL276156 98510 None 21 Rat Binding pKi = 8.4 8.4 3 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 2 1 2 2.2 CC(C)c1ccccc1N1CCNCC1 10.1021/jm00125a020
75 3514 None 7 Human Binding pKi = 8.4 8.4 -3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
9870500 3514 None 7 Human Binding pKi = 8.4 8.4 -3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
CHEMBL191971 3514 None 7 Human Binding pKi = 8.4 8.4 -3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
44402870 71115 None 0 Human Binding pKi = 8.4 8.4 3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 434 3 1 4 4.3 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195432 71115 None 0 Human Binding pKi = 8.4 8.4 3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 434 3 1 4 4.3 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
44402881 165814 None 0 Human Binding pKi = 8.4 8.4 39 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 3 1 4 5.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL424837 165814 None 0 Human Binding pKi = 8.4 8.4 39 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 3 1 4 5.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402868 168345 None 0 Human Binding pKi = 8.4 8.4 31 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 534 5 0 5 6.3 CCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
CHEMBL434355 168345 None 0 Human Binding pKi = 8.4 8.4 31 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 534 5 0 5 6.3 CCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
49850670 56390 None 0 Human Binding pKi = 8.4 8.4 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631536 56390 None 0 Human Binding pKi = 8.4 8.4 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
49850982 56466 None 0 Human Binding pKi = 8.4 8.4 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccccc1C(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632214 56466 None 0 Human Binding pKi = 8.4 8.4 -6 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccccc1C(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49850566 56468 None 0 Human Binding pKi = 8.4 8.4 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)cc1 10.1021/jm100714c
CHEMBL1632216 56468 None 0 Human Binding pKi = 8.4 8.4 -7 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)cc1 10.1021/jm100714c
49850668 56474 None 0 Human Binding pKi = 8.4 8.4 -15 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 445 5 2 4 4.8 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)NC(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632222 56474 None 0 Human Binding pKi = 8.4 8.4 -15 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 445 5 2 4 4.8 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)NC(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
22326688 93597 None 0 Human Binding pKi = 8.4 8.4 -4 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 459 7 0 5 4.6 CCN1C(=O)COc2ccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL246598 93597 None 0 Human Binding pKi = 8.4 8.4 -4 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 459 7 0 5 4.6 CCN1C(=O)COc2ccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
10174078 176894 None 0 Human Binding pKi = 8.4 8.4 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)N[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL461670 176894 None 0 Human Binding pKi = 8.4 8.4 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)N[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44404260 72352 None 0 Human Binding pKi = 8.4 8.4 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 519 5 0 7 4.6 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C(C)C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL198488 72352 None 0 Human Binding pKi = 8.4 8.4 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 519 5 0 7 4.6 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C(C)C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
115 3791 None 80 Rat Binding pKi = 7.5 7.5 1 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
4296 3791 None 80 Rat Binding pKi = 7.5 7.5 1 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
CHEMBL274866 3791 None 80 Rat Binding pKi = 7.5 7.5 1 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
10299410 85057 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 5 1 7 3.2 COc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(F)cc12 10.1016/j.bmc.2006.10.037
CHEMBL224267 85057 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 5 1 7 3.2 COc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(F)cc12 10.1016/j.bmc.2006.10.037
77418 97397 None 64 Rat Binding pKi = 7.5 7.5 3 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1cccc(N2CCNCC2)c1 10.1021/jm00125a020
CHEMBL269784 97397 None 64 Rat Binding pKi = 7.5 7.5 3 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1cccc(N2CCNCC2)c1 10.1021/jm00125a020
10620719 204350 None 0 Western lowland gorilla Binding pKi = 5.5 5.5 -794 5
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71635 204350 None 0 Western lowland gorilla Binding pKi = 5.5 5.5 -794 5
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9995233 165111 None 0 Human Binding pKi = 6.5 6.5 -39 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 304 4 1 2 4.7 CN(C)CCc1c[nH]c2ccc(-c3ccc(Cl)s3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL422737 165111 None 0 Human Binding pKi = 6.5 6.5 -39 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 304 4 1 2 4.7 CN(C)CCc1c[nH]c2ccc(-c3ccc(Cl)s3)cc12 10.1016/s0960-894x(00)00133-5
10379784 204382 None 1 Human Binding pKi = 6.5 6.5 -251 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL71804 204382 None 1 Human Binding pKi = 6.5 6.5 -251 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
11123573 208024 None 0 Human Binding pKi = 7.5 7.5 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 473 6 2 5 3.8 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4c[nH]nn4)cc23)CC1 10.1021/jm020938y
CHEMBL97422 208024 None 0 Human Binding pKi = 7.5 7.5 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 473 6 2 5 3.8 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4c[nH]nn4)cc23)CC1 10.1021/jm020938y
44438461 90973 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 452 6 0 6 5.0 CC(C)N1CCN(C2CCc3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc32)CC1 10.1016/j.bmcl.2006.12.109
CHEMBL239596 90973 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 452 6 0 6 5.0 CC(C)N1CCN(C2CCc3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc32)CC1 10.1016/j.bmcl.2006.12.109
59636742 125701 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1ccccn1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647283 125701 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1ccccn1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44402869 134143 None 0 Human Binding pKi = 7.5 7.5 2 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 548 6 0 5 6.7 CCCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
CHEMBL371655 134143 None 0 Human Binding pKi = 7.5 7.5 2 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 548 6 0 5 6.7 CCCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
10838923 52635 None 0 Human Binding pKi = 7.5 7.5 31 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm970457s
CHEMBL15933 52635 None 0 Human Binding pKi = 7.5 7.5 31 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm970457s
22326704 144937 None 0 Human Binding pKi = 7.5 7.5 -12 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)c(F)ccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391033 144937 None 0 Human Binding pKi = 7.5 7.5 -12 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)c(F)ccc2n1 10.1016/j.bmcl.2006.11.031
49850770 56397 None 0 Human Binding pKi = 7.5 7.5 -125 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631543 56397 None 0 Human Binding pKi = 7.5 7.5 -125 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
44443095 93598 None 0 Human Binding pKi = 7.5 7.5 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 474 8 0 6 3.9 CCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL246599 93598 None 0 Human Binding pKi = 7.5 7.5 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 474 8 0 6 3.9 CCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44443096 93927 None 0 Human Binding pKi = 7.5 7.5 -25 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 9 0 6 4.3 CCCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL248229 93927 None 0 Human Binding pKi = 7.5 7.5 -25 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 9 0 6 4.3 CCCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44443097 93928 None 0 Human Binding pKi = 7.5 7.5 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 8 0 6 4.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CC(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248230 93928 None 0 Human Binding pKi = 7.5 7.5 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 8 0 6 4.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CC(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
44581260 175592 None 0 Human Binding pKi = 7.5 7.5 -31 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@@H](C)NC[C@@H]5C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL457982 175592 None 0 Human Binding pKi = 7.5 7.5 -31 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@@H](C)NC[C@@H]5C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10452875 193165 None 0 Human Binding pKi = 7.5 7.5 -125 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4cccc5cccnc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
CHEMBL523095 193165 None 0 Human Binding pKi = 7.5 7.5 -125 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4cccc5cccnc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
173 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
5011 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
CHEMBL18772 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
173 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
5011 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
CHEMBL18772 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
44461247 104756 None 0 Human Binding pKi = 6.5 6.5 -43 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 422 5 2 4 3.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CCN(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL310744 104756 None 0 Human Binding pKi = 6.5 6.5 -43 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 422 5 2 4 3.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CCN(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
11824522 4890 None 0 Human Binding pKi = 6.5 6.5 -42 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(C#N)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL104484 4890 None 0 Human Binding pKi = 6.5 6.5 -42 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(C#N)cc4)nc23)CC1 10.1021/jm030020m
6918601 18523 None 0 Human Binding pKi = 5.5 5.5 -407 4
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
CHEMBL127411 18523 None 0 Human Binding pKi = 5.5 5.5 -407 4
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
22067856 29540 None 52 Rat Binding pKi = 5.5 5.5 1 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm00124a021
CHEMBL138509 29540 None 52 Rat Binding pKi = 5.5 5.5 1 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm00124a021
11777940 101431 None 0 Human Binding pKi = 6.5 6.5 -123 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 3 1 1 4.1 CC(C)(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL297471 101431 None 0 Human Binding pKi = 6.5 6.5 -123 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 3 1 1 4.1 CC(C)(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
44461306 205931 None 0 Human Binding pKi = 6.5 6.5 -12 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 431 6 2 4 4.1 COc1ccc2[nH]cc(C3=CCN(CCC4OCCc5cc(C(N)=O)ccc54)CC3)c2c1 10.1016/j.bmcl.2004.03.003
CHEMBL84171 205931 None 0 Human Binding pKi = 6.5 6.5 -12 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 431 6 2 4 4.1 COc1ccc2[nH]cc(C3=CCN(CCC4OCCc5cc(C(N)=O)ccc54)CC3)c2c1 10.1016/j.bmcl.2004.03.003
44364048 39139 None 0 Human Binding pKi = 6.5 6.5 -158 6
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligandBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
CHEMBL146942 39139 None 0 Human Binding pKi = 6.5 6.5 -158 6
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligandBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
10022680 19522 None 0 Rat Binding pKi = 6.5 6.5 -251 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 380 5 0 5 3.3 COc1ccc2c(c1)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL129947 19522 None 0 Rat Binding pKi = 6.5 6.5 -251 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 380 5 0 5 3.3 COc1ccc2c(c1)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10066717 20833 None 0 Rat Binding pKi = 6.5 6.5 -177 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 354 3 0 4 3.1 Fc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131018 20833 None 0 Rat Binding pKi = 6.5 6.5 -177 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 354 3 0 4 3.1 Fc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9889681 208063 None 0 Human Binding pKi = 6.5 6.5 -630 5
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 208063 None 0 Human Binding pKi = 6.5 6.5 -630 5
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
75306277 109254 None 0 Human Binding pKi = 6.5 6.5 -158 23
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 109254 None 0 Human Binding pKi = 6.5 6.5 -158 23
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11168182 3534 None 25 Human Binding pKi = 6.5 6.5 -50 13
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 3534 None 25 Human Binding pKi = 6.5 6.5 -50 13
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 3534 None 25 Human Binding pKi = 6.5 6.5 -50 13
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
11476072 69401 None 0 Human Binding pKi = 6.5 6.5 -15 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 436 8 0 7 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1[N+](=O)[O-] 10.1021/jm049039v
CHEMBL193268 69401 None 0 Human Binding pKi = 6.5 6.5 -15 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 436 8 0 7 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1[N+](=O)[O-] 10.1021/jm049039v
11235335 124025 None 0 Human Binding pKi = 6.5 6.5 -125 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 413 6 0 6 3.7 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncncc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL362992 124025 None 0 Human Binding pKi = 6.5 6.5 -125 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 413 6 0 6 3.7 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncncc45)CC3)cccc2n1 10.1021/jm049039v
9804612 90535 None 0 Human Binding pKi = 6.5 6.5 -79 5
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238730 90535 None 0 Human Binding pKi = 6.5 6.5 -79 5
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
44588722 191241 None 0 Human Binding pKi = 6.5 6.5 -3 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 433 8 1 6 3.7 Cc1ccc2c(OCCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL519010 191241 None 0 Human Binding pKi = 6.5 6.5 -3 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 433 8 1 6 3.7 Cc1ccc2c(OCCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
9870053 208284 None 0 Human Binding pKi = 5.5 5.5 -2511 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 208284 None 0 Human Binding pKi = 5.5 5.5 -2511 4
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10198700 120796 None 3 Human Binding pKi = 7.5 7.5 -18 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 2 2 3.4 NCCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL355517 120796 None 3 Human Binding pKi = 7.5 7.5 -18 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 2 2 3.4 NCCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
44376383 55539 None 0 Human Binding pKi = 7.5 7.5 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 6 2 3 5.1 Cc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162049 55539 None 0 Human Binding pKi = 7.5 7.5 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 6 2 3 5.1 Cc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
9802530 35386 None 1 Human Binding pKi = 7.5 7.5 -2 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
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 None 1 Human Binding pKi = 7.5 7.5 -2 4
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
24881686 188389 None 0 Human Binding pKi = 7.5 7.5 -8 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL501645 188389 None 0 Human Binding pKi = 7.5 7.5 -8 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
11728004 4453 None 0 Human Binding pKi = 7.5 7.5 -1 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 356 8 2 3 4.7 CCCCCCCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL101686 4453 None 0 Human Binding pKi = 7.5 7.5 -1 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 356 8 2 3 4.7 CCCCCCCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
173 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
5011 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
CHEMBL18772 3262 None 95 Rat Binding pKi = 6.5 6.5 -2 23
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
44269070 31222 None 0 Rat Binding pKi = 6.5 6.5 -162 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 440 6 0 5 3.3 COc1cccc2c1C1CCN(CCCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
CHEMBL14010 31222 None 0 Rat Binding pKi = 6.5 6.5 -162 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 440 6 0 5 3.3 COc1cccc2c1C1CCN(CCCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
4806 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094.0 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051.0 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
11568826 132798 None 0 Rat Binding pKi = 7.5 7.5 -28 8
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
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 None 0 Rat Binding pKi = 7.5 7.5 -28 8
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
2760216 97061 None 81 Rat Binding pKi = 7.5 7.5 - 1
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1cccc(N2CCNCC2)c1 10.1021/jm00125a020
CHEMBL267153 97061 None 81 Rat Binding pKi = 7.5 7.5 - 1
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1cccc(N2CCNCC2)c1 10.1021/jm00125a020
11759467 5169 None 0 Human Binding pKi = 6.5 6.5 -39 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccncc4)nc23)CC1 10.1021/jm030020m
CHEMBL105958 5169 None 0 Human Binding pKi = 6.5 6.5 -39 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccncc4)nc23)CC1 10.1021/jm030020m
10331436 324 None 10 Human Binding pKi = 5.5 5.5 -1659 6
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 324 None 10 Human Binding pKi = 5.5 5.5 -1659 6
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 324 None 10 Human Binding pKi = 5.5 5.5 -1659 6
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
44582705 186996 None 0 Human Binding pKi = 5.5 5.5 -21 13
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 186996 None 0 Human Binding pKi = 5.5 5.5 -21 13
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
59636771 126207 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1cccnc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650028 126207 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1cccnc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
9910451 164130 None 0 Human Binding pKi = 6.5 6.5 -338 6
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 164130 None 0 Human Binding pKi = 6.5 6.5 -338 6
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
145988313 167235 None 0 Human Binding pKi = 5.5 5.5 -758 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 167235 None 0 Human Binding pKi = 5.5 5.5 -758 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
9881478 6651 None 27 Human Binding pKi = 6.5 6.5 3 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 1 2 2 2.0 COc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL108337 6651 None 27 Human Binding pKi = 6.5 6.5 3 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 1 2 2 2.0 COc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
3016908 204444 None 24 Human Binding pKi = 5.5 5.5 -47 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 2 1 2 2.2 Cc1cc(C)c(CC2=NCCN2)c(C)c1 10.1021/jm970513p
CHEMBL72178 204444 None 24 Human Binding pKi = 5.5 5.5 -47 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 2 1 2 2.2 Cc1cc(C)c(CC2=NCCN2)c(C)c1 10.1021/jm970513p
13096730 203366 None 5 Human Binding pKi = 6.5 6.5 -54 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL65196 203366 None 5 Human Binding pKi = 6.5 6.5 -54 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
13096730 203366 None 5 Human Binding pKi = 6.5 6.5 -54 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL65196 203366 None 5 Human Binding pKi = 6.5 6.5 -54 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10567450 9355 None 1 Human Binding pKi = 7.5 7.5 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 12 2 2 5.2 CCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111284 9355 None 1 Human Binding pKi = 7.5 7.5 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 12 2 2 5.2 CCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44422352 138149 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 6 2 7 2.8 COc1cc(N2CC[C@@H](N(C)C)C2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL376813 138149 None 0 Human Binding pKi = 7.5 7.5 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 6 2 7 2.8 COc1cc(N2CC[C@@H](N(C)C)C2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
59636769 125703 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 467 7 1 6 4.0 O=C(NC1(c2ccccn2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647285 125703 None 0 Chinese hamster Binding pKi = 7.5 7.5 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 467 7 1 6 4.0 O=C(NC1(c2ccccn2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
145 140 None 49 Rat Binding pKi = 6.5 6.5 -47 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
1832 140 None 49 Rat Binding pKi = 6.5 6.5 -47 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
CHEMBL7257 140 None 49 Rat Binding pKi = 6.5 6.5 -47 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
DB14010 140 None 49 Rat Binding pKi = 6.5 6.5 -47 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
11831220 192558 None 8 Human Binding pKi = 6.5 6.5 -8 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 10.1021/jm7011722
CHEMBL521235 192558 None 8 Human Binding pKi = 6.5 6.5 -8 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 10.1021/jm7011722
142601343 185603 None 0 Human Binding pKi = 5.5 5.5 -123 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 185603 None 0 Human Binding pKi = 5.5 5.5 -123 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
9848303 111580 None 0 Human Binding pKi = 7.4 7.4 -12 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
CHEMBL328187 111580 None 0 Human Binding pKi = 7.4 7.4 -12 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
2543 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
5358 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
5358.0 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
54 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
CHEMBL128 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
DB00669 3707 None 68 Human Binding pKi = 7.4 7.4 -3 32
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
44376282 120108 None 0 Human Binding pKi = 7.4 7.4 -3 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL351036 120108 None 0 Human Binding pKi = 7.4 7.4 -3 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
1150 3878 None 121 Human Binding pKi = 7.4 7.4 -7 25
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
125 3878 None 121 Human Binding pKi = 7.4 7.4 -7 25
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
CHEMBL6640 3878 None 121 Human Binding pKi = 7.4 7.4 -7 25
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
DB08653 3878 None 121 Human Binding pKi = 7.4 7.4 -7 25
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
9859280 106334 None 1 Human Binding pKi = 7.4 7.4 56 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL2260920 106334 None 1 Human Binding pKi = 7.4 7.4 56 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL3139165 106334 None 1 Human Binding pKi = 7.4 7.4 56 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
11092112 207628 None 0 Human Binding pKi = 6.4 6.4 -645 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 207628 None 0 Human Binding pKi = 6.4 6.4 -645 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10850769 201832 None 0 Rat Binding pKi = 5.4 5.4 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 286 3 0 5 1.7 CN1CCOC(COc2cccc3c2OCC(C#N)=C3)C1 10.1021/jm970806i
CHEMBL60705 201832 None 0 Rat Binding pKi = 5.4 5.4 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 286 3 0 5 1.7 CN1CCOC(COc2cccc3c2OCC(C#N)=C3)C1 10.1021/jm970806i
44554395 18723 None 0 Human Binding pKi = 5.4 5.4 -2290 7
Displacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 18723 None 0 Human Binding pKi = 5.4 5.4 -2290 7
Displacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
107992 2553 None 49 Rat Binding pKi = 5.4 5.4 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
165 2553 None 49 Rat Binding pKi = 5.4 5.4 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
CHEMBL269521 2553 None 49 Rat Binding pKi = 5.4 5.4 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
DB12111 2553 None 49 Rat Binding pKi = 5.4 5.4 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
178081 102649 None 8 Human Binding pKi = 6.4 6.4 -707 6
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL304426 102649 None 8 Human Binding pKi = 6.4 6.4 -707 6
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
16614092 106241 None 5 Human Binding pKi = 5.4 5.4 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260922 106241 None 5 Human Binding pKi = 5.4 5.4 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138881 106241 None 5 Human Binding pKi = 5.4 5.4 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
9837525 103155 None 1 Human Binding pKi = 7.4 7.4 -33 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 3 1 2 3.0 Cc1cc(C(C)C)cc(C)c1CC1=NCCN1 10.1021/jm970513p
CHEMBL308042 103155 None 1 Human Binding pKi = 7.4 7.4 -33 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 3 1 2 3.0 Cc1cc(C(C)C)cc(C)c1CC1=NCCN1 10.1021/jm970513p
59636775 125681 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 444 7 1 7 2.9 Cn1cnc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647263 125681 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 444 7 1 7 2.9 Cn1cnc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
4595 176715 None 106 Rat Binding pKi = 5.4 5.4 -7 15
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
CHEMBL46 176715 None 106 Rat Binding pKi = 5.4 5.4 -7 15
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
11725335 102270 None 0 Human Binding pKi = 6.4 6.4 -33 4
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 348 6 1 3 3.6 CCCN(CCC)C1CCc2ccc3[nH]cc(S(C)(=O)=O)c3c2C1 10.1021/jm00012a021
CHEMBL303269 102270 None 0 Human Binding pKi = 6.4 6.4 -33 4
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 348 6 1 3 3.6 CCCN(CCC)C1CCc2ccc3[nH]cc(S(C)(=O)=O)c3c2C1 10.1021/jm00012a021
44311908 172701 None 3 Human Binding pKi = 5.4 5.4 - 1
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 176 2 2 3 0.9 Oc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
CHEMBL450281 172701 None 3 Human Binding pKi = 5.4 5.4 - 1
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 176 2 2 3 0.9 Oc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
122483281 138108 None 0 Human Binding pKi = 5.4 5.4 -741 8
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 138108 None 0 Human Binding pKi = 5.4 5.4 -741 8
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 138108 None 0 Human Binding pKi = 5.4 5.4 -741 8
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
9994674 204156 None 0 Human Binding pKi = 7.4 7.4 -44 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL70589 204156 None 0 Human Binding pKi = 7.4 7.4 -44 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
44376723 119858 None 0 Human Binding pKi = 7.4 7.4 -3 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 6 2 3 5.3 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
CHEMBL348756 119858 None 0 Human Binding pKi = 7.4 7.4 -3 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 6 2 3 5.3 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
24882266 188287 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL500230 188287 None 0 Human Binding pKi = 7.4 7.4 -2 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
59636732 126206 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 1 7 3.2 Cc1ncc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3650027 126206 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 1 7 3.2 Cc1ncc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
44403098 70272 None 0 Human Binding pKi = 7.4 7.4 4 4
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccc(F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL194206 70272 None 0 Human Binding pKi = 7.4 7.4 4 4
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccc(F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10946905 163682 None 0 Human Binding pKi = 6.4 6.4 -43 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 2 3 3.1 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCC4)nc23)CC1 10.1021/jm030020m
CHEMBL420475 163682 None 0 Human Binding pKi = 6.4 6.4 -43 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 2 3 3.1 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCC4)nc23)CC1 10.1021/jm030020m
10023301 18927 None 0 Rat Binding pKi = 6.4 6.4 -120 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 390 4 0 4 4.4 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CCC1 10.1021/jm00020a020
CHEMBL128546 18927 None 0 Rat Binding pKi = 6.4 6.4 -120 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 390 4 0 4 4.4 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CCC1 10.1021/jm00020a020
14083212 63065 None 6 Rat Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@@H](C)N)c2c1 10.1021/jm00402a026
CHEMBL1788281 63065 None 6 Rat Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@@H](C)N)c2c1 10.1021/jm00402a026
10445578 120219 None 1 Rat Binding pKi = 5.4 5.4 1 3
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 265 1 0 3 2.4 CN1CCN(c2ccc3c(n2)-c2ccccc2C3)CC1 10.1021/jm970645i
CHEMBL352107 120219 None 1 Rat Binding pKi = 5.4 5.4 1 3
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 265 1 0 3 2.4 CN1CCN(c2ccc3c(n2)-c2ccccc2C3)CC1 10.1021/jm970645i
10541847 102301 None 0 Human Binding pKi = 5.4 5.4 -3 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 294 5 1 3 3.4 Cc1ccc(CC2=NCCN2)c(C)c1OCc1ccccc1 10.1021/jm970513p
CHEMBL303441 102301 None 0 Human Binding pKi = 5.4 5.4 -3 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 294 5 1 3 3.4 Cc1ccc(CC2=NCCN2)c(C)c1OCc1ccccc1 10.1021/jm970513p
49799868 10539 None 0 Human Binding pKi = 6.4 6.4 -54 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL1169435 10539 None 0 Human Binding pKi = 6.4 6.4 -54 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
44342507 110189 None 0 Human Binding pKi = 7.4 7.4 -6 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 4 2 2 6.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL323705 110189 None 0 Human Binding pKi = 7.4 7.4 -6 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 4 2 2 6.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
49850769 56395 None 0 Human Binding pKi = 7.4 7.4 -125 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 429 5 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631541 56395 None 0 Human Binding pKi = 7.4 7.4 -125 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 429 5 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
49850771 56398 None 0 Human Binding pKi = 7.4 7.4 -25 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 428 5 0 5 3.6 Cc1ccc2c(N3CCN(CCc4cccc(N5C(=O)CCC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631544 56398 None 0 Human Binding pKi = 7.4 7.4 -25 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 428 5 0 5 3.6 Cc1ccc2c(N3CCN(CCc4cccc(N5C(=O)CCC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
10183895 93969 None 0 Human Binding pKi = 7.4 7.4 -22 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248456 93969 None 0 Human Binding pKi = 7.4 7.4 -22 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10127149 174914 None 0 Human Binding pKi = 7.4 7.4 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 426 7 0 4 6.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccoc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456460 174914 None 0 Human Binding pKi = 7.4 7.4 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 426 7 0 4 6.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccoc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10173443 175003 None 0 Human Binding pKi = 7.4 7.4 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 429 7 0 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456684 175003 None 0 Human Binding pKi = 7.4 7.4 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 429 7 0 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44593711 184323 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OCC(C)N3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484216 184323 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OCC(C)N3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10128059 187694 None 0 Human Binding pKi = 7.4 7.4 -6 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 483 9 1 6 4.3 COc1ccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1NS(C)(=O)=O 10.1021/jm8001444
CHEMBL495217 187694 None 0 Human Binding pKi = 7.4 7.4 -6 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 483 9 1 6 4.3 COc1ccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1NS(C)(=O)=O 10.1021/jm8001444
24865543 188128 None 0 Human Binding pKi = 7.4 7.4 -31 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 7 0 4 4.9 CC(=O)N(C)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL498356 188128 None 0 Human Binding pKi = 7.4 7.4 -31 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 7 0 4 4.9 CC(=O)N(C)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
22611622 4694 None 8 Human Binding pKi = 6.4 6.4 -39 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 271 2 2 2 2.9 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2c1 10.1021/jm030020m
CHEMBL103424 4694 None 8 Human Binding pKi = 6.4 6.4 -39 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 271 2 2 2 2.9 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2c1 10.1021/jm030020m
11047115 5020 None 0 Human Binding pKi = 6.4 6.4 -9 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc([N+](=O)[O-])c4)nc23)CC1 10.1021/jm030020m
CHEMBL105118 5020 None 0 Human Binding pKi = 6.4 6.4 -9 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc([N+](=O)[O-])c4)nc23)CC1 10.1021/jm030020m
11056946 108893 None 0 Human Binding pKi = 6.4 6.4 -54 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccs4)nc23)CC1 10.1021/jm030020m
CHEMBL321080 108893 None 0 Human Binding pKi = 6.4 6.4 -54 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccs4)nc23)CC1 10.1021/jm030020m
142601329 186517 None 5 Human Binding pKi = 5.4 5.4 -588 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 186517 None 5 Human Binding pKi = 5.4 5.4 -588 7
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
176 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157.0 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 398 None 66 Rat Binding pKi = 4.4 4.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
23533328 85176 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 8 2 7 2.6 COc1cc(N(C)CCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL225308 85176 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 8 2 7 2.6 COc1cc(N(C)CCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
193381 11040 None 21 Rat Binding pKi = 5.4 5.4 -1258 4
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2cccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
CHEMBL11760 11040 None 21 Rat Binding pKi = 5.4 5.4 -1258 4
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2cccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
6918647 100746 None 2 Human Binding pKi = 6.4 6.4 -79 14
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 100746 None 2 Human Binding pKi = 6.4 6.4 -79 14
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
10216160 67595 None 0 Human Binding pKi = 6.4 6.4 -125 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4cccc5cc[nH]c45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL190190 67595 None 0 Human Binding pKi = 6.4 6.4 -125 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4cccc5cc[nH]c45)CC3)cccc2n1 10.1021/jm049039v
11464355 127233 None 0 Human Binding pKi = 6.4 6.4 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 422 7 1 7 3.4 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL365810 127233 None 0 Human Binding pKi = 6.4 6.4 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 422 7 1 7 3.4 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
11178830 148126 None 0 Human Binding pKi = 6.4 6.4 -251 9
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL393539 148126 None 0 Human Binding pKi = 6.4 6.4 -251 9
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
44588742 191249 None 0 Human Binding pKi = 6.4 6.4 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.4 Cc1ccc2c(OCCCN3CC(Oc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL519019 191249 None 0 Human Binding pKi = 6.4 6.4 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.4 Cc1ccc2c(OCCCN3CC(Oc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
10423801 27628 None 0 Rat Binding pKi = 6.4 6.4 - 1
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 280 1 0 4 2.5 Cc1cccc2nc(N3CCN(C)CC3)c3cccn3c12 10.1021/jm990151g
CHEMBL136978 27628 None 0 Rat Binding pKi = 6.4 6.4 - 1
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 280 1 0 4 2.5 Cc1cccc2nc(N3CCN(C)CC3)c3cccn3c12 10.1021/jm990151g
10249573 207593 None 0 Human Binding pKi = 5.4 5.4 -398 11
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL94984 207593 None 0 Human Binding pKi = 5.4 5.4 -398 11
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
10689158 116675 None 0 Rat Binding pKi = 5.4 5.4 - 1
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 349 3 0 6 3.3 c1csc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c1 10.1021/jm990151g
CHEMBL337101 116675 None 0 Rat Binding pKi = 5.4 5.4 - 1
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 349 3 0 6 3.3 c1csc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c1 10.1021/jm990151g
9892409 100950 None 0 Human Binding pKi = 5.4 5.4 -794 9
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 100950 None 0 Human Binding pKi = 5.4 5.4 -794 9
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
108029 3414 None 57 Rat Binding pKi = 8.4 8.4 -3 13
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
23 3414 None 57 Rat Binding pKi = 8.4 8.4 -3 13
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
CHEMBL18785 3414 None 57 Rat Binding pKi = 8.4 8.4 -3 13
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
14479837 207511 None 7 Rat Binding pKi = 8.4 8.4 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 234 5 1 3 2.3 CCCCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9452 207511 None 7 Rat Binding pKi = 8.4 8.4 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 234 5 1 3 2.3 CCCCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
5 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5202 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
CHEMBL39 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
DB08839 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
5202 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
CHEMBL39 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
DB08839 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
5 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5202 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
CHEMBL39 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
DB08839 139 None 72 Human Binding pKi = 8.4 8.4 -11 54
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
107 141 None 121 Rat Binding pKi = 8.4 8.4 -30 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
1833 141 None 121 Rat Binding pKi = 8.4 8.4 -30 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
CHEMBL8165 141 None 121 Rat Binding pKi = 8.4 8.4 -30 30
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
10972931 208065 None 0 Human Binding pKi = 8.4 8.4 8 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm020938y
CHEMBL97650 208065 None 0 Human Binding pKi = 8.4 8.4 8 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm020938y
44342830 167981 None 0 Human Binding pKi = 8.4 8.4 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 5 2 3 5.1 COc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL431866 167981 None 0 Human Binding pKi = 8.4 8.4 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 5 2 3 5.1 COc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
2869 4152 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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
60857.0 4152 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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 None 89 Human Binding pKi = 8.4 8.4 -8 7
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
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
11384146 201733 None 0 Human Binding pKi = 8.4 8.4 -10 9
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 201733 None 0 Human Binding pKi = 8.4 8.4 -10 9
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
107780 1844 None 54 Human Binding pKi = 8.4 8.4 1 17
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
14 1844 None 54 Human Binding pKi = 8.4 8.4 1 17
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
CHEMBL15928 1844 None 54 Human Binding pKi = 8.4 8.4 1 17
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
1355 2011 None 88 Rat Binding pKi = 8.4 8.4 -1 16
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
142 2011 None 88 Rat Binding pKi = 8.4 8.4 -1 16
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
CHEMBL478 2011 None 88 Rat Binding pKi = 8.4 8.4 -1 16
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
DB12110 2011 None 88 Rat Binding pKi = 8.4 8.4 -1 16
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
59636780 125692 None 0 Chinese hamster Binding pKi = 8.4 8.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 404 5 0 5 3.4 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCCC1 nan
CHEMBL3647274 125692 None 0 Chinese hamster Binding pKi = 8.4 8.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 404 5 0 5 3.4 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCCC1 nan
1588 2325 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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
28864.0 2325 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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 None 27 Rat Binding pKi = 8.3 8.3 -58 44
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
10751317 8649 None 21 Human Binding pKi = 8.3 8.3 19 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 218 5 2 2 2.5 CCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL109526 8649 None 21 Human Binding pKi = 8.3 8.3 19 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 218 5 2 2 2.5 CCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
5 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
5202 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
CHEMBL39 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
DB08839 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
44342722 110543 None 0 Human Binding pKi = 8.3 8.3 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 4 2 2 5.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL325175 110543 None 0 Human Binding pKi = 8.3 8.3 -10 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 4 2 2 5.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
19066235 11385 None 0 Human Binding pKi = 7.4 7.4 75 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL110601 11385 None 0 Human Binding pKi = 7.4 7.4 75 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1180011 11385 None 0 Human Binding pKi = 7.4 7.4 75 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
44376516 56384 None 0 Human Binding pKi = 7.4 7.4 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 6 2 3 4.2 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
CHEMBL163151 56384 None 0 Human Binding pKi = 7.4 7.4 -4 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 6 2 3 4.2 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
2105 3054 None 37 Rat Binding pKi = 7.4 7.4 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 3054 None 37 Rat Binding pKi = 7.4 7.4 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 3054 None 37 Rat Binding pKi = 7.4 7.4 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 3054 None 37 Rat Binding pKi = 7.4 7.4 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 3054 None 37 Rat Binding pKi = 7.4 7.4 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
10782681 109467 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 12 1 2 5.4 CCCCCCCCCOc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL322054 109467 None 0 Human Binding pKi = 7.4 7.4 1 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 12 1 2 5.4 CCCCCCCCCOc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
11740280 102926 None 0 Human Binding pKi = 7.4 7.4 -15 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 376 8 1 2 5.4 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL306197 102926 None 0 Human Binding pKi = 7.4 7.4 -15 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 376 8 1 2 5.4 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
107 141 None 121 Rat Binding pKi = 6.4 6.4 -30 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
1833 141 None 121 Rat Binding pKi = 6.4 6.4 -30 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
CHEMBL8165 141 None 121 Rat Binding pKi = 6.4 6.4 -30 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
161 754 None 6 Rat Binding pKi = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
4284720 754 None 6 Rat Binding pKi = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
CHEMBL1255834 754 None 6 Rat Binding pKi = 6.4 6.4 -16 6
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
14083214 60324 None 2 Rat Binding pKi = 5.4 5.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
CHEMBL1744074 60324 None 2 Rat Binding pKi = 5.4 5.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
441383 20333 None 57 Rat Binding pKi = 4.4 4.4 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 20333 None 57 Rat Binding pKi = 4.4 4.4 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10247448 204389 None 0 Human Binding pKi = 6.4 6.4 -7 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 352 6 1 1 5.3 CCCN(CCC)C1CCc2ccc3[nH]cc(CC(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL71899 204389 None 0 Human Binding pKi = 6.4 6.4 -7 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 352 6 1 1 5.3 CCCN(CCC)C1CCc2ccc3[nH]cc(CC(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL5077293 214491 None 0 Human Binding pKi = 6.4 6.4 -144 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
44376491 55490 None 0 Human Binding pKi = 6.4 6.4 -15 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 1 3 5.4 O=S(=O)(c1cccc2ccccc12)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
CHEMBL162011 55490 None 0 Human Binding pKi = 6.4 6.4 -15 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 1 3 5.4 O=S(=O)(c1cccc2ccccc12)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
73346042 91834 None 5 Human Binding pKi = 6.4 6.4 -4073 17
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 91834 None 5 Human Binding pKi = 6.4 6.4 -4073 17
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
44438462 90974 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 506 6 0 6 6.0 CC1CC(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CC1C 10.1016/j.bmcl.2006.12.109
CHEMBL239598 90974 None 0 Human Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 506 6 0 6 6.0 CC1CC(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CC1C 10.1016/j.bmcl.2006.12.109
182596 118486 None 16 Rat Binding pKi = 6.4 6.4 -269 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL341391 118486 None 16 Rat Binding pKi = 6.4 6.4 -269 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
14083211 77865 None 6 Rat Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@H](C)N)c2c1 10.1021/jm00402a026
CHEMBL2093088 77865 None 6 Rat Binding pKi = 6.4 6.4 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@H](C)N)c2c1 10.1021/jm00402a026
76330157 106247 None 0 Human Binding pKi = 5.4 5.4 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260926 106247 None 0 Human Binding pKi = 5.4 5.4 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138918 106247 None 0 Human Binding pKi = 5.4 5.4 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
59636715 125690 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 440 6 1 5 3.7 O=C(NC1CC(F)(F)C1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647272 125690 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 440 6 1 5 3.7 O=C(NC1CC(F)(F)C1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
9796627 96653 None 0 Human Binding pKi = 6.4 6.4 -14 7
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 96653 None 0 Human Binding pKi = 6.4 6.4 -14 7
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
10359357 200500 None 1 Rat Binding pKi = 6.4 6.4 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 331 1 1 4 3.2 c1ccc2c(c1)OCCc1c(N3CCNCC3)nc3ccccc3c1-2 10.1021/jm00014a021
CHEMBL59871 200500 None 1 Rat Binding pKi = 6.4 6.4 - 1
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 331 1 1 4 3.2 c1ccc2c(c1)OCCc1c(N3CCNCC3)nc3ccccc3c1-2 10.1021/jm00014a021
169764 33114 None 8 Rat Binding pKi = 5.4 5.4 -602 2
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 260 7 2 2 3.5 CCCN(CCC)CCc1c[nH]c2ccc(O)cc12 10.1021/jm00399a031
CHEMBL141706 33114 None 8 Rat Binding pKi = 5.4 5.4 -602 2
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 260 7 2 2 3.5 CCCN(CCC)CCc1c[nH]c2ccc(O)cc12 10.1021/jm00399a031
135398745 2914 None 112 Rat Binding pKi = 6.4 6.4 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
135398745.0 2914 None 112 Rat Binding pKi = 6.4 6.4 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
47 2914 None 112 Rat Binding pKi = 6.4 6.4 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
CHEMBL715 2914 None 112 Rat Binding pKi = 6.4 6.4 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
DB00334 2914 None 112 Rat Binding pKi = 6.4 6.4 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
10403260 204286 None 0 Human Binding pKi = 6.4 6.4 -10 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 0 3 4.0 CCCN(CCC)C1CCc2ccc3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
CHEMBL71299 204286 None 0 Human Binding pKi = 6.4 6.4 -10 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 0 3 4.0 CCCN(CCC)C1CCc2ccc3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
44376262 167097 None 0 Human Binding pKi = 7.4 7.4 -5 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 7 2 4 4.2 COc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL428991 167097 None 0 Human Binding pKi = 7.4 7.4 -5 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 7 2 4 4.2 COc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
59636739 126205 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 469 7 1 6 4.4 Cc1ccc(C(C)NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3650026 126205 None 0 Chinese hamster Binding pKi = 7.4 7.4 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 469 7 1 6 4.4 Cc1ccc(C(C)NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
91965 208030 None 96 Rat Binding pKi = 7.4 7.4 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9746 208030 None 96 Rat Binding pKi = 7.4 7.4 1 2
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
9954663 56524 None 0 Human Binding pKi = 6.4 6.4 -20 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 435 6 1 3 4.3 O=S(=O)(c1ccccc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
CHEMBL163639 56524 None 0 Human Binding pKi = 6.4 6.4 -20 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 435 6 1 3 4.3 O=S(=O)(c1ccccc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
44395809 123104 None 0 Human Binding pKi = 6.4 6.4 -91 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 1 3 3.5 CN1CCC(N2CCc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL361061 123104 None 0 Human Binding pKi = 6.4 6.4 -91 4
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 1 3 3.5 CN1CCC(N2CCc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
9881603 123296 None 0 Human Binding pKi = 5.4 5.4 -134 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 258 2 1 2 3.5 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL361470 123296 None 0 Human Binding pKi = 5.4 5.4 -134 2
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 258 2 1 2 3.5 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCCN1 10.1016/j.bmcl.2004.06.085
10563980 199669 None 0 Rat Binding pKi = 6.4 6.4 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 1.9 N#CC1=Cc2cccc(OCC3CNCCO3)c2CC1 10.1021/jm970806i
CHEMBL59300 199669 None 0 Rat Binding pKi = 6.4 6.4 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 1.9 N#CC1=Cc2cccc(OCC3CNCCO3)c2CC1 10.1021/jm970806i
11812916 112327 None 0 Human Binding pKi = 7.4 7.4 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)cn1 10.1021/jm020938y
CHEMBL329280 112327 None 0 Human Binding pKi = 7.4 7.4 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)cn1 10.1021/jm020938y
150885 98663 None 34 Rat Binding pKi = 7.4 7.4 -8 3
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
CHEMBL1256286 98663 None 34 Rat Binding pKi = 7.4 7.4 -8 3
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
CHEMBL277362 98663 None 34 Rat Binding pKi = 7.4 7.4 -8 3
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
15124076 45845 None 0 Rat Binding pKi = 7.4 7.4 -40 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 438 8 0 5 4.0 CCC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL153136 45845 None 0 Rat Binding pKi = 7.4 7.4 -40 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 438 8 0 5 4.0 CCC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
6603907 33015 None 9 Rat Binding pKi = 7.3 7.3 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
CHEMBL1416204 33015 None 9 Rat Binding pKi = 7.3 7.3 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
24881687 172814 None 0 Human Binding pKi = 6.3 6.3 -3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL451394 172814 None 0 Human Binding pKi = 6.3 6.3 -3 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
10406614 204416 None 0 Human Binding pKi = 7.3 7.3 -457 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 366 7 1 3 4.9 CCCN(CCc1cccs1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL72062 204416 None 0 Human Binding pKi = 7.3 7.3 -457 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 366 7 1 3 4.9 CCCN(CCc1cccs1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10064500 204159 None 0 Human Binding pKi = 5.3 5.3 -2398 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 5 1 1 4.9 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL70606 204159 None 0 Human Binding pKi = 5.3 5.3 -2398 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 5 1 1 4.9 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
9955015 63094 None 5 Rat Binding pKi = 7.3 7.3 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL1744087 63094 None 5 Rat Binding pKi = 7.3 7.3 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL1789131 63094 None 5 Rat Binding pKi = 7.3 7.3 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL5276321 193894 None 0 Rat Binding pKi = 7.3 7.3 - 1
Binding affinity to rat 5-HT1BBinding affinity to rat 5-HT1B
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1COCCN1 10.1016/j.ejmech.2016.07.057
10131024 176161 None 16 Human Binding pKi = 7.3 7.3 -47 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 1 1 3.4 CCc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL45929 176161 None 16 Human Binding pKi = 7.3 7.3 -47 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 1 1 3.4 CCc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
31101 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
31101.0 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
35 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
403 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
CHEMBL493 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
DB01200 729 None 40 Rat Binding pKi = 7.3 7.3 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
135 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
1796 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
4184 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
4184.0 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
CHEMBL6437 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
DB06148 2532 None 43 Rat Binding pKi = 5.3 5.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
10912152 101453 None 0 Human Binding pKi = 6.3 6.3 -89 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 4 1 1 3.9 CC(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL297660 101453 None 0 Human Binding pKi = 6.3 6.3 -89 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 4 1 1 3.9 CC(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
44383728 165346 None 1 Human Binding pKi = 6.3 6.3 -15 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 330 4 1 2 5.2 Clc1ccc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)s1 10.1016/s0960-894x(00)00133-5
CHEMBL423610 165346 None 1 Human Binding pKi = 6.3 6.3 -15 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 330 4 1 2 5.2 Clc1ccc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)s1 10.1016/s0960-894x(00)00133-5
9826801 107937 None 0 Human Binding pKi = 7.3 7.3 -208 11
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 107937 None 0 Human Binding pKi = 7.3 7.3 -208 11
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11016418 106122 None 0 Human Binding pKi = 6.3 6.3 -776 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 106122 None 0 Human Binding pKi = 6.3 6.3 -776 8
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
2470 3653 None 50 Rat Binding pKi = 5.3 5.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
3300 3653 None 50 Rat Binding pKi = 5.3 5.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
5265 3653 None 50 Rat Binding pKi = 5.3 5.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
99 3653 None 50 Rat Binding pKi = 5.3 5.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
CHEMBL267930 3653 None 50 Rat Binding pKi = 5.3 5.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
71062768 143736 None 0 Mouse Binding pKi = 5.3 5.3 -12 4
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL3900699 143736 None 0 Mouse Binding pKi = 5.3 5.3 -12 4
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
10376496 102899 None 0 Human Binding pKi = 6.3 6.3 -147 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 228 3 2 1 3.0 CCCNC1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL305976 102899 None 0 Human Binding pKi = 6.3 6.3 -147 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 228 3 2 1 3.0 CCCNC1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
192260 77244 None 7 Rat Binding pKi = 4.3 4.3 -34 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@H]2C1 10.1021/jm00027a013
CHEMBL2079597 77244 None 7 Rat Binding pKi = 4.3 4.3 -34 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@H]2C1 10.1021/jm00027a013
44582678 181574 None 0 Human Binding pKi = 5.3 5.3 -33 10
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 181574 None 0 Human Binding pKi = 5.3 5.3 -33 10
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
9998026 115384 None 0 Rat Binding pKi = 6.3 6.3 -173 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL335010 115384 None 0 Rat Binding pKi = 6.3 6.3 -173 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10379833 102739 None 0 Human Binding pKi = 7.3 7.3 -162 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 296 6 1 2 3.7 C=CCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL304984 102739 None 0 Human Binding pKi = 7.3 7.3 -162 4
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 296 6 1 2 3.7 C=CCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
1809 134 None 32 Rat Binding pKi = 8.3 8.3 -32 36
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
4 134 None 32 Rat Binding pKi = 8.3 8.3 -32 36
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
CHEMBL18840 134 None 32 Rat Binding pKi = 8.3 8.3 -32 36
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
5 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
5202 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
CHEMBL39 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
DB08839 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
59636778 126224 None 0 Chinese hamster Binding pKi = 8.3 8.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 478 5 0 5 3.5 CC(=O)N1CCc2cc(CCN3CCN(c4cc(F)cc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
CHEMBL3650044 126224 None 0 Chinese hamster Binding pKi = 8.3 8.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 478 5 0 5 3.5 CC(=O)N1CCc2cc(CCN3CCN(c4cc(F)cc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
44402894 98209 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 551 5 0 7 5.8 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL274256 98209 None 0 Human Binding pKi = 8.3 8.3 3 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 551 5 0 7 5.8 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
44402895 124552 None 0 Human Binding pKi = 8.3 8.3 50 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 533 5 1 6 5.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4ncccn4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL364056 124552 None 0 Human Binding pKi = 8.3 8.3 50 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 533 5 1 6 5.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4ncccn4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
9871977 166094 None 0 Human Binding pKi = 8.3 8.3 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 539 5 1 6 4.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(N4CCCC4=O)nc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL425919 166094 None 0 Human Binding pKi = 8.3 8.3 79 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 539 5 1 6 4.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(N4CCCC4=O)nc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
5 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
5202 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
CHEMBL39 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
DB08839 139 None 72 Human Binding pKi = 8.3 8.3 -11 54
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
49850980 56465 None 0 Human Binding pKi = 8.3 8.3 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632213 56465 None 0 Human Binding pKi = 8.3 8.3 -12 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
9957376 176157 None 0 Human Binding pKi = 8.3 8.3 -25 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 457 7 0 4 5.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL459282 176157 None 0 Human Binding pKi = 8.3 8.3 -25 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 457 7 0 4 5.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
17947861 71450 None 1 Human Binding pKi = 8.3 8.3 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 6 2.9 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn(C)c2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL196140 71450 None 1 Human Binding pKi = 8.3 8.3 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 6 2.9 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn(C)c2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
134551 358 None 27 Rat Binding pKi = 8.3 8.3 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
271 358 None 27 Rat Binding pKi = 8.3 8.3 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
885 358 None 27 Rat Binding pKi = 8.3 8.3 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
CHEMBL1403281 358 None 27 Rat Binding pKi = 8.3 8.3 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
5 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5202 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
CHEMBL39 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
DB08839 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
5202 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
CHEMBL39 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
DB08839 139 None 72 Rat Binding pKi = 8.3 8.3 -13 54
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
2543 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358.0 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
54 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
CHEMBL128 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
DB00669 3707 None 68 Human Binding pKi = 8.3 8.3 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
10775128 188731 None 3 Human Binding pKi = 8.3 8.3 -2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL50492 188731 None 3 Human Binding pKi = 8.3 8.3 -2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
44342767 114959 None 0 Human Binding pKi = 8.2 8.2 -8 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL334259 114959 None 0 Human Binding pKi = 8.2 8.2 -8 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
11016395 111553 None 0 Human Binding pKi = 8.2 8.2 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1nccc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL328048 111553 None 0 Human Binding pKi = 8.2 8.2 -1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1nccc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
2303 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
4946 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
564 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
63 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
91536 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
CHEMBL27 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
CHEMBL452861 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
DB00571 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
59636757 125707 None 0 Chinese hamster Binding pKi = 7.3 7.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 448 7 1 6 3.3 O=C(NCC1CCOCC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647289 125707 None 0 Chinese hamster Binding pKi = 7.3 7.3 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 448 7 1 6 3.3 O=C(NCC1CCOCC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
2303 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
4946 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
564 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
63 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
91536 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL27 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL452861 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
DB00571 3187 None 68 Rat Binding pKi = 7.3 7.3 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
44402878 71407 None 0 Human Binding pKi = 7.3 7.3 2 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 506 4 1 5 5.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195897 71407 None 0 Human Binding pKi = 7.3 7.3 2 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 506 4 1 5 5.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
44588721 184346 None 0 Human Binding pKi = 7.3 7.3 -6 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.3 Cc1ccc2c(OCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484387 184346 None 0 Human Binding pKi = 7.3 7.3 -6 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.3 Cc1ccc2c(OCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
10024936 184963 None 0 Human Binding pKi = 7.3 7.3 -19 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485395 184963 None 0 Human Binding pKi = 7.3 7.3 -19 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
24865542 188127 None 0 Human Binding pKi = 7.3 7.3 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 1 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL498355 188127 None 0 Human Binding pKi = 7.3 7.3 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 1 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
10194820 188864 None 0 Human Binding pKi = 7.3 7.3 -158 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 432 7 0 5 3.7 CC(=O)N(C)c1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL506942 188864 None 0 Human Binding pKi = 7.3 7.3 -158 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 432 7 0 5 3.7 CC(=O)N(C)c1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
9891618 107124 None 0 Human Binding pKi = 6.3 6.3 -501 6
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 107124 None 0 Human Binding pKi = 6.3 6.3 -501 6
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 107408 None 0 Human Binding pKi = 6.3 6.3 -501 7
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 107408 None 0 Human Binding pKi = 6.3 6.3 -501 7
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
24865539 187645 None 0 Human Binding pKi = 6.3 6.3 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
CHEMBL494991 187645 None 0 Human Binding pKi = 6.3 6.3 -39 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
1534 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
14975310 77233 None 0 Rat Binding pKi = 5.3 5.3 -66 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@@H]2C1 10.1021/jm00027a013
CHEMBL2079544 77233 None 0 Rat Binding pKi = 5.3 5.3 -66 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@@H]2C1 10.1021/jm00027a013
9957068 51944 None 0 Human Binding pKi = 5.3 5.3 -1000 5
Evaluated for the binding affinity to 5-hydroxytryptamine 1B receptorEvaluated for the binding affinity to 5-hydroxytryptamine 1B receptor
ChEMBL 486 8 1 5 4.3 CS(=O)(=O)Oc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccc(F)cc3)CC1)C2 10.1016/s0960-894x(01)00037-3
CHEMBL158627 51944 None 0 Human Binding pKi = 5.3 5.3 -1000 5
Evaluated for the binding affinity to 5-hydroxytryptamine 1B receptorEvaluated for the binding affinity to 5-hydroxytryptamine 1B receptor
ChEMBL 486 8 1 5 4.3 CS(=O)(=O)Oc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccc(F)cc3)CC1)C2 10.1016/s0960-894x(01)00037-3
10164215 142009 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 504 6 1 8 3.2 COc1cc(N2CCN(C)CC2)c2nc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(N(C)C)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL387545 142009 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 504 6 1 8 3.2 COc1cc(N2CCN(C)CC2)c2nc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(N(C)C)c2c1 10.1016/j.bmc.2006.10.037
44339072 111378 None 1 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 5 1 3 2.8 CC(C)C(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL327103 111378 None 1 Human Binding pKi = 7.3 7.3 1 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 5 1 3 2.8 CC(C)C(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
4376990 193009 None 5 Human Binding pKi = 7.3 7.3 -20 11
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 193009 None 5 Human Binding pKi = 7.3 7.3 -20 11
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 193009 None 5 Human Binding pKi = 7.3 7.3 -20 11
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
1574 81 None 60 Rat Binding pKi = 6.3 6.3 -24 21
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
218 81 None 60 Rat Binding pKi = 6.3 6.3 -24 21
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
CHEMBL266591 81 None 60 Rat Binding pKi = 6.3 6.3 -24 21
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
44581972 175600 None 0 Human Binding pKi = 6.3 6.3 -17 10
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 175600 None 0 Human Binding pKi = 6.3 6.3 -17 10
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
10663236 5461 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 11 2 2 5.2 CCCCCCCCCOc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm950498t
CHEMBL107487 5461 None 0 Human Binding pKi = 7.3 7.3 - 1
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 11 2 2 5.2 CCCCCCCCCOc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm950498t
3025067 99382 None 64 Rat Binding pKi = 7.3 7.3 -2 15
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
65853 99382 None 64 Rat Binding pKi = 7.3 7.3 -2 15
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
CHEMBL282614 99382 None 64 Rat Binding pKi = 7.3 7.3 -2 15
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
10248619 115130 None 0 Rat Binding pKi = 6.3 6.3 -138 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 370 3 0 4 3.6 Clc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL334381 115130 None 0 Rat Binding pKi = 6.3 6.3 -138 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 370 3 0 4 3.6 Clc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9997421 204137 None 0 Human Binding pKi = 6.3 6.3 -22 3
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
CHEMBL70431 204137 None 0 Human Binding pKi = 6.3 6.3 -22 3
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
1220 187 None 55 Human Binding pKi = 6.3 6.3 -208 44
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
31 187 None 55 Human Binding pKi = 6.3 6.3 -208 44
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
7 187 None 55 Human Binding pKi = 6.3 6.3 -208 44
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
CHEMBL56 187 None 55 Human Binding pKi = 6.3 6.3 -208 44
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
1534 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 103040 None 53 Human Binding pKi = 6.3 6.3 -5 12
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
2435 3590 None 83 Human Binding pKi = 7.3 7.3 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 3590 None 83 Human Binding pKi = 7.3 7.3 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 3590 None 83 Human Binding pKi = 7.3 7.3 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 3590 None 83 Human Binding pKi = 7.3 7.3 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 3590 None 83 Human Binding pKi = 7.3 7.3 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
10021450 102702 None 0 Human Binding pKi = 7.3 7.3 -1412 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 360 7 1 2 4.8 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL304767 102702 None 0 Human Binding pKi = 7.3 7.3 -1412 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 360 7 1 2 4.8 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10973768 107560 None 0 Human Binding pKi = 6.3 6.3 -1445 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 107560 None 0 Human Binding pKi = 6.3 6.3 -1445 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
9976035 21050 None 0 Rat Binding pKi = 6.3 6.3 -489 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
CHEMBL131184 21050 None 0 Rat Binding pKi = 6.3 6.3 -489 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
14519861 59164 None 0 Rat Binding pKi = 5.3 5.3 -25 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 313 11 0 2 5.5 CCCCN(CCCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL169956 59164 None 0 Rat Binding pKi = 5.3 5.3 -25 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 313 11 0 2 5.5 CCCCN(CCCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
44304338 100580 None 0 Rat Binding pKi = 6.2 6.2 -5 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 275 6 0 2 4.0 CCCN(CCC)C1CCc2c(C)ccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
CHEMBL291620 100580 None 0 Rat Binding pKi = 6.2 6.2 -5 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 275 6 0 2 4.0 CCCN(CCC)C1CCc2c(C)ccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
3228 3146 None 23 Human Binding pKi = 5.2 5.2 -6456 7
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
9909448 3146 None 23 Human Binding pKi = 5.2 5.2 -6456 7
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
CHEMBL71838 3146 None 23 Human Binding pKi = 5.2 5.2 -6456 7
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
3228 3146 None 23 Western lowland gorilla Binding pKi = 5.2 5.2 -6456 7
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
9909448 3146 None 23 Western lowland gorilla Binding pKi = 5.2 5.2 -6456 7
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
CHEMBL71838 3146 None 23 Western lowland gorilla Binding pKi = 5.2 5.2 -6456 7
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
10774567 103822 None 0 Human Binding pKi = 5.2 5.2 -5 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(O)c(C)c1CC1=NCCN1 10.1021/jm970513p
CHEMBL309162 103822 None 0 Human Binding pKi = 5.2 5.2 -5 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(O)c(C)c1CC1=NCCN1 10.1021/jm970513p
44376395 52594 None 0 Human Binding pKi = 7.2 7.2 -9 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 7 2 4 4.8 COc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL159278 52594 None 0 Human Binding pKi = 7.2 7.2 -9 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 7 2 4 4.8 COc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL5094234 215573 None 0 Human Binding pKi = 6.2 6.2 -275 8
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 215573 None 0 Human Binding pKi = 6.2 6.2 -275 8
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
23288790 203964 None 0 Western lowland gorilla Binding pKi = 5.2 5.2 -691 6
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL69385 203964 None 0 Western lowland gorilla Binding pKi = 5.2 5.2 -691 6
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9972838 204303 None 0 Human Binding pKi = 6.2 6.2 -41 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 1 2 4.4 CCCN(CCC)C1CCc2ccc3[nH]cc(C(C)=O)c3c2C1 10.1021/jm00012a021
CHEMBL71395 204303 None 0 Human Binding pKi = 6.2 6.2 -41 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 1 2 4.4 CCCN(CCC)C1CCc2ccc3[nH]cc(C(C)=O)c3c2C1 10.1021/jm00012a021
44581974 175704 None 0 Human Binding pKi = 6.2 6.2 -11 9
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 175704 None 0 Human Binding pKi = 6.2 6.2 -11 9
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
2585 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
2585.0 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
522 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
551 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
CHEMBL723 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
DB01136 803 None 103 Rat Binding pKi = 6.2 6.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
160463 69188 None 31 Rat Binding pKi = 5.2 5.2 -3 3
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cc(O)ccc12 10.1021/jm00384a001
CHEMBL19264 69188 None 31 Rat Binding pKi = 5.2 5.2 -3 3
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cc(O)ccc12 10.1021/jm00384a001
44338900 109644 None 1 Human Binding pKi = 7.2 7.2 -3 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 260 5 1 3 2.6 CCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL322349 109644 None 1 Human Binding pKi = 7.2 7.2 -3 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 260 5 1 3 2.6 CCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
10915350 163406 None 0 Human Binding pKi = 6.2 6.2 -53 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(C#N)c4)nc23)CC1 10.1021/jm030020m
CHEMBL419547 163406 None 0 Human Binding pKi = 6.2 6.2 -53 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(C#N)c4)nc23)CC1 10.1021/jm030020m
10500422 78475 None 0 Human Binding pKi = 8.2 8.2 15 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
CHEMBL2111779 78475 None 0 Human Binding pKi = 8.2 8.2 15 3
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
130 3500 None 47 Human Binding pKi = 8.2 8.2 -1 13
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
3378093 3500 None 47 Human Binding pKi = 8.2 8.2 -1 13
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
CHEMBL281350 3500 None 47 Human Binding pKi = 8.2 8.2 -1 13
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
11796257 98680 None 1 Human Binding pKi = 8.2 8.2 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 417 4 1 4 3.8 COc1ccc(NC(=O)c2ccc(Br)c(C)c2)cc1N1CCN(C)CC1 10.1021/jm970457s
CHEMBL277467 98680 None 1 Human Binding pKi = 8.2 8.2 1 3
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 417 4 1 4 3.8 COc1ccc(NC(=O)c2ccc(Br)c(C)c2)cc1N1CCN(C)CC1 10.1021/jm970457s
10114480 93596 None 0 Human Binding pKi = 8.2 8.2 -3 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL246597 93596 None 0 Human Binding pKi = 8.2 8.2 -3 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10195275 175692 None 0 Human Binding pKi = 8.2 8.2 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 0 5 4.6 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL458199 175692 None 0 Human Binding pKi = 8.2 8.2 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 0 5 4.6 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44581603 176058 None 0 Human Binding pKi = 8.2 8.2 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 1 4 5.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCNCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL459067 176058 None 0 Human Binding pKi = 8.2 8.2 -5 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 1 4 5.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCNCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10127673 187832 None 0 Human Binding pKi = 8.2 8.2 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL496098 187832 None 0 Human Binding pKi = 8.2 8.2 -6 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10048343 184219 None 0 Human Binding pKi = 8.2 8.2 -10 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 430 6 1 5 4.0 Cc1ccc2c(N3CCN(CCCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL483365 184219 None 0 Human Binding pKi = 8.2 8.2 -10 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 430 6 1 5 4.0 Cc1ccc2c(N3CCN(CCCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10127673 187832 None 0 Human Binding pKi = 8.2 8.2 -6 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL496098 187832 None 0 Human Binding pKi = 8.2 8.2 -6 3
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
10481003 102953 None 0 Rat Binding pKi = 8.2 8.2 -1 3
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(C(=O)Nc2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
CHEMBL306384 102953 None 0 Rat Binding pKi = 8.2 8.2 -1 3
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(C(=O)Nc2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
9891594 104881 None 0 Rat Binding pKi = 8.2 8.2 -1 3
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 486 6 1 5 4.4 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=O)N(C)C)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
CHEMBL311150 104881 None 0 Rat Binding pKi = 8.2 8.2 -1 3
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 486 6 1 5 4.4 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=O)N(C)C)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
10076876 101712 None 0 Human Binding pKi = 8.2 8.2 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
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 None 0 Human Binding pKi = 8.2 8.2 -1 3
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
2543 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
5358 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
5358.0 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
54 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
CHEMBL128 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
DB00669 3707 None 68 Western lowland gorilla Binding pKi = 8.2 8.2 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
107 141 None 121 Rat Binding pKi = 8.2 8.2 -30 30
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
1833 141 None 121 Rat Binding pKi = 8.2 8.2 -30 30
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
CHEMBL8165 141 None 121 Rat Binding pKi = 8.2 8.2 -30 30
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
11092142 208168 None 0 Human Binding pKi = 8.2 8.2 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL98299 208168 None 0 Human Binding pKi = 8.2 8.2 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
9817810 17372 None 1 Human Binding pKi = 8.2 8.2 -2 8
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 17372 None 1 Human Binding pKi = 8.2 8.2 -2 8
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
59636777 125689 None 0 Chinese hamster Binding pKi = 8.2 8.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 6 1 5 3.1 O=C(NC1CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647271 125689 None 0 Chinese hamster Binding pKi = 8.2 8.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 6 1 5 3.1 O=C(NC1CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
10944016 207899 None 20 Rat Binding pKi = 8.2 8.2 1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 220 3 1 3 1.9 CC(C)Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9669 207899 None 20 Rat Binding pKi = 8.2 8.2 1 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 220 3 1 3 1.9 CC(C)Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
4233538 198048 None 4 Rat Binding pKi = 7.2 7.2 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
CHEMBL1201939 198048 None 4 Rat Binding pKi = 7.2 7.2 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
CHEMBL57406 198048 None 4 Rat Binding pKi = 7.2 7.2 - 1
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
44560995 179153 None 0 Human Binding pKi = 7.2 7.2 -109 3
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 179153 None 0 Human Binding pKi = 7.2 7.2 -109 3
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
10198320 204610 None 1 Human Binding pKi = 6.2 6.2 -46 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 218 2 2 1 3.1 Cc1cc(C(C)(C)C)cc(C)c1CC(=N)N 10.1021/jm970513p
CHEMBL73281 204610 None 1 Human Binding pKi = 6.2 6.2 -46 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 218 2 2 1 3.1 Cc1cc(C(C)(C)C)cc(C)c1CC(=N)N 10.1021/jm970513p
11024618 108553 None 0 Human Binding pKi = 5.2 5.2 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 2 4 3.2 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL320198 108553 None 0 Human Binding pKi = 5.2 5.2 -89 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 2 4 3.2 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
107992 2553 None 49 Rat Binding pKi = 5.2 5.2 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
165 2553 None 49 Rat Binding pKi = 5.2 5.2 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
CHEMBL269521 2553 None 49 Rat Binding pKi = 5.2 5.2 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
DB12111 2553 None 49 Rat Binding pKi = 5.2 5.2 -12 10
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
182595 19937 None 14 Rat Binding pKi = 6.2 6.2 -1000 4
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130276 19937 None 14 Rat Binding pKi = 6.2 6.2 -1000 4
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
25067564 201300 None 0 Human Binding pKi = 5.2 5.2 -1348 6
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 201300 None 0 Human Binding pKi = 5.2 5.2 -1348 6
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
9860595 10085 None 2 Human Binding pKi = 6.2 6.2 -77 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL115415 10085 None 2 Human Binding pKi = 6.2 6.2 -77 2
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/s0960-894x(03)00779-0
9860595 10085 None 2 Human Binding pKi = 6.2 6.2 -77 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/j.bmcl.2003.11.023
CHEMBL115415 10085 None 2 Human Binding pKi = 6.2 6.2 -77 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/j.bmcl.2003.11.023
11822996 5059 None 0 Human Binding pKi = 6.2 6.2 -32 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 308 3 2 4 1.7 CN1CCC(c2c[nH]c3ccc(NS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
CHEMBL105327 5059 None 0 Human Binding pKi = 6.2 6.2 -32 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 308 3 2 4 1.7 CN1CCC(c2c[nH]c3ccc(NS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
14519859 130209 None 2 Rat Binding pKi = 5.2 5.2 -13 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 285 9 0 2 4.7 CCCN(CCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL367935 130209 None 2 Rat Binding pKi = 5.2 5.2 -13 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 285 9 0 2 4.7 CCCN(CCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
3823 50221 None 42 Rat Binding pKi = 5.2 5.2 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
76973198 50221 None 42 Rat Binding pKi = 5.2 5.2 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL157101 50221 None 42 Rat Binding pKi = 5.2 5.2 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10091074 116666 None 0 Rat Binding pKi = 6.2 6.2 -776 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
CHEMBL337078 116666 None 0 Rat Binding pKi = 6.2 6.2 -776 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
10065239 204289 None 0 Human Binding pKi = 6.2 6.2 -21 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 6 0 3 4.1 CCCN(CCC)C1CCc2cc(F)c3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
CHEMBL71319 204289 None 0 Human Binding pKi = 6.2 6.2 -21 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 6 0 3 4.1 CCCN(CCC)C1CCc2cc(F)c3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
44376722 55494 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 6 2 3 4.5 Cc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162012 55494 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 6 2 3 4.5 Cc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
44339071 8435 None 1 Human Binding pKi = 7.2 7.2 1 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 4 1 3 3.2 CN(C)CCc1c[nH]c2ccc(OC(=O)C(C)(C)C)cc12 10.1021/jm950498t
CHEMBL109360 8435 None 1 Human Binding pKi = 7.2 7.2 1 2
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 4 1 3 3.2 CN(C)CCc1c[nH]c2ccc(OC(=O)C(C)(C)C)cc12 10.1021/jm950498t
59636760 125697 None 0 Chinese hamster Binding pKi = 7.2 7.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1cccnc1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647279 125697 None 0 Chinese hamster Binding pKi = 7.2 7.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1cccnc1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
10150796 67608 None 0 Human Binding pKi = 7.2 7.2 -251 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 401 6 1 5 3.6 Cc1ccc2c(OCCN3CCN(Cc4cccc5[nH]cnc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL190298 67608 None 0 Human Binding pKi = 7.2 7.2 -251 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 401 6 1 5 3.6 Cc1ccc2c(OCCN3CCN(Cc4cccc5[nH]cnc45)CC3)cccc2n1 10.1021/jm049039v
44443098 93929 None 0 Human Binding pKi = 7.2 7.2 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 522 8 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(Cc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248231 93929 None 0 Human Binding pKi = 7.2 7.2 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 522 8 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(Cc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10238762 174912 None 0 Human Binding pKi = 7.2 7.2 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456458 174912 None 0 Human Binding pKi = 7.2 7.2 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10216744 174913 None 0 Human Binding pKi = 7.2 7.2 -7 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 7 0 3 6.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccccc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456459 174913 None 0 Human Binding pKi = 7.2 7.2 -7 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 7 0 3 6.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccccc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
7096 207478 None 119 Rat Binding pKi = 7.2 7.2 7 4
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00125a020
CHEMBL9434 207478 None 119 Rat Binding pKi = 7.2 7.2 7 4
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00125a020
2247 505 None 81 Rat Binding pKi = 6.2 6.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
249 505 None 81 Rat Binding pKi = 6.2 6.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
2603 505 None 81 Rat Binding pKi = 6.2 6.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
CHEMBL296419 505 None 81 Rat Binding pKi = 6.2 6.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
DB00637 505 None 81 Rat Binding pKi = 6.2 6.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
7694 3511 None 36 Human Binding pKi = 6.2 6.2 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
9910352 3511 None 36 Human Binding pKi = 6.2 6.2 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
CHEMBL2219578 3511 None 36 Human Binding pKi = 6.2 6.2 -316 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
10045226 21765 None 0 Rat Binding pKi = 6.2 6.2 -489 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 6 0 4 4.1 c1ccc2c(c1)CC2CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131900 21765 None 0 Rat Binding pKi = 6.2 6.2 -489 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 6 0 4 4.1 c1ccc2c(c1)CC2CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9890119 208057 None 0 Human Binding pKi = 6.2 6.2 -630 7
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 208057 None 0 Human Binding pKi = 6.2 6.2 -630 7
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
11191906 11767 None 0 Human Binding pKi = 6.2 6.2 -12 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 11767 None 0 Human Binding pKi = 6.2 6.2 -12 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 11767 None 0 Human Binding pKi = 6.2 6.2 -12 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
9827938 11771 None 0 Human Binding pKi = 6.2 6.2 -25 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 11771 None 0 Human Binding pKi = 6.2 6.2 -25 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 11771 None 0 Human Binding pKi = 6.2 6.2 -25 12
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
10028436 3532 None 5 Human Binding pKi = 6.2 6.2 -316 12
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 3532 None 5 Human Binding pKi = 6.2 6.2 -316 12
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 3532 None 5 Human Binding pKi = 6.2 6.2 -316 12
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
10238160 124193 None 0 Human Binding pKi = 6.2 6.2 -158 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4cc(Cl)ccc4Cl)CC3)cccc2n1 10.1021/jm049039v
CHEMBL363413 124193 None 0 Human Binding pKi = 6.2 6.2 -158 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4cc(Cl)ccc4Cl)CC3)cccc2n1 10.1021/jm049039v
44439167 90557 None 0 Human Binding pKi = 6.2 6.2 -63 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238732 90557 None 0 Human Binding pKi = 6.2 6.2 -63 10
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
44588772 185120 None 0 Human Binding pKi = 6.2 6.2 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 6 3.8 Cc1ccc2c(OCC3CCN(CC(=O)c4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485630 185120 None 0 Human Binding pKi = 6.2 6.2 -2 3
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 6 3.8 Cc1ccc2c(OCC3CCN(CC(=O)c4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
9935387 99442 None 0 Human Binding pKi = 6.2 6.2 -794 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 99442 None 0 Human Binding pKi = 6.2 6.2 -794 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 100992 None 0 Human Binding pKi = 6.2 6.2 -794 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 100992 None 0 Human Binding pKi = 6.2 6.2 -794 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
1220 187 None 55 Rat Binding pKi = 4.2 4.2 -7413 44
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
31 187 None 55 Rat Binding pKi = 4.2 4.2 -7413 44
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
7 187 None 55 Rat Binding pKi = 4.2 4.2 -7413 44
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
CHEMBL56 187 None 55 Rat Binding pKi = 4.2 4.2 -7413 44
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
71459604 83793 None 0 Human Binding pKi = 5.2 5.2 -11 14
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 83793 None 0 Human Binding pKi = 5.2 5.2 -11 14
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
10767427 84394 None 1 Human Binding pKi = 5.2 5.2 -1258 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
CHEMBL2113352 84394 None 1 Human Binding pKi = 5.2 5.2 -1258 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
CHEMBL2219586 84394 None 1 Human Binding pKi = 5.2 5.2 -1258 4
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
44304328 202909 None 0 Rat Binding pKi = 5.2 5.2 -4 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 311 6 0 2 4.8 CCCN(CCC)C1CCc2c(c(OC)cc3ccccc23)C1 10.1016/S0960-894X(01)81009-X
CHEMBL62776 202909 None 0 Rat Binding pKi = 5.2 5.2 -4 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 311 6 0 2 4.8 CCCN(CCC)C1CCc2c(c(OC)cc3ccccc23)C1 10.1016/S0960-894X(01)81009-X
1220 187 None 55 Human Binding pKi = 6.2 6.2 -208 44
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
31 187 None 55 Human Binding pKi = 6.2 6.2 -208 44
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
7 187 None 55 Human Binding pKi = 6.2 6.2 -208 44
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
CHEMBL56 187 None 55 Human Binding pKi = 6.2 6.2 -208 44
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
44376278 169104 None 0 Human Binding pKi = 7.2 7.2 -2 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 6 2 3 5.1 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
CHEMBL440008 169104 None 0 Human Binding pKi = 7.2 7.2 -2 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 6 2 3 5.1 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
10733070 168468 None 0 Rat Binding pKi = 6.2 6.2 37 2
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 301 1 0 3 3.6 CN1CCN(c2cc3c4c(cccc4n2)-c2ccccc2-3)CC1 10.1021/jm981112s
CHEMBL43512 168468 None 0 Rat Binding pKi = 6.2 6.2 37 2
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 301 1 0 3 3.6 CN1CCN(c2cc3c4c(cccc4n2)-c2ccccc2-3)CC1 10.1021/jm981112s
CHEMBL5081379 214746 None 0 Human Binding pKi = 6.2 6.2 -97 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11727140 109393 None 0 Human Binding pKi = 6.2 6.2 -58 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 326 3 2 3 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCCC4)nc23)CC1 10.1021/jm030020m
CHEMBL321967 109393 None 0 Human Binding pKi = 6.2 6.2 -58 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 326 3 2 3 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCCC4)nc23)CC1 10.1021/jm030020m
21830793 91835 None 10 Human Binding pKi = 6.2 6.2 -4265 45
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 91835 None 10 Human Binding pKi = 6.2 6.2 -4265 45
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
10338821 20799 None 0 Rat Binding pKi = 6.2 6.2 -1445 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 5 0 4 3.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130976 20799 None 0 Rat Binding pKi = 6.2 6.2 -1445 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 5 0 4 3.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
44376541 165388 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
CHEMBL423789 165388 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
59636738 126211 None 0 Chinese hamster Binding pKi = 7.2 7.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1ccnc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)c1 nan
CHEMBL3650032 126211 None 0 Chinese hamster Binding pKi = 7.2 7.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1ccnc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)c1 nan
11393666 192986 None 0 Rat Binding pKi = 6.2 6.2 -1698 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 192986 None 0 Rat Binding pKi = 6.2 6.2 -1698 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 192986 None 0 Rat Binding pKi = 6.2 6.2 -1698 19
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
283 3130 None 57 Rat Binding pKi = 5.2 5.2 -6606 12
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
4847 3130 None 57 Rat Binding pKi = 5.2 5.2 -6606 12
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
CHEMBL18331 3130 None 57 Rat Binding pKi = 5.2 5.2 -6606 12
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
76322956 106204 None 0 Human Binding pKi = 5.2 5.2 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260927 106204 None 0 Human Binding pKi = 5.2 5.2 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138744 106204 None 0 Human Binding pKi = 5.2 5.2 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
9826761 112022 None 0 Human Binding pKi = 7.2 7.2 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL328940 112022 None 0 Human Binding pKi = 7.2 7.2 1 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
125957 120160 None 8 Rat Binding pKi = 7.2 7.2 -1 2
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
CHEMBL351530 120160 None 8 Rat Binding pKi = 7.2 7.2 -1 2
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
10432483 23265 None 0 Rat Binding pKi = 6.2 6.2 -426 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 6 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)CC2 10.1021/jm00020a020
CHEMBL133188 23265 None 0 Rat Binding pKi = 6.2 6.2 -426 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 6 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)CC2 10.1021/jm00020a020
10917920 111446 None 0 Human Binding pKi = 7.2 7.2 -85 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 111446 None 0 Human Binding pKi = 7.2 7.2 -85 9
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
44376272 120229 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 6 2 3 4.8 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
CHEMBL352181 120229 None 0 Human Binding pKi = 7.2 7.2 -7 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 6 2 3 4.8 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
10130620 103649 None 3 Human Binding pKi = 5.2 5.2 -64 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 216 2 1 2 2.5 CC(C)(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
CHEMBL308727 103649 None 3 Human Binding pKi = 5.2 5.2 -64 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 216 2 1 2 2.5 CC(C)(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
9998873 19566 None 0 Rat Binding pKi = 6.2 6.2 -1047 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.4 c1ccc2c(c1)CC(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL129993 19566 None 0 Rat Binding pKi = 6.2 6.2 -1047 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.4 c1ccc2c(c1)CC(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
72550645 114089 None 0 Human Binding pKi = 8.2 8.2 1 8
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 114089 None 0 Human Binding pKi = 8.2 8.2 1 8
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
59636779 126214 None 0 Chinese hamster Binding pKi = 8.2 8.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 446 5 0 5 3.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cccc(C(F)(F)F)n4)CC3)c2o1 nan
CHEMBL3650035 126214 None 0 Chinese hamster Binding pKi = 8.2 8.2 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 446 5 0 5 3.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cccc(C(F)(F)F)n4)CC3)c2o1 nan
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
20810 9185 None 22 Human Binding pKi = 8.1 8.1 -5 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 202 3 2 2 1.9 CC(=O)c1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL110317 9185 None 22 Human Binding pKi = 8.1 8.1 -5 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 202 3 2 2 1.9 CC(=O)c1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636713 125696 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 466 7 1 7 3.4 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3647278 125696 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 466 7 1 7 3.4 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
2543 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
5358 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
5358.0 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
54 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
CHEMBL128 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
DB00669 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
2543 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
5358 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
5358.0 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
54 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
CHEMBL128 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
DB00669 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
59636722 126221 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccnc1CCN1CCN(c2cccc3cc(C(=O)N(C)C)oc23)CC1 nan
CHEMBL3650041 126221 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccnc1CCN1CCN(c2cccc3cc(C(=O)N(C)C)oc23)CC1 nan
188006 5468 None 14 Human Binding pKi = 8.1 8.1 -2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 188 3 2 1 2.2 CCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL107511 5468 None 14 Human Binding pKi = 8.1 8.1 -2 3
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 188 3 2 1 2.2 CCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44402893 69809 None 0 Human Binding pKi = 8.1 8.1 63 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 470 4 1 5 4.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cc(C)ncc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL193616 69809 None 0 Human Binding pKi = 8.1 8.1 63 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 470 4 1 5 4.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cc(C)ncc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
71458050 79017 None 0 Human Binding pKi = 8.1 8.1 3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 6 2.5 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL2113097 79017 None 0 Human Binding pKi = 8.1 8.1 3 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 6 2.5 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
44402888 140532 None 0 Human Binding pKi = 8.1 8.1 25 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 446 3 1 4 4.6 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL381035 140532 None 0 Human Binding pKi = 8.1 8.1 25 2
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 446 3 1 4 4.6 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402871 168597 None 0 Human Binding pKi = 8.1 8.1 10 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 462 3 1 4 5.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL435936 168597 None 0 Human Binding pKi = 8.1 8.1 10 3
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 462 3 1 4 5.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
49852105 56388 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 346 4 1 4 3.5 Cc1ccc2c(N3CCN(CCc4cccc(N)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631534 56388 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 346 4 1 4 3.5 Cc1ccc2c(N3CCN(CCc4cccc(N)c4)CC3)cccc2n1 10.1021/jm100714c
44443093 154693 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 446 6 0 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL399719 154693 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 446 6 0 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10288132 177017 None 0 Human Binding pKi = 8.1 8.1 -7 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccncc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL462916 177017 None 0 Human Binding pKi = 8.1 8.1 -7 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccncc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10127877 189562 None 0 Human Binding pKi = 8.1 8.1 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL514429 189562 None 0 Human Binding pKi = 8.1 8.1 -12 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44580741 192670 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL521873 192670 None 0 Human Binding pKi = 8.1 8.1 -15 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
75 3514 None 7 Human Binding pKi = 8.1 8.1 -3 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
9870500 3514 None 7 Human Binding pKi = 8.1 8.1 -3 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
CHEMBL191971 3514 None 7 Human Binding pKi = 8.1 8.1 -3 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
44404264 72542 None 0 Human Binding pKi = 8.1 8.1 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 4 1 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5C[C@H](C)N[C@H](C)C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL199144 72542 None 0 Human Binding pKi = 8.1 8.1 1 3
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 4 1 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5C[C@H](C)N[C@H](C)C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
10403999 60050 None 0 Human Binding pKi = 7.2 7.2 -27 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 324 4 1 2 5.3 CC1CCC(C)N1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL173656 60050 None 0 Human Binding pKi = 7.2 7.2 -27 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 324 4 1 2 5.3 CC1CCC(C)N1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
10068933 103801 None 0 Human Binding pKi = 7.2 7.2 -3 4
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
CHEMBL309021 103801 None 0 Human Binding pKi = 7.2 7.2 -3 4
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
168293874 192179 None 0 Human Binding pKi = 7.2 7.2 -16 11
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 192179 None 0 Human Binding pKi = 7.2 7.2 -16 11
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
73350823 102530 None 0 Human Binding pKi = 6.2 6.2 -45 9
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 102530 None 0 Human Binding pKi = 6.2 6.2 -45 9
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 102530 None 0 Human Binding pKi = 6.2 6.2 -45 9
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
10068239 22471 None 0 Rat Binding pKi = 6.2 6.2 -257 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 4 0 4 4.1 c1ccc2c(c1)CCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL132514 22471 None 0 Rat Binding pKi = 6.2 6.2 -257 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 4 0 4 4.1 c1ccc2c(c1)CCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
10091445 118485 None 0 Rat Binding pKi = 6.2 6.2 -316 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 384 4 0 4 4.0 Clc1cccc2c1CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL341390 118485 None 0 Rat Binding pKi = 6.2 6.2 -316 3
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 384 4 0 4 4.0 Clc1cccc2c1CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
73213195 104459 None 0 Human Binding pKi = 6.2 6.2 -24 12
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 None 0 Human Binding pKi = 6.2 6.2 -24 12
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
76312088 106211 None 0 Human Binding pKi = 7.2 7.2 3 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
CHEMBL2260929 106211 None 0 Human Binding pKi = 7.2 7.2 3 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
CHEMBL3138771 106211 None 0 Human Binding pKi = 7.2 7.2 3 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
9816035 204133 None 1 Human Binding pKi = 6.2 6.2 -104 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 2 1 2 2.8 Cc1cc(C(C)(C)C)ccc1CC1=NCCN1 10.1021/jm970513p
CHEMBL70409 204133 None 1 Human Binding pKi = 6.2 6.2 -104 2
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 2 1 2 2.8 Cc1cc(C(C)(C)C)ccc1CC1=NCCN1 10.1021/jm970513p
71457690 83798 None 0 Human Binding pKi = 5.2 5.2 -6 5
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 83798 None 0 Human Binding pKi = 5.2 5.2 -6 5
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
10266598 120371 None 1 Human Binding pKi = 6.2 6.2 -37 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 296 4 1 2 4.5 c1csc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)c1 10.1016/s0960-894x(00)00133-5
CHEMBL353256 120371 None 1 Human Binding pKi = 6.2 6.2 -37 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 296 4 1 2 4.5 c1csc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)c1 10.1016/s0960-894x(00)00133-5
73213195 104459 None 0 Human Binding pKi = 6.2 6.2 -24 12
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 104459 None 0 Human Binding pKi = 6.2 6.2 -24 12
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
9947817 5047 None 0 Human Binding pKi = 6.1 6.1 -131 9
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105261 5047 None 0 Human Binding pKi = 6.1 6.1 -131 9
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
9863333 204365 None 0 Western lowland gorilla Binding pKi = 5.1 5.1 -5128 10
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71724 204365 None 0 Western lowland gorilla Binding pKi = 5.1 5.1 -5128 10
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
899056 63066 None 4 Rat Binding pKi = 5.1 5.1 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@H](C)N)c[nH]c2c1 10.1021/jm00402a026
CHEMBL1788282 63066 None 4 Rat Binding pKi = 5.1 5.1 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@H](C)N)c[nH]c2c1 10.1021/jm00402a026
44461443 205353 None 0 Human Binding pKi = 7.1 7.1 -5 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 414 5 1 3 4.8 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL79693 205353 None 0 Human Binding pKi = 7.1 7.1 -5 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 414 5 1 3 4.8 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
66847540 126213 None 0 Chinese hamster Binding pKi = 7.1 7.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 403 5 0 6 2.8 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cc(C#N)ccn4)CC3)c2o1 nan
CHEMBL3650034 126213 None 0 Chinese hamster Binding pKi = 7.1 7.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 403 5 0 6 2.8 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cc(C#N)ccn4)CC3)c2o1 nan
14975318 77243 None 0 Rat Binding pKi = 5.1 5.1 -144 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL2079596 77243 None 0 Rat Binding pKi = 5.1 5.1 -144 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL5074190 214314 None 0 Human Binding pKi = 7.1 7.1 -29 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
70530 96957 None 104 Rat Binding pKi = 7.1 7.1 -2 3
Binding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL266250 96957 None 104 Rat Binding pKi = 7.1 7.1 -2 3
Binding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
50878551 90745 None 61 Human Binding pKi = 6.1 6.1 -7 18
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 90745 None 61 Human Binding pKi = 6.1 6.1 -7 18
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
1355 2011 None 88 Rat Binding pKi = 7.1 7.1 -1 16
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
142 2011 None 88 Rat Binding pKi = 7.1 7.1 -1 16
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
CHEMBL478 2011 None 88 Rat Binding pKi = 7.1 7.1 -1 16
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
DB12110 2011 None 88 Rat Binding pKi = 7.1 7.1 -1 16
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
15724480 119579 None 0 Rat Binding pKi = 7.1 7.1 -117 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 452 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL346168 119579 None 0 Rat Binding pKi = 7.1 7.1 -117 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 452 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCCCC3=O)n2C)CC1 10.1021/jm00081a018
11111280 109198 None 0 Human Binding pKi = 6.1 6.1 -38 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 2 4 3.6 COc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL321562 109198 None 0 Human Binding pKi = 6.1 6.1 -38 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 2 4 3.6 COc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
76322958 106224 None 0 Human Binding pKi = 6.1 6.1 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
CHEMBL2260930 106224 None 0 Human Binding pKi = 6.1 6.1 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
CHEMBL3138809 106224 None 0 Human Binding pKi = 6.1 6.1 -1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
86221574 166687 None 2 Human Binding pKi = 5.1 5.1 -95 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
CHEMBL4282117 166687 None 2 Human Binding pKi = 5.1 5.1 -95 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
11145333 164595 None 0 Human Binding pKi = 7.1 7.1 -6 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL421573 164595 None 0 Human Binding pKi = 7.1 7.1 -6 4
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10513501 102619 None 0 Rat Binding pKi = 7.1 7.1 14 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1cc2ccccc2c2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
CHEMBL304210 102619 None 0 Rat Binding pKi = 7.1 7.1 14 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1cc2ccccc2c2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
44376362 164896 None 0 Human Binding pKi = 6.1 6.1 -10 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 4 2 2 3.2 C1=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CCNC1 10.1016/j.bmcl.2003.11.023
CHEMBL422192 164896 None 0 Human Binding pKi = 6.1 6.1 -10 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 4 2 2 3.2 C1=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CCNC1 10.1016/j.bmcl.2003.11.023
44286629 168148 None 0 Rat Binding pKi = 5.1 5.1 -245 3
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 437 5 0 5 5.0 CN1CCN(c2nc3ccccc3c(-c3ccccc3)c2COC(=O)c2ccccc2)CC1 10.1021/jm981112s
CHEMBL43304 168148 None 0 Rat Binding pKi = 5.1 5.1 -245 3
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 437 5 0 5 5.0 CN1CCN(c2nc3ccccc3c(-c3ccccc3)c2COC(=O)c2ccccc2)CC1 10.1021/jm981112s
9845181 208161 None 3 Human Binding pKi = 5.1 5.1 -5495 13
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 208161 None 3 Human Binding pKi = 5.1 5.1 -5495 13
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
21048816 75500 None 0 Human Binding pKi = 5.1 5.1 -1096 5
Displacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cells
ChEMBL 385 7 0 3 4.9 CC(C)(CCCN1CCCC(c2ccccc2)C1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.11.067
CHEMBL204269 75500 None 0 Human Binding pKi = 5.1 5.1 -1096 5
Displacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cells
ChEMBL 385 7 0 3 4.9 CC(C)(CCCN1CCCC(c2ccccc2)C1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.11.067
10023444 116704 None 0 Rat Binding pKi = 6.1 6.1 -117 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 392 4 0 4 4.5 c1ccc2c(c1)CCCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL337279 116704 None 0 Rat Binding pKi = 6.1 6.1 -117 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 392 4 0 4 4.5 c1ccc2c(c1)CCCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
14083210 60322 None 2 Rat Binding pKi = 6.1 6.1 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@@H](C)N)c12 10.1021/jm00402a026
CHEMBL1744072 60322 None 2 Rat Binding pKi = 6.1 6.1 - 1
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@@H](C)N)c12 10.1021/jm00402a026
44581973 175601 None 0 Human Binding pKi = 6.1 6.1 -363 10
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 175601 None 0 Human Binding pKi = 6.1 6.1 -363 10
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
71061724 145552 None 0 Mouse Binding pKi = 5.1 5.1 -7 5
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 145552 None 0 Mouse Binding pKi = 5.1 5.1 -7 5
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10356544 203991 None 0 Human Binding pKi = 6.1 6.1 -61 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 284 5 1 1 4.5 CCCN(CCC)C1CCc2ccc3[nH]cc(C)c3c2C1 10.1021/jm00012a021
CHEMBL69562 203991 None 0 Human Binding pKi = 6.1 6.1 -61 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 284 5 1 1 4.5 CCCN(CCC)C1CCc2ccc3[nH]cc(C)c3c2C1 10.1021/jm00012a021
24882193 188649 None 0 Human Binding pKi = 7.1 7.1 -263 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL503468 188649 None 0 Human Binding pKi = 7.1 7.1 -263 2
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
11270107 68246 None 0 Human Binding pKi = 7.1 7.1 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 420 7 0 6 4.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(C)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191605 68246 None 0 Human Binding pKi = 7.1 7.1 -39 3
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 420 7 0 6 4.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(C)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
44581235 177016 None 0 Human Binding pKi = 7.1 7.1 -25 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 521 8 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(S(C)(=O)=O)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL462915 177016 None 0 Human Binding pKi = 7.1 7.1 -25 3
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 521 8 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(S(C)(=O)=O)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10341516 115522 None 0 Rat Binding pKi = 6.1 6.1 -251 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 410 6 0 6 3.3 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL335297 115522 None 0 Rat Binding pKi = 6.1 6.1 -251 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 410 6 0 6 3.3 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
276 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
5312149 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
CHEMBL431298 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
6918648 101559 None 1 Human Binding pKi = 6.1 6.1 -1288 14
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 101559 None 1 Human Binding pKi = 6.1 6.1 -1288 14
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
10161027 91976 None 0 Human Binding pKi = 6.1 6.1 -39 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241499 91976 None 0 Human Binding pKi = 6.1 6.1 -39 3
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2006.11.031
276 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
5312149 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
CHEMBL431298 3513 None 50 Human Binding pKi = 6.1 6.1 -537 13
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
6918648 101559 None 1 Human Binding pKi = 6.1 6.1 -1288 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 101559 None 1 Human Binding pKi = 6.1 6.1 -1288 14
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
19066205 11382 None 0 Human Binding pKi = 8.1 8.1 8 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
CHEMBL108722 11382 None 0 Human Binding pKi = 8.1 8.1 8 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
CHEMBL1179986 11382 None 0 Human Binding pKi = 8.1 8.1 8 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
2543 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358.0 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
54 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL128 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB00669 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
2736460 207536 None 57 Rat Binding pKi = 8.1 8.1 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 190 2 1 2 1.7 CCc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9467 207536 None 57 Rat Binding pKi = 8.1 8.1 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 190 2 1 2 1.7 CCc1ccccc1N1CCNCC1 10.1021/jm00125a020
59636734 126223 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cc(F)cc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650043 126223 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cc(F)cc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
19066200 11381 None 0 Human Binding pKi = 8.1 8.1 27 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
CHEMBL108645 11381 None 0 Human Binding pKi = 8.1 8.1 27 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
CHEMBL1179985 11381 None 0 Human Binding pKi = 8.1 8.1 27 3
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
14479835 208327 None 1 Rat Binding pKi = 8.1 8.1 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 218 4 1 2 2.4 CCCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9921 208327 None 1 Rat Binding pKi = 8.1 8.1 2 3
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 218 4 1 2 2.4 CCCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
2176 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
4828 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
4828.0 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
91 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
CHEMBL500 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
DB00960 3127 None 68 Rat Binding pKi = 7.1 7.1 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
10904295 4709 None 0 Human Binding pKi = 7.1 7.1 -6 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1021/jm030020m
CHEMBL103503 4709 None 0 Human Binding pKi = 7.1 7.1 -6 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1021/jm030020m
52899 97254 None 34 Rat Binding pKi = 6.1 6.1 -8 5
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm00164a046
CHEMBL268800 97254 None 34 Rat Binding pKi = 6.1 6.1 -8 5
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm00164a046
10220230 107422 None 2 Human Binding pKi = 6.1 6.1 -7 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 2 3 2.0 CN1CCC(c2c[nH]c3ccc(N)nc23)CC1 10.1021/jm030020m
CHEMBL318105 107422 None 2 Human Binding pKi = 6.1 6.1 -7 3
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 2 3 2.0 CN1CCC(c2c[nH]c3ccc(N)nc23)CC1 10.1021/jm030020m
14975320 77245 None 0 Rat Binding pKi = 6.1 6.1 -478 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL2079598 77245 None 0 Rat Binding pKi = 6.1 6.1 -478 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
2914436 162390 None 3 Rat Binding pKi = 5.1 5.1 -10 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 301 9 1 3 3.7 CCCN(CCC)CC(O)COc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL416564 162390 None 3 Rat Binding pKi = 5.1 5.1 -10 2
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 301 9 1 3 3.7 CCCN(CCC)CC(O)COc1cccc2ccccc12 10.1021/jm00124a021
11723305 169265 None 0 Human Binding pKi = 7.1 7.1 -162 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL441256 169265 None 0 Human Binding pKi = 7.1 7.1 -162 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
44376263 56233 None 0 Human Binding pKi = 7.1 7.1 -13 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 6 2 3 4.9 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162724 56233 None 0 Human Binding pKi = 7.1 7.1 -13 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 6 2 3 4.9 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
59636752 125682 None 0 Chinese hamster Binding pKi = 7.1 7.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 475 6 1 6 2.9 CC(=O)N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
CHEMBL3647264 125682 None 0 Chinese hamster Binding pKi = 7.1 7.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 475 6 1 6 2.9 CC(=O)N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
49783209 17609 None 0 Human Binding pKi = 6.1 6.1 -407 26
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 17609 None 0 Human Binding pKi = 6.1 6.1 -407 26
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
11067619 5135 None 0 Human Binding pKi = 6.1 6.1 -112 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 334 3 2 3 3.6 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccc4)nc23)CC1 10.1021/jm030020m
CHEMBL105743 5135 None 0 Human Binding pKi = 6.1 6.1 -112 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 334 3 2 3 3.6 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccc4)nc23)CC1 10.1021/jm030020m
151 2416 None 44 Human Binding pKi = 7.1 7.1 -89 4
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
20 2416 None 44 Human Binding pKi = 7.1 7.1 -89 4
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
5311258 2416 None 44 Human Binding pKi = 7.1 7.1 -89 4
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
CHEMBL101690 2416 None 44 Human Binding pKi = 7.1 7.1 -89 4
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
134138168 147691 None 0 Human Binding pKi = 6.1 6.1 -75 10
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 147691 None 0 Human Binding pKi = 6.1 6.1 -75 10
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
213 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533.0 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 3853 None 55 Rat Binding pKi = 6.1 6.1 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
76326516 106229 None 0 Human Binding pKi = 6.1 6.1 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL2260933 106229 None 0 Human Binding pKi = 6.1 6.1 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL3138820 106229 None 0 Human Binding pKi = 6.1 6.1 1 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL5091373 215567 None 0 Human Binding pKi = 7.1 7.1 -39 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 215567 None 0 Human Binding pKi = 7.1 7.1 -39 9
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
122483223 138109 None 0 Human Binding pKi = 6.1 6.1 -11 7
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3764650 138109 None 0 Human Binding pKi = 6.1 6.1 -11 7
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765874 138109 None 0 Human Binding pKi = 6.1 6.1 -11 7
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
44269068 98454 None 0 Rat Binding pKi = 6.1 6.1 -954 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 0 5 2.9 COc1cccc2c1C1CCN(CCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
CHEMBL275773 98454 None 0 Rat Binding pKi = 6.1 6.1 -954 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 0 5 2.9 COc1cccc2c1C1CCN(CCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
2351 3286 None 64 Rat Binding pKi = 6.1 6.1 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 3286 None 64 Rat Binding pKi = 6.1 6.1 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 3286 None 64 Rat Binding pKi = 6.1 6.1 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 3286 None 64 Rat Binding pKi = 6.1 6.1 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 3286 None 64 Rat Binding pKi = 6.1 6.1 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
152 364 None 29 Rat Binding pKi = 7.1 7.1 -57 18
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
2107 364 None 29 Rat Binding pKi = 7.1 7.1 -57 18
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
CHEMBL275854 364 None 29 Rat Binding pKi = 7.1 7.1 -57 18
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
9910257 166672 None 0 Rat Binding pKi = 7.1 7.1 -87 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 424 7 0 5 3.6 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL428175 166672 None 0 Rat Binding pKi = 7.1 7.1 -87 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 424 7 0 5 3.6 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
9997422 204276 None 0 Human Binding pKi = 6.1 6.1 -50 4
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
CHEMBL71247 204276 None 0 Human Binding pKi = 6.1 6.1 -50 4
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
41305446 167252 None 1 Human Binding pKi = 5.1 5.1 -15 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292719 167252 None 1 Human Binding pKi = 5.1 5.1 -15 5
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
1212 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372.0 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 1662 None 50 Rat Binding pKi = 6.1 6.1 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
122197405 133476 None 0 Human Binding pKi = 7.1 7.1 -47 3
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL3706925 133476 None 0 Human Binding pKi = 7.1 7.1 -47 3
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
11223004 202214 None 0 Human Binding pKi = 7.1 7.1 -28 5
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 202214 None 0 Human Binding pKi = 7.1 7.1 -28 5
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
130442480 175270 None 0 Human Binding pKi = 5.1 5.1 -107 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 175270 None 0 Human Binding pKi = 5.1 5.1 -107 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
44582675 189701 None 0 Human Binding pKi = 6.1 6.1 -15 15
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 189701 None 0 Human Binding pKi = 6.1 6.1 -15 15
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
9907305 30194 None 0 Rat Binding pKi = 6.1 6.1 -1513 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 368 5 1 3 3.2 COc1cccc2c1C1CCN(CCNC(=O)c3ccc(F)cc3)CC1C2 10.1021/jm00027a013
CHEMBL13904 30194 None 0 Rat Binding pKi = 6.1 6.1 -1513 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 368 5 1 3 3.2 COc1cccc2c1C1CCN(CCNC(=O)c3ccc(F)cc3)CC1C2 10.1021/jm00027a013
90469115 185842 None 4 Human Binding pKi = 6.1 6.1 -295 17
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 185842 None 4 Human Binding pKi = 6.1 6.1 -295 17
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
64622 96854 None 6 Rat Binding pKi = 6.1 6.1 -2238 5
Binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 425 8 1 4 3.9 COc1ccccc1N1CCN(CCCCNC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm00112a043
CHEMBL26533 96854 None 6 Rat Binding pKi = 6.1 6.1 -2238 5
Binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 425 8 1 4 3.9 COc1ccccc1N1CCN(CCCCNC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm00112a043
127036932 137348 None 0 Human Binding pKi = 6.1 6.1 -29 22
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 137348 None 0 Human Binding pKi = 6.1 6.1 -29 22
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
59636704 125683 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 1 6 4.1 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccccn1 nan
CHEMBL3647265 125683 None 0 Chinese hamster Binding pKi = 8.1 8.1 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 1 6 4.1 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccccn1 nan
2543 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
5358 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
5358.0 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
54 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
CHEMBL128 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
DB00669 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
59636741 125698 None 0 Chinese hamster Binding pKi = 8.0 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647280 125698 None 0 Chinese hamster Binding pKi = 8.0 8.0 - 1
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
150 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
1764 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
8226.0 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
CHEMBL1201356 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
DB00353 2509 None 21 Rat Binding pKi = 8.0 8.0 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
46232642 200834 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
CHEMBL601012 200834 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
23533306 85181 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 465 4 2 6 2.5 CN1CCN(c2cc(F)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)CC1 10.1016/j.bmc.2006.10.037
CHEMBL225363 85181 None 0 Human Binding pKi = 8.0 8.0 - 1
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 465 4 2 6 2.5 CN1CCN(c2cc(F)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)CC1 10.1016/j.bmc.2006.10.037
71459954 79182 None 0 Human Binding pKi = 8.0 8.0 -9 7
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 79182 None 0 Human Binding pKi = 8.0 8.0 -9 7
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
46232642 200834 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
CHEMBL601012 200834 None 0 Human Binding pKi = 8.0 8.0 - 1
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
2543 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
5358 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
5358.0 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
54 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
CHEMBL128 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
DB00669 3707 None 68 Human Binding pKi = 8.0 8.0 -3 32
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 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/jm9805945
44403106 71415 None 0 Human Binding pKi = 8.0 8.0 1 4
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 438 6 1 6 3.3 COc1ccccc1N1CCC(C(=O)Nc2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL195927 71415 None 0 Human Binding pKi = 8.0 8.0 1 4
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 438 6 1 6 3.3 COc1ccccc1N1CCC(C(=O)Nc2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.bmcl.2005.07.024
44383737 132521 None 0 Human Binding pKi = 8 8.0 -5 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 340 6 1 3 4.6 COC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL369798 132521 None 0 Human Binding pKi = 8 8.0 -5 2
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 340 6 1 3 4.6 COC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
145 140 None 49 Rat Binding pKi = 7.1 7.1 -47 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
1832 140 None 49 Rat Binding pKi = 7.1 7.1 -47 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
CHEMBL7257 140 None 49 Rat Binding pKi = 7.1 7.1 -47 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
DB14010 140 None 49 Rat Binding pKi = 7.1 7.1 -47 30
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
14519863 115201 None 1 Rat Binding pKi = 5.1 5.1 -58 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL334465 115201 None 1 Rat Binding pKi = 5.1 5.1 -58 3
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm00124a021
10197933 97033 None 39 Rat Binding pKi = 6.0 6.0 -7 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 177 1 1 2 1.5 COc1cccc2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
CHEMBL26688 97033 None 39 Rat Binding pKi = 6.0 6.0 -7 2
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 177 1 1 2 1.5 COc1cccc2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
44431533 88026 None 0 Human Binding pKi = 7.0 7.0 -1 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL234448 88026 None 0 Human Binding pKi = 7.0 7.0 -1 4
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
10257 738 None 31 Rat Binding pKi = 6.0 6.0 -141 19
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
144 738 None 31 Rat Binding pKi = 6.0 6.0 -141 19
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
CHEMBL416526 738 None 31 Rat Binding pKi = 6.0 6.0 -141 19
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
DB01445 738 None 31 Rat Binding pKi = 6.0 6.0 -141 19
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
11747350 107332 None 0 Human Binding pKi = 6.0 6.0 -45 10
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 107332 None 0 Human Binding pKi = 6.0 6.0 -45 10
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
76312090 106249 None 0 Human Binding pKi = 6.0 6.0 6 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL2260934 106249 None 0 Human Binding pKi = 6.0 6.0 6 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL3138934 106249 None 0 Human Binding pKi = 6.0 6.0 6 2
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
9996017 21246 None 0 Rat Binding pKi = 6.0 6.0 -114 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 318 3 0 3 3.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
CHEMBL131324 21246 None 0 Rat Binding pKi = 6.0 6.0 -114 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 318 3 0 3 3.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
6918542 204924 None 24 Human Binding pKi = 5.0 5.0 -2238 10
Compound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptorCompound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
CHEMBL76237 204924 None 24 Human Binding pKi = 5.0 5.0 -2238 10
Compound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptorCompound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
11120893 4522 None 0 Human Binding pKi = 6.0 6.0 -204 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccoc4)nc23)CC1 10.1021/jm030020m
CHEMBL102250 4522 None 0 Human Binding pKi = 6.0 6.0 -204 4
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccoc4)nc23)CC1 10.1021/jm030020m
75201901 166425 None 19 Human Binding pKi = 5.0 5.0 -691 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 166425 None 19 Human Binding pKi = 5.0 5.0 -691 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 171908 None 0 Human Binding pKi = 5.0 5.0 -199 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 171908 None 0 Human Binding pKi = 5.0 5.0 -199 24
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10361292 116656 None 0 Rat Binding pKi = 6.0 6.0 -1737 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)Cc2ccccc21 10.1021/jm00020a020
CHEMBL337036 116656 None 0 Rat Binding pKi = 6.0 6.0 -1737 2
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)Cc2ccccc21 10.1021/jm00020a020
4189 206922 None 96 Rat Binding pKi = 5.0 5.0 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 206922 None 96 Rat Binding pKi = 5.0 5.0 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 206922 None 96 Rat Binding pKi = 5.0 5.0 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9948210 103121 None 1 Human Binding pKi = 6.0 6.0 -1479 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL307786 103121 None 1 Human Binding pKi = 6.0 6.0 -1479 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL4777443 214046 None 0 Human Binding pKi = 6.0 6.0 -45 14
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR1BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR1B
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 10.6019/CHEMBL5212743
10401862 102671 None 1 Human Binding pKi = 6.0 6.0 -257 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL304573 102671 None 1 Human Binding pKi = 6.0 6.0 -257 5
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
44376363 55352 None 0 Human Binding pKi = 7.0 7.0 -6 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
CHEMBL161894 55352 None 0 Human Binding pKi = 7.0 7.0 -6 2
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
15724503 46197 None 0 Rat Binding pKi = 7.0 7.0 -2 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 400 5 0 4 3.5 Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)ccc1CN1CCCCC1=O 10.1021/jm00081a018
CHEMBL153451 46197 None 0 Rat Binding pKi = 7.0 7.0 -2 3
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 400 5 0 4 3.5 Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)ccc1CN1CCCCC1=O 10.1021/jm00081a018
127036953 137515 None 0 Human Binding pKi = 6.0 6.0 -95 22
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 137515 None 0 Human Binding pKi = 6.0 6.0 -95 22
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
71452384 83797 None 0 Human Binding pKi = 6.0 6.0 -4 5
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 83797 None 0 Human Binding pKi = 6.0 6.0 -4 5
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 83797 None 0 Human Binding pKi = 6.0 6.0 -4 5
Inhibition of 5-HT1B receptor (unknown origin) by PDSP assayInhibition of 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 83797 None 0 Human Binding pKi = 6.0 6.0 -4 5
Inhibition of 5-HT1B receptor (unknown origin) by PDSP assayInhibition of 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
135398737 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
135398737.0 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 958 None 93 Rat Binding pKi = 6.0 6.0 -691 89
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44461248 205359 None 0 Human Binding pKi = 7.0 7.0 -3 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 407 5 2 3 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)C1 10.1016/j.bmcl.2004.03.003
CHEMBL79725 205359 None 0 Human Binding pKi = 7.0 7.0 -3 3
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 407 5 2 3 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)C1 10.1016/j.bmcl.2004.03.003
14975317 77235 None 0 Rat Binding pKi = 4.0 4.0 -138 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
CHEMBL2079546 77235 None 0 Rat Binding pKi = 4.0 4.0 -138 2
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
118464425 138309 None 0 Human Binding pKi = 5.0 5.0 -257 9
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 138309 None 0 Human Binding pKi = 5.0 5.0 -257 9
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
146025727 171685 None 0 Human Binding pKi = 5 5.0 -371 27
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 171685 None 0 Human Binding pKi = 5 5.0 -371 27
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10383010 163499 None 0 Human Binding pKi = 6 6.0 -371 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 346 6 1 2 4.8 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL420191 163499 None 0 Human Binding pKi = 6 6.0 -371 5
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 346 6 1 2 4.8 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
1524 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 None 96 Human Binding pIC50 = 8.3 8.3 -2511 52
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.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
135398737 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 None 93 Rat Binding pIC50 = 8.3 8.3 -691 89
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
123606 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
123606.0 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
128 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
7110 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
CHEMBL1505 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
DB00918 352 None 70 Human Binding pIC50 = 7.9 7.9 -1 3
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
40 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
77993 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
77993.0 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
995 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
CHEMBL1510 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
DB00216 1547 None 58 Human Binding pKd = 8.1 8.1 -2 5
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
5 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
5202 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5202 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
CHEMBL39 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
CHEMBL39 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
DB08839 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
DB08839 139 None 72 Human Binding pKd = 8.0 8.0 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
117 353 None 19 Human Binding pKd = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
120 353 None 19 Human Binding pKd = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
66004 353 None 19 Human Binding pKd = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
CHEMBL88240 353 None 19 Human Binding pKd = 8.8 8.8 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
1220 187 None 55 Human Binding pKd = 8.9 8.9 -208 44
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
31 187 None 55 Human Binding pKd = 8.9 8.9 -208 44
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
7 187 None 55 Human Binding pKd = 8.9 8.9 -208 44
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
CHEMBL56 187 None 55 Human Binding pKd = 8.9 8.9 -208 44
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
None 215938 3H-5HT 0 Human Binding pKi = 11.2 11.2 -3 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215938 3H-5HT 0 Human Binding pKi = 11.2 11.2 -3 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215938 3H-5HT 0 Rat Binding pKi = 10.7 10.7 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
11954224 215953 3H-5HT 0 Rat Binding pKi = 10.5 10.5 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 3H-5HT 0 Rat Binding pKi = 10.5 10.5 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 3H-5HT 0 Rat Binding pKi = 10.5 10.5 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 3H-5HT 0 Rat Binding pKi = 10.5 10.5 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
71299720 215951 3H-5HT 0 Human Binding pKi = 10.4 10.4 1 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
11797998 35692 UNDEFINED 0 Human Binding pKi = 10 10.0 1 3
NoneNone
PDSP KiDatabase 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 None
CHEMBL144030 35692 UNDEFINED 0 Human Binding pKi = 10 10.0 1 3
NoneNone
PDSP KiDatabase 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 None
24881753 137202 UNDEFINED 0 Human Binding pKi = 10 10.0 14 2
NoneNone
PDSP KiDatabase 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL374973 137202 UNDEFINED 0 Human Binding pKi = 10 10.0 14 2
NoneNone
PDSP KiDatabase 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
1809 134 3H-5HT 32 Human Binding pKi = 9.9 9.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 9.9 9.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 9.9 9.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107780 1844 3H-5HT 54 Human Binding pKi = 9.9 9.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-5HT 54 Human Binding pKi = 9.9 9.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-5HT 54 Human Binding pKi = 9.9 9.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1809 134 3H-5HT 32 Human Binding pKi = 9.8 9.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 9.8 9.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 9.8 9.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4106 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Human Binding pKi = 9.7 9.7 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1809 134 3H-5HT 32 Human Binding pKi = 9.6 9.6 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 9.6 9.6 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 9.6 9.6 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
132 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
124 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 3H-5HT 47 Human Binding pKi = 9.6 9.6 1 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
132 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-5HT 13 Rat Binding pKi = 9.6 9.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
11954224 215953 3H-GR125743 0 Human Binding pKi = 9.5 9.5 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 3H-GR125743 0 Human Binding pKi = 9.5 9.5 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 3H-GR125743 0 Human Binding pKi = 9.5 9.5 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 3H-GR125743 0 Human Binding pKi = 9.5 9.5 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 215946 3H-GR-125743 0 Rat Binding pKi = 9.5 9.5 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
1809 134 3H-GR-125743 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-GR-125743 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-GR-125743 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 3H-5HT 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Rat Binding pKi = 9.5 9.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 215946 3H-5HT 0 Rat Binding pKi = 9.4 9.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 215946 3H-5HT 0 Rat Binding pKi = 9.4 9.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
152662 215957 3H-5HT 0 Rat Binding pKi = 9.4 9.4 109 7
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
107780 1844 3H-GR-125743 54 Human Binding pKi = 9.4 9.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-GR-125743 54 Human Binding pKi = 9.4 9.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-GR-125743 54 Human Binding pKi = 9.4 9.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
152662 215957 125I-CYP 0 Rat Binding pKi = 9.3 9.3 109 7
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
24881204 188422 UNDEFINED 0 Human Binding pKi = 9.3 9.3 3 2
NoneNone
PDSP KiDatabase 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL502138 188422 UNDEFINED 0 Human Binding pKi = 9.3 9.3 3 2
NoneNone
PDSP KiDatabase 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
None 215938 3H-5HT 0 Human Binding pKi = 9.3 9.3 -3 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
5 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 9.2 9.2 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
24881754 188292 UNDEFINED 0 Human Binding pKi = 9.2 9.2 3 2
NoneNone
PDSP KiDatabase 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL500284 188292 UNDEFINED 0 Human Binding pKi = 9.2 9.2 3 2
NoneNone
PDSP KiDatabase 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
5 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 9.2 9.2 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
12312583 216017 3H-5HT 0 Human Binding pKi = 9.2 9.2 1 3
NoneNone
PDSP KiDatabase 254 1 2 2 2.0 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)CO None
9832057 52315 UNDEFINED 0 Human Binding pKi = 9.2 9.2 1 3
NoneNone
PDSP KiDatabase 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 None
CHEMBL158941 52315 UNDEFINED 0 Human Binding pKi = 9.2 9.2 1 3
NoneNone
PDSP KiDatabase 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 None
1809 134 3H-5HT 32 Human Binding pKi = 9.2 9.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 9.2 9.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 9.2 9.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 215938 125I-CYP 0 Rat Binding pKi = 9.1 9.1 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
107 141 3H-5HT 121 Human Binding pKi = 9.1 9.1 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Human Binding pKi = 9.1 9.1 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Human Binding pKi = 9.1 9.1 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
44279525 105512 UNDEFINED 0 Human Binding pKi = 9.1 9.1 -1 3
NoneNone
PDSP KiDatabase 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 None
CHEMBL31217 105512 UNDEFINED 0 Human Binding pKi = 9.1 9.1 -1 3
NoneNone
PDSP KiDatabase 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 None
24881689 170132 UNDEFINED 0 Human Binding pKi = 9.1 9.1 1 2
NoneNone
PDSP KiDatabase 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL444404 170132 UNDEFINED 0 Human Binding pKi = 9.1 9.1 1 2
NoneNone
PDSP KiDatabase 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
1809 134 3H-GR-125743 32 Guinea pig Binding pKi = 9.1 9.1 -8 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-GR-125743 32 Guinea pig Binding pKi = 9.1 9.1 -8 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-GR-125743 32 Guinea pig Binding pKi = 9.1 9.1 -8 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
24881203 173231 UNDEFINED 0 Human Binding pKi = 9.1 9.1 1 2
NoneNone
PDSP KiDatabase 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL452387 173231 UNDEFINED 0 Human Binding pKi = 9.1 9.1 1 2
NoneNone
PDSP KiDatabase 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
124 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
24881264 188307 UNDEFINED 0 Human Binding pKi = 9.1 9.1 13 2
NoneNone
PDSP KiDatabase 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL500488 188307 UNDEFINED 0 Human Binding pKi = 9.1 9.1 13 2
NoneNone
PDSP KiDatabase 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
124 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 3H-5HT 47 Rat Binding pKi = 9.1 9.1 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
5 139 3H-GR-125743 72 Rat Binding pKi = 9.1 9.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-GR-125743 72 Rat Binding pKi = 9.1 9.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-GR-125743 72 Rat Binding pKi = 9.1 9.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-GR-125743 72 Rat Binding pKi = 9.1 9.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1809 134 3H-5HT 32 Human Binding pKi = 9.1 9.1 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 9.1 9.1 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 9.1 9.1 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
133 2496 3H-5HT 52 Rat Binding pKi = 9.1 9.1 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-5HT 52 Rat Binding pKi = 9.1 9.1 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-5HT 52 Rat Binding pKi = 9.1 9.1 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-5HT 52 Rat Binding pKi = 9.1 9.1 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-5HT 52 Rat Binding pKi = 9.1 9.1 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
None 215946 3H-5HT 0 Rat Binding pKi = 9.0 9.0 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
107780 1844 35S-GTPGammaS 54 Human Binding pKi = 9.0 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 35S-GTPGammaS 54 Human Binding pKi = 9.0 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 35S-GTPGammaS 54 Human Binding pKi = 9.0 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2865 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-Alniditan 73 Human Binding pKi = 9 9.0 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
107780 1844 35S-GTPGammaS 54 Human Binding pKi = 9 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 35S-GTPGammaS 54 Human Binding pKi = 9 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 35S-GTPGammaS 54 Human Binding pKi = 9 9.0 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
28 3496 35S-GTPGammaS 46 Human Binding pKi = 9 9.0 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3496 35S-GTPGammaS 46 Human Binding pKi = 9 9.0 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3496 35S-GTPGammaS 46 Human Binding pKi = 9 9.0 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
None 215946 125I-ICYP 0 Rat Binding pKi = 9 9.0 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
132 1275 3H-GR-125743 13 Rat Binding pKi = 9.0 9.0 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-GR-125743 13 Rat Binding pKi = 9.0 9.0 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-GR-125743 13 Rat Binding pKi = 9.0 9.0 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
5 139 3H-5HT 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 UNDEFINED 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 UNDEFINED 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 UNDEFINED 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 UNDEFINED 72 Human Binding pKi = 9.0 9.0 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2543 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-Alniditan 68 Human Binding pKi = 8.9 8.9 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
12312583 216017 3H-5HT 0 Human Binding pKi = 8.9 8.9 1 3
NoneNone
PDSP KiDatabase 254 1 2 2 2.0 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)CO None
107780 1844 3H-5HT 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-5HT 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-5HT 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107780 1844 3H-GR-125743 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-GR-125743 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-GR-125743 54 Human Binding pKi = 8.9 8.9 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
24881752 171759 UNDEFINED 0 Human Binding pKi = 8.9 8.9 -1 2
NoneNone
PDSP KiDatabase 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL446745 171759 UNDEFINED 0 Human Binding pKi = 8.9 8.9 -1 2
NoneNone
PDSP KiDatabase 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
24881202 172586 UNDEFINED 0 Human Binding pKi = 8.9 8.9 -1 2
NoneNone
PDSP KiDatabase 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL448902 172586 UNDEFINED 0 Human Binding pKi = 8.9 8.9 -1 2
NoneNone
PDSP KiDatabase 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
None 215938 3H-GR-125743 0 Guinea pig Binding pKi = 8.8 8.8 -25 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 134 3H-5HT 32 Human Binding pKi = 8.8 8.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 8.8 8.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 8.8 8.8 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 215946 125I-ICYP 0 Rat Binding pKi = 8.8 8.8 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
107 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Rat Binding pKi = 8.8 8.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
132 1275 125I-CYP 13 Rat Binding pKi = 8.7 8.7 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 125I-CYP 13 Rat Binding pKi = 8.7 8.7 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 125I-CYP 13 Rat Binding pKi = 8.7 8.7 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2543 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1809 134 3H-5HT 32 Mouse Binding pKi = 8 8.0 -97 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Mouse Binding pKi = 8 8.0 -97 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Mouse Binding pKi = 8 8.0 -97 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 215946 3H-5HT 0 Mouse Binding pKi = 8 8.0 -7 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
71299720 215951 3H-5HT 0 Human Binding pKi = 8 8.0 1 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
11954224 215953 None 0 Rat Binding pKi = 8 8.0 -12 58
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 None 0 Rat Binding pKi = 8 8.0 -12 58
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 None 0 Rat Binding pKi = 8 8.0 -12 58
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 None 0 Rat Binding pKi = 8 8.0 -12 58
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1342 35 3H-5HT 49 Human Binding pKi = 8 8.0 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 3H-5HT 49 Human Binding pKi = 8 8.0 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 3H-5HT 49 Human Binding pKi = 8 8.0 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
4106 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 216343 3H-GR-125743 0 Guinea pig Binding pKi = 8.0 8.0 1 2
NoneNone
PDSP KiDatabase 228 2 1 3 2.6 C1CNCCC1SC2=NC(=CC=C2)Cl None
4106 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Rat Binding pKi = 8.0 8.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 216483 125I-ICYP 0 Rat Binding pKi = 8.0 8.0 -58 3
NoneNone
PDSP KiDatabase None None None None None
4106 2502 3H-GR-125743 22 Guinea pig Binding pKi = 8.0 8.0 -27 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-GR-125743 22 Guinea pig Binding pKi = 8.0 8.0 -27 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-GR-125743 22 Guinea pig Binding pKi = 8.0 8.0 -27 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-GR-125743 22 Guinea pig Binding pKi = 8.0 8.0 -27 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2543 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
137 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 370 3H-5HT 52 Rat Binding pKi = 7 7.0 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
4106 2502 3H-GR-125743 22 Rat Binding pKi = 7 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-GR-125743 22 Rat Binding pKi = 7 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-GR-125743 22 Rat Binding pKi = 7 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-GR-125743 22 Rat Binding pKi = 7 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
24881617 188326 UNDEFINED 0 Human Binding pKi = 7 7.0 -165 2
NoneNone
PDSP KiDatabase 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500737 188326 UNDEFINED 0 Human Binding pKi = 7 7.0 -165 2
NoneNone
PDSP KiDatabase 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
152 364 125I-CYP 29 Rat Binding pKi = 6 6.0 -57 18
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 364 125I-CYP 29 Rat Binding pKi = 6 6.0 -57 18
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 364 125I-CYP 29 Rat Binding pKi = 6 6.0 -57 18
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
41 1659 3H-5CT 0 Guinea pig Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
41 1659 3H-GR-125743 0 Human Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 1659 3H-5CT 0 Guinea pig Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 1659 3H-GR-125743 0 Human Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 1659 3H-5CT 0 Guinea pig Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 1659 3H-GR-125743 0 Human Binding pKi = 6 6.0 -794 17
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
173 3262 3H-5HT 95 Human Binding pKi = 6 6.0 -11 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Human Binding pKi = 6 6.0 -11 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Human Binding pKi = 6 6.0 -11 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2605 3783 3H-GR-125743 30 Guinea pig Binding pKi = 6 6.0 -218 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 3783 3H-GR-125743 30 Guinea pig Binding pKi = 6 6.0 -218 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 3783 3H-GR-125743 30 Guinea pig Binding pKi = 6 6.0 -218 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 3783 3H-GR-125743 30 Guinea pig Binding pKi = 6 6.0 -218 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 3783 3H-GR-125743 30 Guinea pig Binding pKi = 6 6.0 -218 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
18922713 98498 3H-5HT 0 Rat Binding pKi = 6 6.0 -12882 9
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 98498 3H-5HT 0 Rat Binding pKi = 6 6.0 -12882 9
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
24840389 115213 3H-GR-125743 4 Human Binding pKi = 6 6.0 -741 16
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 115213 3H-GR-125743 4 Human Binding pKi = 6 6.0 -741 16
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
12016890 190776 3H-CYANOPINDOLOL 6 Rat Binding pKi = 6 6.0 -1698 11
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 190776 3H-CYANOPINDOLOL 6 Rat Binding pKi = 6 6.0 -1698 11
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
54841 203127 3H-5HT 52 Human Binding pKi = 6 6.0 1 27
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 203127 3H-5HT 52 Human Binding pKi = 6 6.0 1 27
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 216379 UNDEFINED 0 Human Binding pKi = 6 6.0 -1122 11
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
None 217236 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 768 9 4 4 9.4 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC(C(F)(F)F)N5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
None 217237 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 507 13 3 3 6.9 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CCCCCCCCCC(=O)O None
None 217238 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 422 7 2 3 4.7 CN(C)CCCN1CCC(CC1)C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F None
None 217239 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 448 6 2 3 5.2 C1CCN(CC1)CCN2CCC(CC2)C3=CNC4=C3C=C(C=C4)NC(=O)C5=CC=C(C=C5)F None
None 217240 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 381 5 3 3 3.7 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CCO None
None 217241 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 427 5 2 2 5.9 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC5=CC=CC=C5 None
None 217242 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 449 10 2 2 7.1 CCCCCCCCN1CCC(CC1)C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F None
None 217243 UNDEFINED 0 Human Binding pKi = 6 6.0 1 2
NoneNone
PDSP KiDatabase 743 10 5 5 7.3 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC(C(=O)N)N5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
3075702 217332 125I-CYP 0 Human Binding pKi = 6 6.0 -2 37
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1574 81 125I-CYP 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1574 81 3H-5HT 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 125I-CYP 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 3H-5HT 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 125I-CYP 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 3H-5HT 60 Rat Binding pKi = 5 5.0 -24 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1192 147 3H-5HT 47 Rat Binding pKi = 5 5.0 -162 17
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 147 3H-5HT 47 Rat Binding pKi = 5 5.0 -162 17
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 147 3H-5HT 47 Rat Binding pKi = 5 5.0 -162 17
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1220 187 125I-CYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 187 125I-ICYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 187 3H-5HT 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 125I-CYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 125I-ICYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 125I-CYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 125I-ICYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 125I-CYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 125I-ICYP 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Rat Binding pKi = 5 5.0 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
179 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159.0 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 3H-5HT 115 Rat Binding pKi = 5 5.0 -4365 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
242 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 3H-5CT 124 Human Binding pKi = 5 5.0 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2249 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249.0 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249.0 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249.0 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 512 125I-CYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 512 125I-ICYP 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 512 3H-5HT 111 Rat Binding pKi = 5 5.0 -295 12
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2369 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2369 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2369.0 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2369.0 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 622 125I-ICYP 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 622 3H-5HT 80 Rat Binding pKi = 5 5.0 -3235 8
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2477 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477.0 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477.0 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477.0 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 125I-CYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 125I-ICYP 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 3H-5HT 59 Rat Binding pKi = 5 5.0 -16 29
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2398 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801.0 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 954 3H-GR-125743 62 Human Binding pKi = 5 5.0 -1230 29
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2803 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
2803.0 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 955 125I-ICYP 58 Rat Binding pKi = 5 5.0 -602 19
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
141 1427 3H-5-CT 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 3H-5-CT 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 3H-5-CT 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 3H-5-CT 35 Human Binding pKi = 5 5.0 -114 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
681 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
681.0 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 1465 125I-CYP 72 Rat Binding pKi = 5 5.0 -1995 39
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-5HT 93 Rat Binding pKi = 5 5.0 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1204 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774.0 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 1932 3H-5HT 119 Rat Binding pKi = 5 5.0 -1949 24
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
12575 1988 125I-CYP 30 Rat Binding pKi = 5 5.0 -6606 17
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 1988 125I-CYP 30 Rat Binding pKi = 5 5.0 -6606 17
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459.0 1988 125I-CYP 30 Rat Binding pKi = 5 5.0 -6606 17
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 1988 125I-CYP 30 Rat Binding pKi = 5 5.0 -6606 17
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 1988 125I-CYP 30 Rat Binding pKi = 5 5.0 -6606 17
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
42 2063 3H-5HT 57 Bovine Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 2063 125I-CYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 2063 125I-ICYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 2063 3H-5HT 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 2063 3H-5HT 57 Bovine Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 2063 125I-CYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 2063 125I-ICYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 2063 3H-5HT 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 2063 3H-5HT 57 Bovine Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 2063 125I-CYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 2063 125I-ICYP 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 2063 3H-5HT 57 Rat Binding pKi = 5 5.0 -1778 18
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 3H-GR-125743 96 Guinea pig Binding pKi = 5 5.0 -7585 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 125I-ICYP 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 3H-5HT 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 3H-GR-125743 96 Rat Binding pKi = 5 5.0 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1531 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869.0 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2266 125I-CYP 69 Rat Binding pKi = 5 5.0 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
206 2493 125I-CYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2493 125I-ICYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 2493 3H-5HT 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 125I-CYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 125I-ICYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 3H-5HT 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 125I-CYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 125I-ICYP 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 3H-5HT 16 Rat Binding pKi = 5 5.0 -7585 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1786 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
1786 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171.0 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171.0 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2520 3H-5-CT 85 Human Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 2520 125I-ICYP 85 Rat Binding pKi = 5 5.0 -524 11
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
135 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 3H-5HT 43 Rat Binding pKi = 5 5.0 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
484 2858 125I-ICYP 51 Rat Binding pKi = 5 5.0 -24 35
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 2858 125I-ICYP 51 Rat Binding pKi = 5 5.0 -24 35
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 2858 125I-ICYP 51 Rat Binding pKi = 5 5.0 -24 35
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
283 3130 3H-5HT 57 Rat Binding pKi = 5 5.0 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3130 3H-5HT 57 Rat Binding pKi = 5 5.0 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3130 3H-5HT 57 Rat Binding pKi = 5 5.0 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
2202 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850.0 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 3132 3H-GR-125743 96 Human Binding pKi = 5 5.0 -316 21
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
2220 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400.0 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3134 125I-ICYP 82 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
3486 3157 125I-ICYP 56 Rat Binding pKi = 5 5.0 -204 11
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 3157 125I-ICYP 56 Rat Binding pKi = 5 5.0 -204 11
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 3157 125I-ICYP 56 Rat Binding pKi = 5 5.0 -204 11
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 3157 125I-ICYP 56 Rat Binding pKi = 5 5.0 -204 11
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 3157 125I-ICYP 56 Rat Binding pKi = 5 5.0 -204 11
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
2303 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 3H-5HT 68 Human Binding pKi = 5 5.0 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
243 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762.0 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 3202 3H-Alniditan 91 Human Binding pKi = 5 5.0 -1096 34
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 3261 3H-GR-125743 23 Human Binding pKi = 5 5.0 -2089 29
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 3261 3H-GR-125743 23 Human Binding pKi = 5 5.0 -2089 29
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 3261 3H-GR-125743 23 Human Binding pKi = 5 5.0 -2089 29
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
5074 3332 125I-CYP 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 3332 3H-GR-125743 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 125I-CYP 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 3H-GR-125743 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 125I-CYP 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 3H-GR-125743 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 125I-CYP 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 3H-GR-125743 80 Rat Binding pKi = 5 5.0 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2402 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095.0 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 3370 3H-GR-125743 62 Human Binding pKi = 5 5.0 -660 24
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 3464 3H-5-CT 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
128563 3464 3H-GR-125743 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 3H-5-CT 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 3464 3H-GR-125743 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 3H-5-CT 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 3464 3H-GR-125743 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 3H-5-CT 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 3464 3H-GR-125743 33 Human Binding pKi = 5 5.0 -2398 42
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
221 3491 UNDEFINED 71 Human Binding pKi = 5 5.0 -478 14
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 3491 UNDEFINED 71 Human Binding pKi = 5 5.0 -478 14
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 3491 UNDEFINED 71 Human Binding pKi = 5 5.0 -478 14
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
2464 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253.0 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 3640 125I-ICYP 58 Rat Binding pKi = 5 5.0 -165 6
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
2470 3653 3H-5HT 50 Human Binding pKi = 5 5.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 125I-ICYP 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 3H-5HT 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 3H-5HT 50 Human Binding pKi = 5 5.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 125I-ICYP 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 3H-5HT 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 3H-5HT 50 Human Binding pKi = 5 5.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 125I-ICYP 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 3H-5HT 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 3H-5HT 50 Human Binding pKi = 5 5.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 125I-ICYP 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 3H-5HT 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 3H-5HT 50 Human Binding pKi = 5 5.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 125I-ICYP 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 3H-5HT 50 Rat Binding pKi = 5 5.0 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5268 3656 125I-CYP 40 Rat Binding pKi = 5 5.0 -31622 18
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 3656 125I-CYP 40 Rat Binding pKi = 5 5.0 -31622 18
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 3656 125I-CYP 40 Rat Binding pKi = 5 5.0 -31622 18
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
1267 3804 3H-5HT 49 Rat Binding pKi = 5 5.0 -4168 26
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 3804 3H-5HT 49 Rat Binding pKi = 5 5.0 -4168 26
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 3804 3H-5HT 49 Rat Binding pKi = 5 5.0 -4168 26
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
213 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533.0 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 3H-GR-125743 55 Human Binding pKi = 5 5.0 -912 44
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1150 3878 125I-CYP 121 Rat Binding pKi = 5 5.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 125I-CYP 121 Rat Binding pKi = 5 5.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 125I-CYP 121 Rat Binding pKi = 5 5.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 125I-CYP 121 Rat Binding pKi = 5 5.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
185 4006 3H-GR-125743 60 Rat Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 4006 3H-GR-125743 60 Rat Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 4006 3H-GR-125743 60 Rat Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 4006 3H-GR-125743 60 Rat Binding pKi = 5 5.0 -30902 37
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
102 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Mouse Binding pKi = 5 5.0 -186 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
108182 4131 3H-5HT 22 Human Binding pKi = 5 5.0 -32 16
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 4131 3H-5HT 22 Human Binding pKi = 5 5.0 -32 16
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 4131 3H-5HT 22 Human Binding pKi = 5 5.0 -32 16
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
2662 11384 3H-GR-125743 131 Human Binding pKi = 5 5.0 -41 30
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 11384 3H-GR-125743 131 Human Binding pKi = 5 5.0 -41 30
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
5090 15561 3H-GR-125743 106 Human Binding pKi = 5 5.0 -1348 30
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 15561 3H-GR-125743 106 Human Binding pKi = 5 5.0 -1348 30
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
671690 27097 125I-ICYP 35 Rat Binding pKi = 5 5.0 -10 10
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
CHEMBL1365455 27097 125I-ICYP 35 Rat Binding pKi = 5 5.0 -10 10
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
10297 27112 3H-GR-125743 30 Human Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 27112 3H-GR-125743 30 Human Binding pKi = 5 5.0 -38 42
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
127151 35330 3H-GR-125743 18 Human Binding pKi = 5 5.0 -1584 10
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
3022645 35330 3H-GR-125743 18 Human Binding pKi = 5 5.0 -1584 10
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
CHEMBL14370 35330 3H-GR-125743 18 Human Binding pKi = 5 5.0 -1584 10
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
156391 46800 3H-GR-125743 99 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 46800 3H-GR-125743 99 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 46800 3H-GR-125743 99 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
5475158 67213 3H-5HT 25 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 67213 3H-5HT 25 Rat Binding pKi = 5 5.0 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
10624 70300 3H-GR-125743 19 Human Binding pKi = 5 5.0 -776 33
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
10624.0 70300 3H-GR-125743 19 Human Binding pKi = 5 5.0 -776 33
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 70300 3H-GR-125743 19 Human Binding pKi = 5 5.0 -776 33
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 70300 3H-GR-125743 19 Human Binding pKi = 5 5.0 -776 33
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
DB11664 70300 3H-GR-125743 19 Human Binding pKi = 5 5.0 -776 33
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
108107 79944 3H-5HT 38 Rat Binding pKi = 5 5.0 -15 16
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 79944 3H-5HT 38 Rat Binding pKi = 5 5.0 -15 16
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 79944 3H-5HT 38 Rat Binding pKi = 5 5.0 -15 16
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 79944 3H-5HT 38 Rat Binding pKi = 5 5.0 -15 16
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
442108 84636 3H-5-CT 6 Human Binding pKi = 5 5.0 -1 12
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 84636 3H-5-CT 6 Human Binding pKi = 5 5.0 -1 12
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
2244 94233 3H-GR-125743 100 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 94233 3H-GR-125743 100 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
104870 98880 3H-GR-125743 47 Human Binding pKi = 5 5.0 -549 21
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 98880 3H-GR-125743 47 Human Binding pKi = 5 5.0 -549 21
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 98880 3H-GR-125743 47 Human Binding pKi = 5 5.0 -549 21
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
55191 99617 125I-CYP 64 Rat Binding pKi = 5 5.0 -446 9
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
55191.0 99617 125I-CYP 64 Rat Binding pKi = 5 5.0 -446 9
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
CHEMBL284092 99617 125I-CYP 64 Rat Binding pKi = 5 5.0 -446 9
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
DB12184 99617 125I-CYP 64 Rat Binding pKi = 5 5.0 -446 9
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
44208932 140707 UNDEFINED 7 Human Binding pKi = 5 5.0 -89125 36
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 140707 UNDEFINED 7 Human Binding pKi = 5 5.0 -89125 36
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1615 167791 3H-GR-125743 24 Human Binding pKi = 5 5.0 -26 44
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 167791 3H-GR-125743 24 Human Binding pKi = 5 5.0 -26 44
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
43815 186920 3H-5HT 64 Rat Binding pKi = 5 5.0 -1995 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 186920 3H-5HT 64 Rat Binding pKi = 5 5.0 -1995 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 186920 3H-5HT 64 Rat Binding pKi = 5 5.0 -1995 25
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
24882267 188327 UNDEFINED 0 Human Binding pKi = 5 5.0 -776 2
NoneNone
PDSP KiDatabase 840 19 4 4 12.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500749 188327 UNDEFINED 0 Human Binding pKi = 5 5.0 -776 2
NoneNone
PDSP KiDatabase 840 19 4 4 12.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24882192 188802 UNDEFINED 0 Human Binding pKi = 5 5.0 -125 2
NoneNone
PDSP KiDatabase 714 10 4 4 8.9 O=C(Nc1ccc2[nH]cc(C3CCN(CCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL505954 188802 UNDEFINED 0 Human Binding pKi = 5 5.0 -125 2
NoneNone
PDSP KiDatabase 714 10 4 4 8.9 O=C(Nc1ccc2[nH]cc(C3CCN(CCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24881552 189111 UNDEFINED 0 Human Binding pKi = 5 5.0 -45 2
NoneNone
PDSP KiDatabase 700 9 4 4 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL510280 189111 UNDEFINED 0 Human Binding pKi = 5 5.0 -45 2
NoneNone
PDSP KiDatabase 700 9 4 4 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
3672 192533 3H-GR-125743 136 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 192533 3H-GR-125743 136 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 193615 3H-GR-125743 112 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 193615 3H-GR-125743 112 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
2771 195017 3H-5CT 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 195017 3H-GR-125743 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 195017 3H-5HT 74 Rat Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 3H-5CT 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 3H-GR-125743 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 195017 3H-5HT 74 Rat Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 3H-5CT 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 3H-GR-125743 74 Human Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 195017 3H-5HT 74 Rat Binding pKi = 5 5.0 -120 27
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
4495 196535 3H-GR-125743 92 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 196535 3H-GR-125743 92 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 200551 3H-GR-125743 115 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 200551 3H-GR-125743 115 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 200551 3H-GR-125743 115 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 202274 3H-GR-125743 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 202274 3H-GR-125743 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 202274 3H-GR-125743 22 Human Binding pKi = 5 5.0 -239 43
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3036864 202754 125I-CYP 19 Rat Binding pKi = 5 5.0 -41686 28
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 202754 125I-CYP 19 Rat Binding pKi = 5 5.0 -41686 28
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 202754 125I-CYP 19 Rat Binding pKi = 5 5.0 -41686 28
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 202754 125I-CYP 19 Rat Binding pKi = 5 5.0 -41686 28
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5281600 203025 3H-5CT 92 Human Binding pKi = 5 5.0 -173 33
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203025 3H-5CT 92 Human Binding pKi = 5 5.0 -173 33
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 203066 3H-5HT 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
5656 203066 3H-GR-125743 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 3H-5HT 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 203066 3H-GR-125743 87 Human Binding pKi = 5 5.0 -79 40
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 203483 3H-CYANOPINDOLOL 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 203483 3H-CYANOPINDOLOL 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 203483 3H-CYANOPINDOLOL 15 Rat Binding pKi = 5 5.0 -3 36
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
1614 203655 3H-5HT 24 Rat Binding pKi = 5 5.0 -81 10
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 203655 3H-5HT 24 Rat Binding pKi = 5 5.0 -81 10
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
202478 204687 3H-GR-125743 20 Rat Binding pKi = 5 5.0 -97 25
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 204687 3H-GR-125743 20 Rat Binding pKi = 5 5.0 -97 25
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 204718 3H-GR125743 17 Human Binding pKi = 5 5.0 -1 18
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 204718 3H-GR125743 17 Human Binding pKi = 5 5.0 -1 18
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4158 205341 3H-GR-125743 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 205341 3H-GR-125743 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 205341 3H-GR-125743 21 Human Binding pKi = 5 5.0 -141 21
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 205501 3H-GR-125743 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 205501 3H-GR-125743 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 205501 3H-GR-125743 72 Human Binding pKi = 5 5.0 -1 36
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
119607 206203 3H-GR-125743 113 Human Binding pKi = 5 5.0 -97 27
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 206203 3H-GR-125743 113 Human Binding pKi = 5 5.0 -97 27
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
16231 207509 3H-5HT 57 Rat Binding pKi = 5 5.0 -7 17
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 207509 3H-5HT 57 Rat Binding pKi = 5 5.0 -7 17
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
16212426 215931 125I-CYP 0 Rat Binding pKi = 5 5.0 -1 4
NoneNone
PDSP KiDatabase 403 2 7 8 -0.8 CN1CC(=O)N=C1N.C1=C(C=C(C2=C1C(=CN2)CCN)O)O.OS(=O)(=O)O None
57174031 215940 3H-5HT 0 Human Binding pKi = 5 5.0 -1778 19
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 215940 125I-CYP 0 Rat Binding pKi = 5 5.0 -1778 19
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 215940 125I-ICYP 0 Rat Binding pKi = 5 5.0 -1778 19
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 215940 3H-5HT 0 Rat Binding pKi = 5 5.0 -1778 19
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 215943 3H-5HT 0 Rat Binding pKi = 5 5.0 -7943 11
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
138107169 215952 125I-CYP 0 Rat Binding pKi = 5 5.0 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 125I-CYP 0 Rat Binding pKi = 5 5.0 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
77590 215955 3H-5HT 0 Rat Binding pKi = 5 5.0 -138 6
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
None 215993 3H-5-CT 0 Human Binding pKi = 5 5.0 -1 28
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 216019 3H-GR-125743 0 Human Binding pKi = 5 5.0 -38018 37
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 216020 3H-8-OH-DPAT 0 Human Binding pKi = 5 5.0 -154 7
NoneNone
PDSP KiDatabase 265 5 1 2 3.5 CCCN(CCC)C1CCC2=C(C=CC(=C2C1)O)F None
None 216128 125I-ICYP 0 Human Binding pKi = 5 5.0 -1 13
NoneNone
PDSP KiDatabase 164 3 1 3 0.8 C1CNC1COC2=CN=CC=C2 None
None 216135 3H-KETANSERIN 0 Rat Binding pKi = 5 5.0 -3162 24
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
25137849 216179 3H-GR-125743 0 Human Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 216179 3H-GR-125743 0 Human Binding pKi = 5 5.0 -4 40
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
62857 216181 3H-5HT 0 Rat Binding pKi = 5 5.0 -154 7
NoneNone
PDSP KiDatabase 345 6 1 2 4.9 CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl None
None 216254 3H-5HT 0 Rat Binding pKi = 5 5.0 -8317 19
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 216311 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 216312 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 216313 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 216314 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 33
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 216316 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 39
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 216317 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 38
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 216318 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 30
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 216325 3H-GR-125743 0 Human Binding pKi = 5 5.0 -13 40
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 216326 3H-GR-125743 0 Human Binding pKi = 5 5.0 -16 40
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 216342 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1862 19
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 216389 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 216390 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 28
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 216391 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 28
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 216392 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 27
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 216393 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1412 26
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 216394 3H-GR-125743 0 Human Binding pKi = 5 5.0 -1 29
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 216395 3H-GR-125743 0 Human Binding pKi = 5 5.0 -7 28
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
688390 216485 125I-ICYP 0 Rat Binding pKi = 5 5.0 -21 3
NoneNone
PDSP KiDatabase 267 5 2 4 2.5 C[C@H]([C@H](C1=C(C=CC(=C1)OC)OC)O)NC(C)(C)C None
None 216489 3H-GR-125743 0 Human Binding pKi = 5 5.0 -4570 27
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1150 3878 125I-CYP 121 Rat Binding pKi = 6.0 6.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 125I-CYP 121 Rat Binding pKi = 6.0 6.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 125I-CYP 121 Rat Binding pKi = 6.0 6.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 125I-CYP 121 Rat Binding pKi = 6.0 6.0 -204 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
None 217235 UNDEFINED 0 Human Binding pKi = 7.0 7.0 -4 2
NoneNone
PDSP KiDatabase 726 10 4 4 9.0 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC=CCN5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
115 3791 125I-ICYP 80 Rat Binding pKi = 7.0 7.0 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-ICYP 80 Rat Binding pKi = 7.0 7.0 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-ICYP 80 Rat Binding pKi = 7.0 7.0 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
11297 67345 125I-CYP 18 Rat Binding pKi = 6.0 6.0 -26 6
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
11297 67345 3H-5HT 18 Rat Binding pKi = 6.0 6.0 -26 6
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
CHEMBL18855 67345 125I-CYP 18 Rat Binding pKi = 6.0 6.0 -26 6
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
CHEMBL18855 67345 3H-5HT 18 Rat Binding pKi = 6.0 6.0 -26 6
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
3033677 202944 125I-CYP 40 Rat Binding pKi = 6.0 6.0 -5370 9
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
CHEMBL2355519 202944 125I-CYP 40 Rat Binding pKi = 6.0 6.0 -5370 9
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
CHEMBL62919 202944 125I-CYP 40 Rat Binding pKi = 6.0 6.0 -5370 9
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
2995 204405 3H-5CT 53 Human Binding pKi = 7.0 7.0 -3 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995.0 204405 3H-5CT 53 Human Binding pKi = 7.0 7.0 -3 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 3H-5CT 53 Human Binding pKi = 7.0 7.0 -3 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 3H-5CT 53 Human Binding pKi = 7.0 7.0 -3 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 204405 3H-5CT 53 Human Binding pKi = 7.0 7.0 -3 23
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
None 215956 125I-CYP 0 Rat Binding pKi = 6.0 6.0 -141 6
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
None 215956 3H-5HT 0 Rat Binding pKi = 6.0 6.0 -141 6
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
None 216278 3H-5CT 0 Human Binding pKi = 6.0 6.0 -12022 12
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
None 215971 3H-5HT 0 Rat Binding pKi = 6.0 6.0 -2344 15
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
115237 55585 3H-GR-125743 119 Human Binding pKi = 7.0 7.0 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-GR-125743 119 Human Binding pKi = 7.0 7.0 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-GR-125743 119 Human Binding pKi = 7.0 7.0 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-GR-125743 119 Human Binding pKi = 7.0 7.0 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
100 3805 3H-GR-125743 58 Human Binding pKi = 7.0 7.0 -13 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 3H-GR-125743 58 Human Binding pKi = 7.0 7.0 -13 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 3H-GR-125743 58 Human Binding pKi = 7.0 7.0 -13 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 3H-GR-125743 58 Human Binding pKi = 7.0 7.0 -13 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 3H-GR-125743 58 Human Binding pKi = 7.0 7.0 -13 55
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
71299720 215951 125I-ICYP 0 Rat Binding pKi = 7.0 7.0 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
2337 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-GR-125743 77 Human Binding pKi = 6.0 6.0 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
7153 98020 125I-ICYP 77 Rat Binding pKi = 7.0 7.0 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 125I-ICYP 77 Rat Binding pKi = 7.0 7.0 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
31101 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101.0 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 125I-CYP 40 Rat Binding pKi = 7.0 7.0 -48 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
127404 97584 125I-CYP 22 Rat Binding pKi = 7.0 7.0 -2 4
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
127404 97584 3H-5HT 22 Rat Binding pKi = 7.0 7.0 -2 4
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
CHEMBL27077 97584 125I-CYP 22 Rat Binding pKi = 7.0 7.0 -2 4
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
CHEMBL27077 97584 3H-5HT 22 Rat Binding pKi = 7.0 7.0 -2 4
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
None 216344 3H-GR-125743 0 Rat Binding pKi = 7.0 7.0 -26 2
NoneNone
PDSP KiDatabase 338 6 3 5 1.7 C1CNC(=NC1)NCCCNCC2CCC3=CC=CC=C3O2.Cl None
1222 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396.0 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 3H-Alniditan 49 Human Binding pKi = 6.0 6.0 -134 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
115 3791 3H-5HT 80 Human Binding pKi = 6.9 6.9 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Human Binding pKi = 6.9 6.9 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Human Binding pKi = 6.9 6.9 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
71299720 215951 125I-CYP 0 Rat Binding pKi = 6.9 6.9 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
71299720 215951 3H-5HT 0 Rat Binding pKi = 6.9 6.9 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1809 134 3H-GR-125743 32 Human Binding pKi = 7.9 7.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-GR-125743 32 Human Binding pKi = 7.9 7.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-GR-125743 32 Human Binding pKi = 7.9 7.9 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
115237 55585 3H-Alniditan 119 Human Binding pKi = 7.9 7.9 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-Alniditan 119 Human Binding pKi = 7.9 7.9 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-Alniditan 119 Human Binding pKi = 7.9 7.9 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-Alniditan 119 Human Binding pKi = 7.9 7.9 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1342 35 3H-5HT 49 Human Binding pKi = 7.9 7.9 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 3H-5HT 49 Human Binding pKi = 7.9 7.9 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 3H-5HT 49 Human Binding pKi = 7.9 7.9 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
None 215946 3H-5HT 0 Human Binding pKi = 7.9 7.9 -8 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 215946 3H-5HT 0 Human Binding pKi = 7.9 7.9 -8 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 216343 3H-GR-125743 0 Rat Binding pKi = 7.9 7.9 -1 2
NoneNone
PDSP KiDatabase 228 2 1 3 2.6 C1CNCCC1SC2=NC(=CC=C2)Cl None
4106 2502 125I-ICYP 22 Rat Binding pKi = 7.9 7.9 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-ICYP 22 Rat Binding pKi = 7.9 7.9 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-ICYP 22 Rat Binding pKi = 7.9 7.9 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-ICYP 22 Rat Binding pKi = 7.9 7.9 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 187 3H-5HT 55 Human Binding pKi = 6.9 6.9 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 6.9 6.9 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 6.9 6.9 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 6.9 6.9 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
135398737 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2176 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-8-OH-DPAT 68 Human Binding pKi = 5.9 5.9 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
10060720 205672 3H-5HT 14 Rat Binding pKi = 5.9 5.9 -46 4
NoneNone
PDSP KiDatabase 251 7 1 3 2.9 CCCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8214 205672 3H-5HT 14 Rat Binding pKi = 5.9 5.9 -46 4
NoneNone
PDSP KiDatabase 251 7 1 3 2.9 CCCCc1cc(OC)c(CC(C)N)cc1OC None
None 216450 UNDEFINED 0 Human Binding pKi = 6.9 6.9 -8 28
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
24881618 188787 UNDEFINED 0 Human Binding pKi = 6.9 6.9 -125 2
NoneNone
PDSP KiDatabase 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL505750 188787 UNDEFINED 0 Human Binding pKi = 6.9 6.9 -125 2
NoneNone
PDSP KiDatabase 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24881619 189038 UNDEFINED 0 Human Binding pKi = 6.9 6.9 -9 2
NoneNone
PDSP KiDatabase 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL509314 189038 UNDEFINED 0 Human Binding pKi = 6.9 6.9 -9 2
NoneNone
PDSP KiDatabase 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
11957541 1459 3H-5HT 40 Rat Binding pKi = 5.9 5.9 -288 16
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 1459 3H-5HT 40 Rat Binding pKi = 5.9 5.9 -288 16
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 1459 3H-5HT 40 Rat Binding pKi = 5.9 5.9 -288 16
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 1459 3H-5HT 40 Rat Binding pKi = 5.9 5.9 -288 16
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 1459 3H-5HT 40 Rat Binding pKi = 5.9 5.9 -288 16
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
133 2496 125I-ICYP 52 Rat Binding pKi = 6.9 6.9 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 125I-ICYP 52 Rat Binding pKi = 6.9 6.9 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 125I-ICYP 52 Rat Binding pKi = 6.9 6.9 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 125I-ICYP 52 Rat Binding pKi = 6.9 6.9 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 125I-ICYP 52 Rat Binding pKi = 6.9 6.9 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
206 2493 3H-5HT 16 Human Binding pKi = 5.9 5.9 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 3H-5HT 16 Human Binding pKi = 5.9 5.9 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 3H-5HT 16 Human Binding pKi = 5.9 5.9 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
123707 216484 125I-ICYP 0 Rat Binding pKi = 5.9 5.9 -295 3
NoneNone
PDSP KiDatabase 416 9 3 6 1.8 CC1=C(C=C(C=C1)C(CNCCOC2=CC=CC=C2OC)O)S(=O)(=O)N.Cl None
122 1437 3H-5HT 9 Human Binding pKi = 7.9 7.9 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 1437 3H-5HT 9 Human Binding pKi = 7.9 7.9 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 1437 3H-5HT 9 Human Binding pKi = 7.9 7.9 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
2865 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-5HT 73 Rat Binding pKi = 6.9 6.9 -263 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
135398737 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-5HT 93 Rat Binding pKi = 5.9 5.9 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2176 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-ICYP 68 Rat Binding pKi = 6.9 6.9 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
115 3791 125I-CYP 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 3791 3H-5HT 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-CYP 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-CYP 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 6.9 6.9 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2389 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-5HT 118 Rat Binding pKi = 5.9 5.9 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1346 83 125I-ICYP 117 Rat Binding pKi = 6.9 6.9 -40 9
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
280 83 125I-ICYP 117 Rat Binding pKi = 6.9 6.9 -40 9
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
9899402 83 125I-ICYP 117 Rat Binding pKi = 6.9 6.9 -40 9
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
CHEMBL9666 83 125I-ICYP 117 Rat Binding pKi = 6.9 6.9 -40 9
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
135398745 2914 3H-5HT 112 Rat Binding pKi = 5.9 5.9 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-5HT 112 Rat Binding pKi = 5.9 5.9 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-5HT 112 Rat Binding pKi = 5.9 5.9 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-5HT 112 Rat Binding pKi = 5.9 5.9 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-5HT 112 Rat Binding pKi = 5.9 5.9 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5 139 125I-ICYP 72 Rat Binding pKi = 7.9 7.9 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-ICYP 72 Rat Binding pKi = 7.9 7.9 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-ICYP 72 Rat Binding pKi = 7.9 7.9 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-ICYP 72 Rat Binding pKi = 7.9 7.9 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
180 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160.0 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 3H-MESULERGINE 56 Cat Binding pKi = 6.8 6.8 -281 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
71299720 215951 3H-5HT 0 Rat Binding pKi = 6.8 6.8 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
127 3126 3H-GR-125743 52 Guinea pig Binding pKi = 5.8 5.8 -3388 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 3H-GR-125743 52 Guinea pig Binding pKi = 5.8 5.8 -3388 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 3H-GR-125743 52 Guinea pig Binding pKi = 5.8 5.8 -3388 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
2726 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 3H-GR-125743 68 Human Binding pKi = 5.8 5.8 -54 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 3H-5HT 68 Rat Binding pKi = 5.8 5.8 -147 72
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
107 141 3H-5HT 121 Rat Binding pKi = 7.8 7.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Rat Binding pKi = 7.8 7.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Rat Binding pKi = 7.8 7.8 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 139 3H-5HT 72 Human Binding pKi = 7.8 7.8 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 125I-ICYP 72 Rat Binding pKi = 7.8 7.8 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 7.8 7.8 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-ICYP 72 Rat Binding pKi = 7.8 7.8 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 7.8 7.8 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-ICYP 72 Rat Binding pKi = 7.8 7.8 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 7.8 7.8 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-ICYP 72 Rat Binding pKi = 7.8 7.8 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
133 2496 3H-GR-125743 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-GR-125743 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-GR-125743 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-GR-125743 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-GR-125743 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2220 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400.0 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3134 3H-5HT 82 Rat Binding pKi = 5.8 5.8 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
1621 2429 125I-CYP 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 125I-CYP 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 125I-CYP 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 125I-CYP 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 125I-CYP 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954259 215979 3H-GR-125743 0 Human Binding pKi = 6.8 6.8 -501 43
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
2176 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-ICYP 68 Rat Binding pKi = 6.8 6.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
102 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Rat Binding pKi = 6.8 6.8 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
134 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 125I-CYP 24 Rat Binding pKi = 5.8 5.8 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1342 35 125I-CYP 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 35 3H-5HT 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 125I-CYP 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 3H-5HT 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 125I-CYP 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 3H-5HT 49 Rat Binding pKi = 6.8 6.8 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
102 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 35S-GTPGammaS 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-GR-125743 48 Human Binding pKi = 6.8 6.8 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1588 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864.0 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 3H-5-CT 27 Human Binding pKi = 7.8 7.8 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
24881201 186849 UNDEFINED 0 Human Binding pKi = 7.8 7.8 -4 2
NoneNone
PDSP KiDatabase 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL489453 186849 UNDEFINED 0 Human Binding pKi = 7.8 7.8 -4 2
NoneNone
PDSP KiDatabase 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
138107169 215952 3H-5HT 0 Human Binding pKi = 7.8 7.8 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 3H-5HT 0 Human Binding pKi = 7.8 7.8 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
4106 2502 3H-5HT 22 Human Binding pKi = 7.8 7.8 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Human Binding pKi = 7.8 7.8 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Human Binding pKi = 7.8 7.8 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Human Binding pKi = 7.8 7.8 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2181 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830.0 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 3H-Alniditan 46 Human Binding pKi = 6.8 6.8 -70 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
277 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 3H-5CT 62 Human Binding pKi = 5.8 5.8 -1905 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
134 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Human Binding pKi = 6.8 6.8 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
7153 98020 3H-5CT 77 Human Binding pKi = 6.8 6.8 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5CT 77 Human Binding pKi = 6.8 6.8 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
45266826 217691 [3H] 5-CT 0 Human Binding pKi = 5.8 5.8 -2 8
NoneNone
PDSP KiDatabase 177 3 1 2 1.8 CC1=CC=C(C=C1)C(=O)C(C)NC None
133 2496 125I-ICYP 52 Rat Binding pKi = 6.8 6.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 125I-ICYP 52 Rat Binding pKi = 6.8 6.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 125I-ICYP 52 Rat Binding pKi = 6.8 6.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 125I-ICYP 52 Rat Binding pKi = 6.8 6.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 125I-ICYP 52 Rat Binding pKi = 6.8 6.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1353 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-GR-125743 93 Human Binding pKi = 6.8 6.8 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
133 2496 125I-ICYP 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 125I-ICYP 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 125I-ICYP 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 125I-ICYP 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 125I-ICYP 52 Rat Binding pKi = 7.8 7.8 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
165193 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Rat Binding pKi = 7.8 7.8 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2176 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-CYP 68 Rat Binding pKi = 7.8 7.8 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1621 2429 3H-5HT 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 3H-5HT 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 3H-5HT 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 3H-5HT 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 3H-5HT 17 Rat Binding pKi = 6.8 6.8 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2543 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-GR-125743 68 Guinea pig Binding pKi = 6.8 6.8 -48 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4631 194972 125I-ICYP 29 Rat Binding pKi = 6.8 6.8 -22 7
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
4631.0 194972 125I-ICYP 29 Rat Binding pKi = 6.8 6.8 -22 7
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
CHEMBL546 194972 125I-ICYP 29 Rat Binding pKi = 6.8 6.8 -22 7
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
DB01580 194972 125I-ICYP 29 Rat Binding pKi = 6.8 6.8 -22 7
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
132787 3430 3H-5HT 45 Rat Binding pKi = 5.8 5.8 -1000 6
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
26 3430 3H-5HT 45 Rat Binding pKi = 5.8 5.8 -1000 6
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
32 3430 3H-5HT 45 Rat Binding pKi = 5.8 5.8 -1000 6
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
CHEMBL49247 3430 3H-5HT 45 Rat Binding pKi = 5.8 5.8 -1000 6
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
179 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159.0 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 3H-5CT 115 Human Binding pKi = 5.8 5.8 -43 49
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
24882268 172557 UNDEFINED 0 Human Binding pKi = 7.7 7.7 -11 2
NoneNone
PDSP KiDatabase 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL448555 172557 UNDEFINED 0 Human Binding pKi = 7.7 7.7 -11 2
NoneNone
PDSP KiDatabase 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
None 215938 3H-5HT 0 Human Binding pKi = 7.7 7.7 -3 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1588 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864.0 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 3H-GR-125743 27 Human Binding pKi = 7.7 7.7 -42 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2605 3783 3H-5HT 30 Rat Binding pKi = 6.7 6.7 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 3783 3H-5HT 30 Rat Binding pKi = 6.7 6.7 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 3783 3H-5HT 30 Rat Binding pKi = 6.7 6.7 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 3783 3H-5HT 30 Rat Binding pKi = 6.7 6.7 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 3783 3H-5HT 30 Rat Binding pKi = 6.7 6.7 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
134 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 125I-ICYP 24 Rat Binding pKi = 5.7 5.7 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
3337 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
164 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
134 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-GR-125743 24 Guinea pig Binding pKi = 6.7 6.7 -158 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1809 134 3H-5HT 32 Rat Binding pKi = 7.7 7.7 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Rat Binding pKi = 7.7 7.7 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Rat Binding pKi = 7.7 7.7 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
102 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5-CT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3337 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-GR-125743 27 Human Binding pKi = 5.7 5.7 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
173 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1524 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 125I-CYP 96 Rat Binding pKi = 5.7 5.7 -512 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1531 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869.0 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 2266 125I-ICYP 69 Rat Binding pKi = 5.7 5.7 -676 16
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
2543 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.7 8.7 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
11954224 215953 125I-CYP 0 Rat Binding pKi = 8.7 8.7 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 125I-CYP 0 Rat Binding pKi = 8.7 8.7 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 125I-CYP 0 Rat Binding pKi = 8.7 8.7 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 125I-CYP 0 Rat Binding pKi = 8.7 8.7 -12 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
71299720 215951 3H-5HT 0 Human Binding pKi = 8.7 8.7 1 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
5 139 3H-GR-125743 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-GR-125743 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-GR-125743 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-GR-125743 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 215938 3H-5HT 0 Human Binding pKi = 8.6 8.6 -3 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
134 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-GR-125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-GR125743 24 Human Binding pKi = 8.6 8.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
5 139 3H-5CT 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5CT 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5CT 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5CT 72 Guinea pig Binding pKi = 8.6 8.6 -5 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
132 1275 3H-5HT 13 Mouse Binding pKi = 8.6 8.6 -125 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-5HT 13 Mouse Binding pKi = 8.6 8.6 -125 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-5HT 13 Mouse Binding pKi = 8.6 8.6 -125 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
124 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 3H-5HT 47 Rat Binding pKi = 8.6 8.6 -2 33
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 215946 3H-5HT 0 Rat Binding pKi = 8.6 8.6 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 139 3H-5HT 72 Rat Binding pKi = 8.6 8.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.6 8.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.6 8.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.6 8.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 215938 3H-GR-125743 0 Rat Binding pKi = 8.6 8.6 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
132 1275 125I-ICYP 13 Rat Binding pKi = 8.6 8.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 125I-ICYP 13 Rat Binding pKi = 8.6 8.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 125I-ICYP 13 Rat Binding pKi = 8.6 8.6 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
71299720 215951 3H-5HT 0 Human Binding pKi = 8.5 8.5 1 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
152662 215957 125I-CYP 0 Rat Binding pKi = 8.5 8.5 109 7
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
None 215938 125I-ICYP 0 Rat Binding pKi = 8.5 8.5 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
2389 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-Alniditan 118 Human Binding pKi = 7.7 7.7 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
173 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
21163 215930 3H-5HT 0 Rat Binding pKi = 6.7 6.7 -4 5
NoneNone
PDSP KiDatabase 192 2 4 3 1.1 C1=C2C(=CC(=C1O)O)NC=C2CCN None
2337 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-Alniditan 77 Human Binding pKi = 5.7 5.7 -26 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
164 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 1460 3H-5HT 19 Rat Binding pKi = 5.7 5.7 -89 10
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
None 216322 3H-5HT 0 Rat Binding pKi = 5.7 5.7 -69 6
NoneNone
PDSP KiDatabase 390 4 1 4 3.2 C1CN(CCN1CCN2C3=CC=CC=C3NC2=O)C4=CC=C(C=C4)C(F)(F)F None
132 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
135398737 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-5CT 93 Human Binding pKi = 5.7 5.7 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
7153 98020 3H-5HT 77 Human Binding pKi = 6.7 6.7 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Human Binding pKi = 6.7 6.7 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
132 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-5HT 13 Human Binding pKi = 7.7 7.7 -602 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
102 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Human Binding pKi = 7.7 7.7 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
141 1427 125I-CYP 35 Rat Binding pKi = 5.7 5.7 -25 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 1427 125I-CYP 35 Rat Binding pKi = 5.7 5.7 -25 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 1427 125I-CYP 35 Rat Binding pKi = 5.7 5.7 -25 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 1427 125I-CYP 35 Rat Binding pKi = 5.7 5.7 -25 22
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
173 3262 125I-ICYP 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 125I-ICYP 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 125I-ICYP 95 Rat Binding pKi = 6.7 6.7 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1588 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864.0 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 125I-CYP 27 Rat Binding pKi = 6.7 6.7 -58 44
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
132 1275 3H-GR-125743 13 Guinea pig Binding pKi = 6.6 6.6 -6456 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 3H-GR-125743 13 Guinea pig Binding pKi = 6.6 6.6 -6456 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 3H-GR-125743 13 Guinea pig Binding pKi = 6.6 6.6 -6456 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
115237 55585 3H-Alniditan 119 Human Binding pKi = 7.6 7.6 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-Alniditan 119 Human Binding pKi = 7.6 7.6 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-Alniditan 119 Human Binding pKi = 7.6 7.6 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-Alniditan 119 Human Binding pKi = 7.6 7.6 -93 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
5 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 140 3H-5HT 49 Human Binding pKi = 7.6 7.6 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 3H-5HT 49 Human Binding pKi = 7.6 7.6 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 3H-5HT 49 Human Binding pKi = 7.6 7.6 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 3H-5HT 49 Human Binding pKi = 7.6 7.6 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
15897 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
542051 206100 3H-5HT 6 Rat Binding pKi = 5.6 5.6 -2630 7
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 206100 3H-5HT 6 Rat Binding pKi = 5.6 5.6 -2630 7
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
127 3126 125I-ICYP 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 125I-ICYP 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 125I-ICYP 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
5 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-CYP 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 7.6 7.6 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
15897 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-GR-125743 0 Human Binding pKi = 5.6 5.6 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
115 3791 3H-5HT 80 Human Binding pKi = 6.6 6.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Human Binding pKi = 6.6 6.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Human Binding pKi = 6.6 6.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
123686 1981 3H-5HT 51 Rat Binding pKi = 5.6 5.6 -2630 9
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
12581 1981 3H-5HT 51 Rat Binding pKi = 5.6 5.6 -2630 9
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
CHEMBL11268 1981 3H-5HT 51 Rat Binding pKi = 5.6 5.6 -2630 9
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
27402 205686 3H-5HT 18 Rat Binding pKi = 5.6 5.6 -46 6
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8224 205686 3H-5HT 18 Rat Binding pKi = 5.6 5.6 -46 6
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
173 3262 125I-ICYP 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 125I-ICYP 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 125I-ICYP 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
134 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Human Binding pKi = 7.6 7.6 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
127 3126 3H-GR-125743 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 3H-GR-125743 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 3H-GR-125743 52 Rat Binding pKi = 7.6 7.6 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
133 2496 3H-5HT 52 Rat Binding pKi = 7.6 7.6 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-5HT 52 Rat Binding pKi = 7.6 7.6 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-5HT 52 Rat Binding pKi = 7.6 7.6 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-5HT 52 Rat Binding pKi = 7.6 7.6 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-5HT 52 Rat Binding pKi = 7.6 7.6 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135398737 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-5HT 93 Rat Binding pKi = 5.6 5.6 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 215944 3H-5HT 0 Rat Binding pKi = 6.6 6.6 -229 7
NoneNone
PDSP KiDatabase 455 6 5 5 1.6 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C.C(=CC(=O)O)C(=O)O None
138107169 215952 3H-5HT 0 Human Binding pKi = 6.6 6.6 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 3H-5HT 0 Human Binding pKi = 6.6 6.6 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
7153 98020 UNDEFINED 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 UNDEFINED 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1524 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 3H-GR-125743 96 Human Binding pKi = 5.6 5.6 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
7153 98020 125I-ICYP 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 125I-ICYP 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1220 187 3H-5HT 55 Human Binding pKi = 6.6 6.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 6.6 6.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 6.6 6.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 6.6 6.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
2601 3780 3H-GR-125743 33 Human Binding pKi = 6.6 6.6 -87 21
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 3H-GR-125743 33 Human Binding pKi = 6.6 6.6 -87 21
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 3H-GR-125743 33 Human Binding pKi = 6.6 6.6 -87 21
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 3H-GR-125743 33 Human Binding pKi = 6.6 6.6 -87 21
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 3H-GR-125743 33 Human Binding pKi = 6.6 6.6 -87 21
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1220 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
115 3791 125I-ICYP 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-ICYP 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-ICYP 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
102 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Human Binding pKi = 7.6 7.6 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
173 3262 3H-5HT 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Rat Binding pKi = 6.6 6.6 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
7153 98020 125I-CYP 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 125I-CYP 77 Rat Binding pKi = 6.6 6.6 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5074 3332 3H-GR-125743 80 Human Binding pKi = 6.6 6.6 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 3H-GR-125743 80 Human Binding pKi = 6.6 6.6 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 3H-GR-125743 80 Human Binding pKi = 6.6 6.6 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 3H-GR-125743 80 Human Binding pKi = 6.6 6.6 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2303 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 3H-5HT 68 Human Binding pKi = 5.6 5.6 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
115 3791 3H-5HT 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 7.6 7.6 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
1353 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2389 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-5HT 118 Rat Binding pKi = 5.6 5.6 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1342 35 125I-CYP 49 Rat Binding pKi = 6.6 6.6 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 125I-CYP 49 Rat Binding pKi = 6.6 6.6 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 125I-CYP 49 Rat Binding pKi = 6.6 6.6 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
165193 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-GR-125743 0 Guinea pig Binding pKi = 5.6 5.6 -11748 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2543 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-GR-125743 68 Human Binding pKi = 7.6 7.6 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Human Binding pKi = 7.6 7.6 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
133 2496 3H-GR-125743 52 Guinea pig Binding pKi = 7.6 7.6 -52 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-GR-125743 52 Guinea pig Binding pKi = 7.6 7.6 -52 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-GR-125743 52 Guinea pig Binding pKi = 7.6 7.6 -52 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-GR-125743 52 Guinea pig Binding pKi = 7.6 7.6 -52 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-GR-125743 52 Guinea pig Binding pKi = 7.6 7.6 -52 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 125I-ICYP 43 Rat Binding pKi = 5.6 5.6 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2105 3054 3H-GR-125743 37 Human Binding pKi = 6.6 6.6 -436 33
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 3H-GR-125743 37 Human Binding pKi = 6.6 6.6 -436 33
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 3H-GR-125743 37 Human Binding pKi = 6.6 6.6 -436 33
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 3H-GR-125743 37 Human Binding pKi = 6.6 6.6 -436 33
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 3H-GR-125743 37 Human Binding pKi = 6.6 6.6 -436 33
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
4452 2762 3H-5CT 19 Human Binding pKi = 5.6 5.6 -95499 19
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 2762 3H-5CT 19 Human Binding pKi = 5.6 5.6 -95499 19
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 2762 3H-5CT 19 Human Binding pKi = 5.6 5.6 -95499 19
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
1220 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 5.6 5.6 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1353 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-Alniditan 93 Human Binding pKi = 6.6 6.6 -66 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 2914 3H-5HT 112 Rat Binding pKi = 5.6 5.6 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-5HT 112 Rat Binding pKi = 5.6 5.6 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-5HT 112 Rat Binding pKi = 5.6 5.6 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-5HT 112 Rat Binding pKi = 5.6 5.6 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-5HT 112 Rat Binding pKi = 5.6 5.6 -162 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3337 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 3H-GR-125743 27 Human Binding pKi = 5.6 5.6 -74 40
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
60820 4308 UNDEFINED 14 Human Binding pKi = 5.5 5.5 -144543 13
NoneNone
PDSP KiDatabase 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 None
CHEMBL10085 4308 UNDEFINED 14 Human Binding pKi = 5.5 5.5 -144543 13
NoneNone
PDSP KiDatabase 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 None
5074 3332 3H-GR-125743 80 Human Binding pKi = 6.5 6.5 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 3H-GR-125743 80 Human Binding pKi = 6.5 6.5 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 3H-GR-125743 80 Human Binding pKi = 6.5 6.5 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 3H-GR-125743 80 Human Binding pKi = 6.5 6.5 -478 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
4209 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893.0 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3163 125I-ICYP 75 Rat Binding pKi = 6.5 6.5 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
6437377 215954 125I-CYP 0 Rat Binding pKi = 5.5 5.5 -2398 5
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
25058166 215960 3H-GR-125743 0 Human Binding pKi = 5.5 5.5 -1479 27
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 215960 3H-GR-125743 0 Human Binding pKi = 5.5 5.5 -1479 27
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
5 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.5 8.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 2502 3H-5HT 22 Human Binding pKi = 8.5 8.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Human Binding pKi = 8.5 8.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Human Binding pKi = 8.5 8.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Human Binding pKi = 8.5 8.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
107780 1844 3H-5HT 54 Rat Binding pKi = 8.5 8.5 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-5HT 54 Rat Binding pKi = 8.5 8.5 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-5HT 54 Rat Binding pKi = 8.5 8.5 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
115 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 8.5 8.5 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
1809 134 3H-5HT 32 Rat Binding pKi = 8.5 8.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Rat Binding pKi = 8.5 8.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Rat Binding pKi = 8.5 8.5 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2543 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.5 8.5 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
134 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Human Binding pKi = 8.4 8.4 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
130 3500 3H-GR-125743 47 Guinea pig Binding pKi = 8.4 8.4 1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3500 3H-GR-125743 47 Guinea pig Binding pKi = 8.4 8.4 1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3500 3H-GR-125743 47 Guinea pig Binding pKi = 8.4 8.4 1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
None 215938 3H-5HT 0 Rat Binding pKi = 8.4 8.4 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 215946 125I-CYP 0 Rat Binding pKi = 8.4 8.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 215946 3H-5HT 0 Rat Binding pKi = 8.4 8.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1621 2429 3H-GR-125743 17 Rat Binding pKi = 8.4 8.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 3H-GR-125743 17 Rat Binding pKi = 8.4 8.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 3H-GR-125743 17 Rat Binding pKi = 8.4 8.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 3H-GR-125743 17 Rat Binding pKi = 8.4 8.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 3H-GR-125743 17 Rat Binding pKi = 8.4 8.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3036780.0 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 3H-Alniditan 20 Human Binding pKi = 8.4 8.4 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 215946 125I-CYP 0 Rat Binding pKi = 8.4 8.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6971132 216009 3H-5-CT 0 Human Binding pKi = 8.4 8.4 1 14
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
5 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
130 3500 3H-GR-125743 47 Rat Binding pKi = 7.5 7.5 -8 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3500 3H-GR-125743 47 Rat Binding pKi = 7.5 7.5 -8 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3500 3H-GR-125743 47 Rat Binding pKi = 7.5 7.5 -8 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107 141 3H-5HT 121 Rat Binding pKi = 7.5 7.5 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Rat Binding pKi = 7.5 7.5 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Rat Binding pKi = 7.5 7.5 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
165193 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Rat Binding pKi = 7.5 7.5 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
152662 215957 125I-CYP 0 Rat Binding pKi = 7.5 7.5 109 7
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
173 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
173 3262 125I-CYP 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
173 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 125I-CYP 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 125I-CYP 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 3262 3H-5HT 95 Rat Binding pKi = 6.5 6.5 -2 23
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
134 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-GR-125743 24 Rat Binding pKi = 6.5 6.5 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2220 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400.0 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 3134 125I-CYP 82 Rat Binding pKi = 5.5 5.5 -1023 14
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
4106 2502 3H-GR-125743 22 Human Binding pKi = 7.5 7.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-GR-125743 22 Human Binding pKi = 7.5 7.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-GR-125743 22 Human Binding pKi = 7.5 7.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-GR-125743 22 Human Binding pKi = 7.5 7.5 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135398745 2914 3H-5CT 112 Human Binding pKi = 5.5 5.5 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-5CT 112 Human Binding pKi = 5.5 5.5 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-5CT 112 Human Binding pKi = 5.5 5.5 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-5CT 112 Human Binding pKi = 5.5 5.5 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-5CT 112 Human Binding pKi = 5.5 5.5 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5311189 204841 3H-GR-125743 11 Rat Binding pKi = 5.5 5.5 -61 27
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 204841 3H-GR-125743 11 Rat Binding pKi = 5.5 5.5 -61 27
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
24881686 188389 UNDEFINED 0 Human Binding pKi = 7.5 7.5 -8 2
NoneNone
PDSP KiDatabase 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL501645 188389 UNDEFINED 0 Human Binding pKi = 7.5 7.5 -8 2
NoneNone
PDSP KiDatabase 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
71299720 215951 125I-ICYP 0 Rat Binding pKi = 7.5 7.5 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
None 215946 3H-GR-125743 0 Guinea pig Binding pKi = 7.5 7.5 -22 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 139 125I-ICYP 72 Rat Binding pKi = 7.5 7.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-ICYP 72 Rat Binding pKi = 7.5 7.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-ICYP 72 Rat Binding pKi = 7.5 7.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-ICYP 72 Rat Binding pKi = 7.5 7.5 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 140 3H-5HT 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 3H-5HT 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 3H-5HT 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 3H-5HT 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
None 216239 3H-GR-125743 0 Human Binding pKi = 6.5 6.5 -4677 30
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
115237 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398737 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-5HT 93 Rat Binding pKi = 5.5 5.5 -691 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
107 141 3H-5HT 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1212 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372.0 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 3H-GR-125743 50 Human Binding pKi = 6.5 6.5 -93 65
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
7153 98020 125I-CYP 77 Rat Binding pKi = 6.5 6.5 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 98020 3H-5HT 77 Rat Binding pKi = 6.5 6.5 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 125I-CYP 77 Rat Binding pKi = 6.5 6.5 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Rat Binding pKi = 6.5 6.5 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
446220 133521 3H-GR-125743 14 Human Binding pKi = 5.5 5.5 -23 45
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 3H-GR-125743 14 Human Binding pKi = 5.5 5.5 -23 45
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
2176 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-5HT 68 Rat Binding pKi = 7.5 7.5 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
15897 2862 3H-GR-125743 0 Human Binding pKi = 5.5 5.5 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 2862 3H-GR-125743 0 Human Binding pKi = 5.5 5.5 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 2862 3H-GR-125743 0 Human Binding pKi = 5.5 5.5 -95 36
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
107 141 3H-GR-125743 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-GR-125743 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-GR-125743 121 Human Binding pKi = 7.5 7.5 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 215950 125I-ICYP 0 Rat Binding pKi = 7.5 7.5 - 1
NoneNone
PDSP KiDatabase 310 7 2 4 2.6 CC(C)NCC(COC1=CC=CC=C1N2C=CC=C2)O.Cl None
115237 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 3H-5HT 119 Rat Binding pKi = 5.5 5.5 -14454 54
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
119570 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570.0 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 3H-GR-125743 96 Human Binding pKi = 5.5 5.5 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
145 140 125I-ICYP 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 125I-ICYP 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 125I-ICYP 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 125I-ICYP 49 Rat Binding pKi = 6.5 6.5 -47 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
11831220 192558 UNDEFINED 8 Human Binding pKi = 6.5 6.5 -8 2
NoneNone
PDSP KiDatabase 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 None
CHEMBL521235 192558 UNDEFINED 8 Human Binding pKi = 6.5 6.5 -8 2
NoneNone
PDSP KiDatabase 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 None
31101 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101.0 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 3H-GR-125743 40 Human Binding pKi = 6.5 6.5 -128 36
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
133 2496 3H-5HT 52 Human Binding pKi = 7.4 7.4 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-5HT 52 Human Binding pKi = 7.4 7.4 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-5HT 52 Human Binding pKi = 7.4 7.4 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-5HT 52 Human Binding pKi = 7.4 7.4 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-5HT 52 Human Binding pKi = 7.4 7.4 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
165193 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-GR-125743 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
7153 98020 3H-5HT 77 Human Binding pKi = 6.4 6.4 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Human Binding pKi = 6.4 6.4 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
2181 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830.0 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 3H-5HT 46 Rat Binding pKi = 5.4 5.4 -3090 35
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4595 176715 3H-Serotonin 106 Rat Binding pKi = 5.4 5.4 -7 15
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176715 3H-Serotonin 106 Rat Binding pKi = 5.4 5.4 -7 15
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
5074 3332 3H-GR-125743 80 Guinea pig Binding pKi = 6.4 6.4 -645 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 3H-GR-125743 80 Guinea pig Binding pKi = 6.4 6.4 -645 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 3H-GR-125743 80 Guinea pig Binding pKi = 6.4 6.4 -645 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 3H-GR-125743 80 Guinea pig Binding pKi = 6.4 6.4 -645 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5 139 3H-GR-125743 72 Human Binding pKi = 7.4 7.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-GR-125743 72 Human Binding pKi = 7.4 7.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-GR-125743 72 Human Binding pKi = 7.4 7.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-GR-125743 72 Human Binding pKi = 7.4 7.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 141 3H-GR-125743 121 Human Binding pKi = 7.4 7.4 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-GR-125743 121 Human Binding pKi = 7.4 7.4 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-GR-125743 121 Human Binding pKi = 7.4 7.4 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1220 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
24882266 188287 UNDEFINED 0 Human Binding pKi = 7.4 7.4 -2 2
NoneNone
PDSP KiDatabase 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500230 188287 UNDEFINED 0 Human Binding pKi = 7.4 7.4 -2 2
NoneNone
PDSP KiDatabase 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
1220 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 7.4 7.4 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
134 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 125I-ICYP 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1613 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964.0 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 3H-GR-125743 53 Human Binding pKi = 6.4 6.4 -13 44
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3682 189437 125I-ICYP 12 Rat Binding pKi = 5.4 5.4 -7585 8
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 189437 125I-ICYP 12 Rat Binding pKi = 5.4 5.4 -7585 8
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 189437 125I-ICYP 12 Rat Binding pKi = 5.4 5.4 -7585 8
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
1621 2429 125I-ICYP 17 Rat Binding pKi = 7.4 7.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 125I-ICYP 17 Rat Binding pKi = 7.4 7.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 125I-ICYP 17 Rat Binding pKi = 7.4 7.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 125I-ICYP 17 Rat Binding pKi = 7.4 7.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 125I-ICYP 17 Rat Binding pKi = 7.4 7.4 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
165193 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-ICYP 0 Rat Binding pKi = 7.4 7.4 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
1342 35 125I-ICYP 49 Rat Binding pKi = 7.4 7.4 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 125I-ICYP 49 Rat Binding pKi = 7.4 7.4 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 125I-ICYP 49 Rat Binding pKi = 7.4 7.4 -50 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
5 139 3H-5HT 72 Mouse Binding pKi = 7.4 7.4 -41 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Mouse Binding pKi = 7.4 7.4 -41 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Mouse Binding pKi = 7.4 7.4 -41 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Mouse Binding pKi = 7.4 7.4 -41 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 2502 3H-5HT 22 Human Binding pKi = 7.4 7.4 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Human Binding pKi = 7.4 7.4 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Human Binding pKi = 7.4 7.4 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Human Binding pKi = 7.4 7.4 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2543 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-GR-125743 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
138107169 215952 3H-5HT 0 Human Binding pKi = 7.4 7.4 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 3H-5HT 0 Human Binding pKi = 7.4 7.4 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
135398737 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-Alniditan 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
202 1508 3H-5HT 77 Human Binding pKi = 5.4 5.4 -1 30
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 3H-5HT 77 Human Binding pKi = 5.4 5.4 -1 30
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 3H-5HT 77 Human Binding pKi = 5.4 5.4 -1 30
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 3H-5HT 77 Human Binding pKi = 5.4 5.4 -1 30
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 3H-5HT 77 Human Binding pKi = 5.4 5.4 -1 30
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
107 141 125I-CYP 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 141 3H-5HT 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 125I-CYP 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 125I-CYP 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Rat Binding pKi = 6.4 6.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
135398737 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-GR-125743 93 Human Binding pKi = 6.4 6.4 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1809 134 125I-ICYP 32 Rat Binding pKi = 8.4 8.4 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 125I-ICYP 32 Rat Binding pKi = 8.4 8.4 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 125I-ICYP 32 Rat Binding pKi = 8.4 8.4 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107 141 125I-ICYP 121 Rat Binding pKi = 8.4 8.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 125I-ICYP 121 Rat Binding pKi = 8.4 8.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 125I-ICYP 121 Rat Binding pKi = 8.4 8.4 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2865 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-GR-125743 73 Human Binding pKi = 8.4 8.4 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 215946 125I-ICYP 0 Rat Binding pKi = 8.4 8.4 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
1809 134 3H-5HT 32 Human Binding pKi = 8.4 8.4 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 8.4 8.4 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 8.4 8.4 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 139 35S-GTPGammaS 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 35S-GTPGammaS 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 35S-GTPGammaS 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 35S-GTPGammaS 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 215938 125I-ICYP 0 Rat Binding pKi = 8.4 8.4 -18 21
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 216344 3H-GR-125743 0 Guinea pig Binding pKi = 8.4 8.4 26 2
NoneNone
PDSP KiDatabase 338 6 3 5 1.7 C1CNC(=NC1)NCCCNCC2CCC3=CC=CC=C3O2.Cl None
5 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Human Binding pKi = 8.4 8.4 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107780 1844 3H-GR-125743 54 Guinea pig Binding pKi = 8.4 8.4 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-GR-125743 54 Guinea pig Binding pKi = 8.4 8.4 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-GR-125743 54 Guinea pig Binding pKi = 8.4 8.4 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107780 1844 3H-GR-125743 54 Human Binding pKi = 8.4 8.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-GR-125743 54 Human Binding pKi = 8.4 8.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-GR-125743 54 Human Binding pKi = 8.4 8.4 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
441383 20333 None 57 Rat Binding pKi = 8.4 8.4 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 20333 None 57 Rat Binding pKi = 8.4 8.4 -19 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
176 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157.0 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 398 None 66 Rat Binding pKi = 8.4 8.4 -10 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
11954224 215953 3H-GR-125743 0 Human Binding pKi = 8.3 8.3 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 3H-GR-125743 0 Human Binding pKi = 8.3 8.3 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 3H-GR-125743 0 Human Binding pKi = 8.3 8.3 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 3H-GR-125743 0 Human Binding pKi = 8.3 8.3 -32 58
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
31703 194717 None 63 Rat Binding pKi = 8.3 8.3 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL359744 194717 None 63 Rat Binding pKi = 8.3 8.3 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL53463 194717 None 63 Rat Binding pKi = 8.3 8.3 -1 2
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
107 141 3H-5HT 121 Human Binding pKi = 8.3 8.3 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 3H-5HT 121 Human Binding pKi = 8.3 8.3 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 3H-5HT 121 Human Binding pKi = 8.3 8.3 -16 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2812 4779 None 101 Rat Binding pKi = 8.3 8.3 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 4779 None 101 Rat Binding pKi = 8.3 8.3 -51 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
None 215946 125I-ICYP 0 Rat Binding pKi = 8.3 8.3 2 24
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
133 2496 125I-CYP 52 Rat Binding pKi = 7.4 7.4 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 125I-CYP 52 Rat Binding pKi = 7.4 7.4 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 125I-CYP 52 Rat Binding pKi = 7.4 7.4 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 125I-CYP 52 Rat Binding pKi = 7.4 7.4 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 125I-CYP 52 Rat Binding pKi = 7.4 7.4 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Human Binding pKi = 7.4 7.4 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2389 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-5HT 118 Rat Binding pKi = 5.4 5.4 -6456 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135409468 2035 3H-GR-125743 69 Human Binding pKi = 6.4 6.4 -144 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 2035 3H-GR-125743 69 Human Binding pKi = 6.4 6.4 -144 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 2035 3H-GR-125743 69 Human Binding pKi = 6.4 6.4 -144 39
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
5281600 203025 3H-GR-125743 92 Human Binding pKi = 5.4 5.4 -173 33
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 203025 3H-GR-125743 92 Human Binding pKi = 5.4 5.4 -173 33
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
122 1437 3H-5HT 9 Human Binding pKi = 7.4 7.4 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 1437 3H-5HT 9 Human Binding pKi = 7.4 7.4 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 1437 3H-5HT 9 Human Binding pKi = 7.4 7.4 -5 11
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
2176 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-5HT 68 Human Binding pKi = 5.4 5.4 -1737 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
182596 118486 3H-5HT 16 Rat Binding pKi = 6.4 6.4 -269 3
NoneNone
PDSP KiDatabase 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
CHEMBL341391 118486 3H-5HT 16 Rat Binding pKi = 6.4 6.4 -269 3
NoneNone
PDSP KiDatabase 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
1978 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
1978.0 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
40 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
7107 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
CHEMBL642 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
DB01193 250 125I-ICYP 60 Rat Binding pKi = 5.4 5.4 -645 6
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
182585 15447 3H-5HT 15 Rat Binding pKi = 6.4 6.4 -1 4
NoneNone
PDSP KiDatabase 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 None
CHEMBL12152 15447 3H-5HT 15 Rat Binding pKi = 6.4 6.4 -1 4
NoneNone
PDSP KiDatabase 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 None
2142 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775.0 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 125I-CYP 58 Rat Binding pKi = 5.4 5.4 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4106 2502 125I-ICYP 22 Rat Binding pKi = 7.4 7.4 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-ICYP 22 Rat Binding pKi = 7.4 7.4 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-ICYP 22 Rat Binding pKi = 7.4 7.4 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-ICYP 22 Rat Binding pKi = 7.4 7.4 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 4153 3H-5CT 61 Human Binding pKi = 6.4 6.4 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-5CT 61 Human Binding pKi = 6.4 6.4 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-5CT 61 Human Binding pKi = 6.4 6.4 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-5CT 61 Human Binding pKi = 6.4 6.4 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-5CT 61 Human Binding pKi = 6.4 6.4 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1524 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 3H-GR-125743 96 Human Binding pKi = 5.4 5.4 -2511 52
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Rat Binding pKi = 6.4 6.4 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 3791 125I-CYP 80 Rat Binding pKi = 6.4 6.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-CYP 80 Rat Binding pKi = 6.4 6.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-CYP 80 Rat Binding pKi = 6.4 6.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2543 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
44668 215942 3H-5HT 0 Rat Binding pKi = 5.4 5.4 -1 4
NoneNone
PDSP KiDatabase 228 3 2 1 3.1 C1CNCCC1CCC2=CNC3=CC=CC=C32 None
138107169 215952 3H-5HT 0 Rat Binding pKi = 5.4 5.4 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 3H-5HT 0 Rat Binding pKi = 5.4 5.4 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2543 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 125I-CYP 68 Rat Binding pKi = 6.4 6.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Rat Binding pKi = 7.4 7.4 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 3791 3H-5HT 80 Rat Binding pKi = 7.4 7.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 7.4 7.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 7.4 7.4 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
107 141 125I-ICYP 121 Rat Binding pKi = 7.3 7.3 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 141 125I-ICYP 121 Rat Binding pKi = 7.3 7.3 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 141 125I-ICYP 121 Rat Binding pKi = 7.3 7.3 -30 30
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
152662 215957 3H-5HT 0 Rat Binding pKi = 7.3 7.3 109 7
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
24881687 172814 UNDEFINED 0 Human Binding pKi = 6.3 6.3 -3 2
NoneNone
PDSP KiDatabase 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL451394 172814 UNDEFINED 0 Human Binding pKi = 6.3 6.3 -3 2
NoneNone
PDSP KiDatabase 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 None
138107169 215952 3H-5HT 0 Human Binding pKi = 7.3 7.3 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 3H-5HT 0 Human Binding pKi = 7.3 7.3 -141 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
165193 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
165193 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-CYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2543 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 125I-ICYP 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Rat Binding pKi = 6.3 6.3 -17 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
135 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 3H-5HT 43 Rat Binding pKi = 5.3 5.3 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2176 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-5HT 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
None 216341 3H-GR-125743 0 Human Binding pKi = 6.3 6.3 -630 19
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
277 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 125I-CYP 62 Rat Binding pKi = 5.3 5.3 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2470 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3198 205513 None 76 Rat Binding pKi = 8.3 8.3 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 205513 None 76 Rat Binding pKi = 8.3 8.3 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 205513 None 76 Rat Binding pKi = 8.3 8.3 -44 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
102 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
165193 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
102 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5HT 48 Human Binding pKi = 8.3 8.3 -64 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
165193 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Rat Binding pKi = 8.3 8.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4189 206922 None 96 Rat Binding pKi = 8.3 8.3 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 206922 None 96 Rat Binding pKi = 8.3 8.3 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 206922 None 96 Rat Binding pKi = 8.3 8.3 -41 34
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1884 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440.0 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 2735 3H-GR-125743 58 Human Binding pKi = 8.3 8.3 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
1809 134 3H-5HT 32 Human Binding pKi = 8.3 8.3 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Human Binding pKi = 8.3 8.3 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Human Binding pKi = 8.3 8.3 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 125I-CYP 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 134 3H-5HT 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 125I-CYP 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-5HT 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 125I-CYP 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-5HT 32 Rat Binding pKi = 8.3 8.3 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3036780.0 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 3H-GR-125743 20 Human Binding pKi = 8.3 8.3 -32 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3823 50221 None 42 Rat Binding pKi = 8.3 8.3 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 50221 None 42 Rat Binding pKi = 8.3 8.3 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 50221 None 42 Rat Binding pKi = 8.3 8.3 -38 10
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
5 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
133 2496 3H-5HT 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-5HT 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-5HT 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-5HT 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-5HT 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
132 1275 125I-CYP 13 Rat Binding pKi = 8.3 8.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 125I-CYP 13 Rat Binding pKi = 8.3 8.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 125I-CYP 13 Rat Binding pKi = 8.3 8.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2470 3653 None 50 Rat Binding pKi = 8.3 8.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 None 50 Rat Binding pKi = 8.3 8.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 None 50 Rat Binding pKi = 8.3 8.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 None 50 Rat Binding pKi = 8.3 8.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 None 50 Rat Binding pKi = 8.3 8.3 -43651 59
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 None 43 Rat Binding pKi = 8.3 8.3 -851 58
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.3 8.3 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4595 176715 None 106 Rat Binding pKi = 8.3 8.3 -7 15
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 176715 None 106 Rat Binding pKi = 8.3 8.3 -7 15
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
446220 133521 None 14 Human Binding pKi = 8.3 8.3 -23 45
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 133521 None 14 Human Binding pKi = 8.3 8.3 -23 45
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
133 2496 3H-GR-125743 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-GR-125743 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-GR-125743 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-GR-125743 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-GR-125743 52 Human Binding pKi = 8.3 8.3 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
3117 207841 None 103 Rat Binding pKi = 8.3 8.3 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 207841 None 103 Rat Binding pKi = 8.3 8.3 -3 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4106 2502 3H-GR-125743 22 Human Binding pKi = 8.2 8.2 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-GR-125743 22 Human Binding pKi = 8.2 8.2 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-GR-125743 22 Human Binding pKi = 8.2 8.2 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-GR-125743 22 Human Binding pKi = 8.2 8.2 -11 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1524 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 None 96 Rat Binding pKi = 8.2 8.2 -512 52
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
66265 94013 None 15 Human Binding pKi = 8.2 8.2 -1 19
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 94013 None 15 Human Binding pKi = 8.2 8.2 -1 19
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
2726 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 None 68 Rat Binding pKi = 8.2 8.2 -147 72
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2605 3783 3H-GR-125743 30 Rat Binding pKi = 8.2 8.2 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 3783 3H-GR-125743 30 Rat Binding pKi = 8.2 8.2 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 3783 3H-GR-125743 30 Rat Binding pKi = 8.2 8.2 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 3783 3H-GR-125743 30 Rat Binding pKi = 8.2 8.2 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 3783 3H-GR-125743 30 Rat Binding pKi = 8.2 8.2 -7 10
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
180 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160.0 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 None 56 Rat Binding pKi = 8.2 8.2 -389 40
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2337 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 None 77 Human Binding pKi = 8.2 8.2 -26 62
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2726 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726.0 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 919 None 68 Human Binding pKi = 8.2 8.2 -54 72
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1971 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543.0 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 2866 None 38 Rat Binding pKi = 8.2 8.2 -18 30
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
3191 102858 None 97 Rat Binding pKi = 8.2 8.2 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
3191.0 102858 None 97 Rat Binding pKi = 8.2 8.2 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 102858 None 97 Rat Binding pKi = 8.2 8.2 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
DB11742 102858 None 97 Rat Binding pKi = 8.2 8.2 -17 25
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
6761 67799 None 19 Rat Binding pKi = 8.2 8.2 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 67799 None 19 Rat Binding pKi = 8.2 8.2 -43 18
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
277 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 None 62 Rat Binding pKi = 8.2 8.2 -501 50
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2274 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917.0 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 3173 None 58 Rat Binding pKi = 8.2 8.2 -39 31
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1222 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396.0 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 None 49 Human Binding pKi = 8.2 8.2 -134 33
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4106 2502 3H-5HT 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 3H-5HT 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 3H-5HT 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 3H-5HT 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
102 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 3H-5CT 48 Guinea pig Binding pKi = 7.3 7.3 -125 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3652 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809.0 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 3H-5HT 79 Human Binding pKi = 7.3 7.3 -3 18
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1222 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396.0 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 1664 3H-5HT 49 Rat Binding pKi = 5.3 5.3 -8317 33
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 3H-5HT 93 Rat Binding pKi = 5.3 5.3 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2337 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2435 3590 3H-5CT 83 Human Binding pKi = 6.3 6.3 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 3H-5CT 83 Human Binding pKi = 6.3 6.3 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 3H-5CT 83 Human Binding pKi = 6.3 6.3 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 3H-5CT 83 Human Binding pKi = 6.3 6.3 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 3H-5CT 83 Human Binding pKi = 6.3 6.3 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
7153 98020 3H-5HT 77 Human Binding pKi = 6.3 6.3 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Human Binding pKi = 6.3 6.3 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
68604 78205 125I-CYP 29 Rat Binding pKi = 5.3 5.3 -11748 6
NoneNone
PDSP KiDatabase 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 None
CHEMBL2105437 78205 125I-CYP 29 Rat Binding pKi = 5.3 5.3 -11748 6
NoneNone
PDSP KiDatabase 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 None
135398745 2914 3H-GR-125743 112 Human Binding pKi = 6.3 6.3 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-GR-125743 112 Human Binding pKi = 6.3 6.3 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-GR-125743 112 Human Binding pKi = 6.3 6.3 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-GR-125743 112 Human Binding pKi = 6.3 6.3 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-GR-125743 112 Human Binding pKi = 6.3 6.3 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1574 81 3H-5HT 60 Human Binding pKi = 6.3 6.3 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 3H-5HT 60 Human Binding pKi = 6.3 6.3 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 3H-5HT 60 Human Binding pKi = 6.3 6.3 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2176 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-CYP 68 Rat Binding pKi = 5.3 5.3 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
10257 738 3H-5HT 31 Rat Binding pKi = 7.3 7.3 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 3H-5HT 31 Rat Binding pKi = 7.3 7.3 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 3H-5HT 31 Rat Binding pKi = 7.3 7.3 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 3H-5HT 31 Rat Binding pKi = 7.3 7.3 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
133 2496 3H-5HT 52 Rat Binding pKi = 7.3 7.3 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-5HT 52 Rat Binding pKi = 7.3 7.3 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-5HT 52 Rat Binding pKi = 7.3 7.3 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-5HT 52 Rat Binding pKi = 7.3 7.3 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-5HT 52 Rat Binding pKi = 7.3 7.3 -40 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
103 4153 3H-Alniditan 61 Human Binding pKi = 7.3 7.3 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-Alniditan 61 Human Binding pKi = 7.3 7.3 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-Alniditan 61 Human Binding pKi = 7.3 7.3 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-Alniditan 61 Human Binding pKi = 7.3 7.3 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-Alniditan 61 Human Binding pKi = 7.3 7.3 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3025067 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
4106 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-CYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
134 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Rat Binding pKi = 6.3 6.3 -251 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2435 3590 3H-5HT 83 Rat Binding pKi = 6.3 6.3 -1023 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 3H-5HT 83 Rat Binding pKi = 6.3 6.3 -1023 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 3H-5HT 83 Rat Binding pKi = 6.3 6.3 -1023 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 3H-5HT 83 Rat Binding pKi = 6.3 6.3 -1023 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 3H-5HT 83 Rat Binding pKi = 6.3 6.3 -1023 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1150 3878 3H-5HT 121 Human Binding pKi = 6.3 6.3 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 3H-5HT 121 Human Binding pKi = 6.3 6.3 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 3H-5HT 121 Human Binding pKi = 6.3 6.3 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 3H-5HT 121 Human Binding pKi = 6.3 6.3 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
2389 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-GR-125743 118 Human Binding pKi = 7.3 7.3 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3025067 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 99382 3H-5HT 64 Rat Binding pKi = 7.3 7.3 -2 15
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
2470 3653 125I-CYP 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 125I-CYP 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 125I-CYP 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 125I-CYP 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 125I-CYP 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 3H-5HT 50 Rat Binding pKi = 5.3 5.3 -43651 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
115 3791 125I-ICYP 80 Rat Binding pKi = 7.3 7.3 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-ICYP 80 Rat Binding pKi = 7.3 7.3 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-ICYP 80 Rat Binding pKi = 7.3 7.3 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2337 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002.0 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 3256 3H-5HT 77 Rat Binding pKi = 5.3 5.3 -575 62
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
18971832 2418 3H-5HT 0 Human Binding pKi = 6.3 6.3 -85 13
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 2418 3H-5HT 0 Human Binding pKi = 6.3 6.3 -85 13
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 2418 3H-5HT 0 Human Binding pKi = 6.3 6.3 -85 13
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
3036780.0 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 3H-5HT 20 Rat Binding pKi = 7.3 7.3 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
4106 2502 125I-ICYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-ICYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-ICYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-ICYP 22 Rat Binding pKi = 7.3 7.3 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
132 1275 125I-CYP 13 Rat Binding pKi = 7.3 7.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 1275 125I-CYP 13 Rat Binding pKi = 7.3 7.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 1275 125I-CYP 13 Rat Binding pKi = 7.3 7.3 -54 15
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2303 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 3H-5HT 68 Human Binding pKi = 7.3 7.3 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
165193 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-ICYP 0 Rat Binding pKi = 7.3 7.3 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
283 3130 125I-CYP 57 Rat Binding pKi = 5.3 5.3 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3130 125I-CYP 57 Rat Binding pKi = 5.3 5.3 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3130 125I-CYP 57 Rat Binding pKi = 5.3 5.3 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
165193 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-ICYP 0 Rat Binding pKi = 7.2 7.2 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
5074 3332 125I-ICYP 80 Rat Binding pKi = 6.2 6.2 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 3332 125I-ICYP 80 Rat Binding pKi = 6.2 6.2 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 3332 125I-ICYP 80 Rat Binding pKi = 6.2 6.2 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 3332 125I-ICYP 80 Rat Binding pKi = 6.2 6.2 -4168 30
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5475158 67213 125I-CYP 25 Rat Binding pKi = 5.2 5.2 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 67213 125I-CYP 25 Rat Binding pKi = 5.2 5.2 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
2865 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 3H-5CT 73 Human Binding pKi = 7.2 7.2 -12 53
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2176 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-ICYP 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2176 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-ICYP 68 Rat Binding pKi = 5.2 5.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1809 134 3H-GR-125743 32 Human Binding pKi = 8.2 8.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 3H-GR-125743 32 Human Binding pKi = 8.2 8.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 3H-GR-125743 32 Human Binding pKi = 8.2 8.2 -15 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107780 1844 3H-GR-125743 54 Rat Binding pKi = 8.2 8.2 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 3H-GR-125743 54 Rat Binding pKi = 8.2 8.2 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 3H-GR-125743 54 Rat Binding pKi = 8.2 8.2 -4 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1212 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372.0 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 None 50 Rat Binding pKi = 8.2 8.2 -144 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2351 3286 None 64 Rat Binding pKi = 8.2 8.2 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 3286 None 64 Rat Binding pKi = 8.2 8.2 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 3286 None 64 Rat Binding pKi = 8.2 8.2 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 3286 None 64 Rat Binding pKi = 8.2 8.2 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 3286 None 64 Rat Binding pKi = 8.2 8.2 -10 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
213 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533.0 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 3853 None 55 Rat Binding pKi = 8.2 8.2 -6 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
242 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 None 124 Human Binding pKi = 8.2 8.2 -380 51
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
49831411 217746 None 0 Human Binding pKi = 8.2 8.2 1 15
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
2247 505 None 81 Rat Binding pKi = 8.2 8.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 505 None 81 Rat Binding pKi = 8.2 8.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 505 None 81 Rat Binding pKi = 8.2 8.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 505 None 81 Rat Binding pKi = 8.2 8.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 505 None 81 Rat Binding pKi = 8.2 8.2 -35 42
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
135398737 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 None 93 Human Binding pKi = 8.2 8.2 -151 89
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2181 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830.0 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 3128 None 46 Human Binding pKi = 8.2 8.2 -70 35
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2303 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 None 68 Human Binding pKi = 8.2 8.2 -1174 26
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
2585 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
2585.0 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 803 None 103 Rat Binding pKi = 8.2 8.2 -100 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
135398745 2914 None 112 Human Binding pKi = 8.2 8.2 -199 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 None 112 Human Binding pKi = 8.2 8.2 -199 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 None 112 Human Binding pKi = 8.2 8.2 -199 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 None 112 Human Binding pKi = 8.2 8.2 -199 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 None 112 Human Binding pKi = 8.2 8.2 -199 65
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
37 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746.0 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 778 None 60 Human Binding pKi = 8.2 8.2 -22 17
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
135398745 2914 None 112 Rat Binding pKi = 8.2 8.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 None 112 Rat Binding pKi = 8.2 8.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 None 112 Rat Binding pKi = 8.2 8.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 None 112 Rat Binding pKi = 8.2 8.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 None 112 Rat Binding pKi = 8.2 8.2 -162 65
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1613 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964.0 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 2348 None 53 Human Binding pKi = 8.2 8.2 -13 44
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1212 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372.0 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 1662 None 50 Human Binding pKi = 8.2 8.2 -93 65
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 217711 None 0 Human Binding pKi = 8.2 8.2 -1 26
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
31101 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101.0 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 None 40 Human Binding pKi = 8.2 8.2 -128 36
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1353 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 None 93 Human Binding pKi = 8.2 8.2 -66 83
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2601 3780 None 33 Human Binding pKi = 8.2 8.2 -87 21
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 3780 None 33 Human Binding pKi = 8.2 8.2 -87 21
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 3780 None 33 Human Binding pKi = 8.2 8.2 -87 21
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 3780 None 33 Human Binding pKi = 8.2 8.2 -87 21
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 3780 None 33 Human Binding pKi = 8.2 8.2 -87 21
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1621 2429 3H-5HT 17 Rat Binding pKi = 8.2 8.2 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 2429 3H-5HT 17 Rat Binding pKi = 8.2 8.2 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 2429 3H-5HT 17 Rat Binding pKi = 8.2 8.2 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 2429 3H-5HT 17 Rat Binding pKi = 8.2 8.2 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 2429 3H-5HT 17 Rat Binding pKi = 8.2 8.2 -97 45
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
26987 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
26987.0 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 949 None 33 Rat Binding pKi = 8.2 8.2 -138 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
212 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651.0 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 3806 None 47 Human Binding pKi = 8.2 8.2 -6 25
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2393 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
5078 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
5078.0 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
51 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
CHEMBL905 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
DB00953 3334 None 82 Human Binding pKi = 8.2 8.2 -1 5
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
130 3500 35S-GTPGammaS 47 Human Binding pKi = 8.2 8.2 -1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 3500 35S-GTPGammaS 47 Human Binding pKi = 8.2 8.2 -1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 3500 35S-GTPGammaS 47 Human Binding pKi = 8.2 8.2 -1 13
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
100 3805 None 58 Human Binding pKi = 8.2 8.2 -13 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 3805 None 58 Human Binding pKi = 8.2 8.2 -13 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 3805 None 58 Human Binding pKi = 8.2 8.2 -13 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 3805 None 58 Human Binding pKi = 8.2 8.2 -13 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 3805 None 58 Human Binding pKi = 8.2 8.2 -13 55
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
134 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 None 24 Rat Binding pKi = 8.2 8.2 -251 67
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2435 3590 3H-Alniditan 83 Human Binding pKi = 7.2 7.2 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 3H-Alniditan 83 Human Binding pKi = 7.2 7.2 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 3H-Alniditan 83 Human Binding pKi = 7.2 7.2 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 3H-Alniditan 83 Human Binding pKi = 7.2 7.2 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 3H-Alniditan 83 Human Binding pKi = 7.2 7.2 -128 48
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2543 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-GR-125743 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 3791 3H-5HT 80 Rat Binding pKi = 7.2 7.2 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Rat Binding pKi = 7.2 7.2 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Rat Binding pKi = 7.2 7.2 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
182595 19937 3H-5HT 14 Rat Binding pKi = 6.2 6.2 -1000 4
NoneNone
PDSP KiDatabase 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
CHEMBL130276 19937 3H-5HT 14 Rat Binding pKi = 6.2 6.2 -1000 4
NoneNone
PDSP KiDatabase 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
1220 187 125I-CYP 55 Rat Binding pKi = 5.2 5.2 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 125I-CYP 55 Rat Binding pKi = 5.2 5.2 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 125I-CYP 55 Rat Binding pKi = 5.2 5.2 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 125I-CYP 55 Rat Binding pKi = 5.2 5.2 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3151 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
3151.0 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 1462 125I-CYP 97 Rat Binding pKi = 5.2 5.2 -7762 27
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
2176 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-5HT 68 Rat Binding pKi = 7.2 7.2 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2543 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 7.2 7.2 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1209 1658 3H-5HT 75 Rat Binding pKi = 5.2 5.2 -1148 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 1658 3H-5HT 75 Rat Binding pKi = 5.2 5.2 -1148 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 1658 3H-5HT 75 Rat Binding pKi = 5.2 5.2 -1148 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 1658 3H-5HT 75 Rat Binding pKi = 5.2 5.2 -1148 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 1658 3H-5HT 75 Rat Binding pKi = 5.2 5.2 -1148 32
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
None 215971 3H-8-OH-DPAT 0 Human Binding pKi = 6.2 6.2 -1348 15
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
135 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 125I-CYP 43 Rat Binding pKi = 5.2 5.2 -851 58
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
21163 215930 125I-CYP 0 Rat Binding pKi = 5.2 5.2 -4 5
NoneNone
PDSP KiDatabase 192 2 4 3 1.1 C1=C2C(=CC(=C1O)O)NC=C2CCN None
5475158 67213 3H-5HT 25 Rat Binding pKi = 5.2 5.2 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 67213 3H-5HT 25 Rat Binding pKi = 5.2 5.2 -1023 14
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
2176 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 3H-5HT 68 Mouse Binding pKi = 7.2 7.2 -199 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1220 187 3H-5HT 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
206 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
2303 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 3H-5HT 68 Human Binding pKi = 6.2 6.2 -1174 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
138107169 215952 125I-ICYP 0 Rat Binding pKi = 5.2 5.2 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 125I-ICYP 0 Rat Binding pKi = 5.2 5.2 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 216214 3H-5HT 0 Human Binding pKi = 5.2 5.2 -588 14
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
88747 204478 125I-CYP 128 Rat Binding pKi = 5.2 5.2 -4 5
NoneNone
PDSP KiDatabase 164 1 1 4 -0.1 c1cnc(N2CCNCC2)nc1 None
CHEMBL724 204478 125I-CYP 128 Rat Binding pKi = 5.2 5.2 -4 5
NoneNone
PDSP KiDatabase 164 1 1 4 -0.1 c1cnc(N2CCNCC2)nc1 None
115 3791 3H-5HT 80 Human Binding pKi = 7.2 7.2 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 3H-5HT 80 Human Binding pKi = 7.2 7.2 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 3H-5HT 80 Human Binding pKi = 7.2 7.2 -2 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
71299720 215951 3H-GR-125743 0 Guinea pig Binding pKi = 7.2 7.2 -51 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
127 3126 125I-CYP 52 Rat Binding pKi = 7.2 7.2 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 125I-CYP 52 Rat Binding pKi = 7.2 7.2 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 125I-CYP 52 Rat Binding pKi = 7.2 7.2 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
206 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 2493 3H-5HT 16 Human Binding pKi = 6.2 6.2 -549 25
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
165193 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5HT 0 Human Binding pKi = 6.2 6.2 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
21830793 91835 3H-8-OH-DPAT 10 Bovine Binding pKi = 6.2 6.2 -4265 45
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 91835 3H-8-OH-DPAT 10 Bovine Binding pKi = 6.2 6.2 -4265 45
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
135398737 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
135398737.0 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 958 3H-Alniditan 93 Human Binding pKi = 6.2 6.2 -151 89
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
71299720 215951 3H-GR-125743 0 Rat Binding pKi = 7.2 7.2 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
135398745 2914 3H-Alniditan 112 Human Binding pKi = 6.2 6.2 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
135398745.0 2914 3H-Alniditan 112 Human Binding pKi = 6.2 6.2 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 2914 3H-Alniditan 112 Human Binding pKi = 6.2 6.2 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 2914 3H-Alniditan 112 Human Binding pKi = 6.2 6.2 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 2914 3H-Alniditan 112 Human Binding pKi = 6.2 6.2 -199 65
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
283 3130 3H-5HT 57 Rat Binding pKi = 5.2 5.2 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 3130 3H-5HT 57 Rat Binding pKi = 5.2 5.2 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 3130 3H-5HT 57 Rat Binding pKi = 5.2 5.2 -6606 12
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
103 4153 3H-GR-125743 61 Human Binding pKi = 7.2 7.2 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-GR-125743 61 Human Binding pKi = 7.2 7.2 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-GR-125743 61 Human Binding pKi = 7.2 7.2 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-GR-125743 61 Human Binding pKi = 7.2 7.2 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-GR-125743 61 Human Binding pKi = 7.2 7.2 -48 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3036780.0 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 3H-5HT 20 Rat Binding pKi = 7.2 7.2 -363 53
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 215939 3H-5HT 0 Rat Binding pKi = 6.2 6.2 -218 6
NoneNone
PDSP KiDatabase 370 6 2 7 2.1 CC(C1=CC=CC2=NC3=C(C=CC=C3N=C21)C(=O)O)OC(=O)C(CO)OC None
6917970 3691 3H-GR-125743 61 Human Binding pKi = 5.2 5.2 -1584 34
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 3691 3H-GR-125743 61 Human Binding pKi = 5.2 5.2 -1584 34
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 3691 3H-GR-125743 61 Human Binding pKi = 5.2 5.2 -1584 34
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
3294 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360.0 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 None 111 Human Binding pKi = 8.2 8.2 -57 45
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2176 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 None 68 Rat Binding pKi = 8.2 8.2 -741 27
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2176 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 None 68 Human Binding pKi = 8.2 8.2 -1737 27
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
133 2496 None 52 Human Binding pKi = 8.1 8.1 -23 42
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 None 52 Human Binding pKi = 8.1 8.1 -23 42
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 None 52 Human Binding pKi = 8.1 8.1 -23 42
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 None 52 Human Binding pKi = 8.1 8.1 -23 42
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 None 52 Human Binding pKi = 8.1 8.1 -23 42
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
103 4153 None 61 Human Binding pKi = 8.1 8.1 -48 53
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 None 61 Human Binding pKi = 8.1 8.1 -48 53
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 None 61 Human Binding pKi = 8.1 8.1 -48 53
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 None 61 Human Binding pKi = 8.1 8.1 -48 53
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 None 61 Human Binding pKi = 8.1 8.1 -48 53
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1809 134 125I-ICYP 32 Rat Binding pKi = 8.1 8.1 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 134 125I-ICYP 32 Rat Binding pKi = 8.1 8.1 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 134 125I-ICYP 32 Rat Binding pKi = 8.1 8.1 -32 36
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2435 3590 None 83 Human Binding pKi = 8.1 8.1 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 3590 None 83 Human Binding pKi = 8.1 8.1 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 3590 None 83 Human Binding pKi = 8.1 8.1 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 3590 None 83 Human Binding pKi = 8.1 8.1 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 3590 None 83 Human Binding pKi = 8.1 8.1 -128 48
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2303 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 None 68 Rat Binding pKi = 8.1 8.1 -57 26
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
3652 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809.0 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 4097 None 79 Human Binding pKi = 8.1 8.1 -3 18
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
31101 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
31101.0 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 729 None 40 Rat Binding pKi = 8.1 8.1 -48 36
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
2105 3054 None 37 Rat Binding pKi = 8.1 8.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 3054 None 37 Rat Binding pKi = 8.1 8.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 3054 None 37 Rat Binding pKi = 8.1 8.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 3054 None 37 Rat Binding pKi = 8.1 8.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 3054 None 37 Rat Binding pKi = 8.1 8.1 -27 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1342 35 3H-5HT 49 Human Binding pKi = 8.1 8.1 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 35 3H-5HT 49 Human Binding pKi = 8.1 8.1 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 35 3H-5HT 49 Human Binding pKi = 8.1 8.1 -4 19
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
71299720 215951 3H-5HT 0 Rat Binding pKi = 8.1 8.1 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
71299720 215951 3H-5HT 0 Rat Binding pKi = 8.1 8.1 -44 17
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
4806 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
71768094.0 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051.0 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 4008 None 88 Human Binding pKi = 8.1 8.1 -2 13
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2389 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 None 118 Human Binding pKi = 8.1 8.1 -93 67
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11978813 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
11978813.0 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 721 None 79 Human Binding pKi = 8.1 8.1 -9 24
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
135 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 None 43 Human Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
134 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 3H-5HT 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
133 2496 None 52 Rat Binding pKi = 8.1 8.1 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 None 52 Rat Binding pKi = 8.1 8.1 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 None 52 Rat Binding pKi = 8.1 8.1 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 None 52 Rat Binding pKi = 8.1 8.1 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 None 52 Rat Binding pKi = 8.1 8.1 -40 42
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681.0 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 2514 None 24 Human Binding pKi = 8.1 8.1 -14 67
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
102 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 None 48 Human Binding pKi = 8.1 8.1 -64 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5 139 3H-5HT 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-5HT 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-5HT 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-5HT 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2543 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 None 68 Rat Binding pKi = 8.1 8.1 -17 32
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 55585 None 119 Human Binding pKi = 8.1 8.1 -93 54
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
115237.0 55585 None 119 Human Binding pKi = 8.1 8.1 -93 54
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 55585 None 119 Human Binding pKi = 8.1 8.1 -93 54
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 55585 None 119 Human Binding pKi = 8.1 8.1 -93 54
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1588 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864.0 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 None 27 Human Binding pKi = 8.1 8.1 -42 44
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2869 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60857 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60857.0 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
CHEMBL1185 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
DB00315 4152 None 89 Human Binding pKi = 8.1 8.1 -8 7
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
2543 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.1 8.1 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2477 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477.0 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 745 None 59 Rat Binding pKi = 8.1 8.1 -16 29
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
3658 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709.0 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 4107 None 53 Human Binding pKi = 8.1 8.1 -4 8
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5 139 35S-GTPGammaS 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 35S-GTPGammaS 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 35S-GTPGammaS 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 35S-GTPGammaS 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107780 1844 35S-GTPGammaS 54 Human Binding pKi = 8.1 8.1 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 1844 35S-GTPGammaS 54 Human Binding pKi = 8.1 8.1 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 1844 35S-GTPGammaS 54 Human Binding pKi = 8.1 8.1 1 17
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
28 3496 35S-GTPGammaS 46 Human Binding pKi = 8.1 8.1 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 3496 35S-GTPGammaS 46 Human Binding pKi = 8.1 8.1 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 3496 35S-GTPGammaS 46 Human Binding pKi = 8.1 8.1 13 10
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107715 200945 None 22 Rat Binding pKi = 8.1 8.1 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 200945 None 22 Rat Binding pKi = 8.1 8.1 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 200945 None 22 Rat Binding pKi = 8.1 8.1 -22 19
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
1251 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
7191 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
77992 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
77992.0 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
CHEMBL1279 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
DB00998 1692 None 30 Human Binding pKi = 8.1 8.1 -1 3
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
186 1807 3H-GR-125743 52 Rat Binding pKi = 7.2 7.2 -11 17
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 1807 3H-GR-125743 52 Rat Binding pKi = 7.2 7.2 -11 17
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 1807 3H-GR-125743 52 Rat Binding pKi = 7.2 7.2 -11 17
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
137 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 370 125I-ICYP 52 Rat Binding pKi = 7.2 7.2 -154 12
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
1220 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
21138 98451 125I-ICYP 39 Rat Binding pKi = 5.2 5.2 -162 7
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
CHEMBL275742 98451 125I-ICYP 39 Rat Binding pKi = 5.2 5.2 -162 7
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
1220 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-GR-125743 55 Human Binding pKi = 6.2 6.2 -208 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
2389 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-5CT 118 Human Binding pKi = 6.1 6.1 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 216239 3H-GR-125743 0 Human Binding pKi = 6.1 6.1 -4677 30
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
1220 187 3H-5HT 55 Rat Binding pKi = 5.1 5.1 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 187 3H-5HT 55 Rat Binding pKi = 5.1 5.1 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 187 3H-5HT 55 Rat Binding pKi = 5.1 5.1 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 187 3H-5HT 55 Rat Binding pKi = 5.1 5.1 -7413 44
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
145 140 3H-5-CT 49 Human Binding pKi = 7.1 7.1 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 140 3H-5-CT 49 Human Binding pKi = 7.1 7.1 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 140 3H-5-CT 49 Human Binding pKi = 7.1 7.1 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 140 3H-5-CT 49 Human Binding pKi = 7.1 7.1 -8 30
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
165193 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-ICYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
102 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 125I-ICYP 48 Rat Binding pKi = 5.1 5.1 -2691 49
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
127 3126 3H-5HT 52 Rat Binding pKi = 7.1 7.1 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 3126 3H-5HT 52 Rat Binding pKi = 7.1 7.1 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 3126 3H-5HT 52 Rat Binding pKi = 7.1 7.1 -95 15
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
2303 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 3187 125I-ICYP 68 Rat Binding pKi = 7.1 7.1 -57 26
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
24882193 188649 UNDEFINED 0 Human Binding pKi = 7.1 7.1 -263 2
NoneNone
PDSP KiDatabase 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL503468 188649 UNDEFINED 0 Human Binding pKi = 7.1 7.1 -263 2
NoneNone
PDSP KiDatabase 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
4209 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893.0 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 3163 125I-CYP 75 Rat Binding pKi = 5.1 5.1 -9549 33
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
123606 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
123606.0 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
128 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
7110 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
CHEMBL1505 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
DB00918 352 None 70 Human Binding pKi = 8.1 8.1 -1 3
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
150 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226.0 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 2509 None 21 Rat Binding pKi = 8.1 8.1 -6 16
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
2543 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 None 68 Western lowland gorilla Binding pKi = 8.1 8.1 -2 32
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 None 68 Human Binding pKi = 8.1 8.1 -3 32
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
134551 358 None 27 Rat Binding pKi = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 358 None 27 Rat Binding pKi = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 358 None 27 Rat Binding pKi = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 358 None 27 Rat Binding pKi = 8.1 8.1 -5 21
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
1524 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822.0 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 2181 None 96 Mouse Binding pKi = 8.1 8.1 -4 52
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
135 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184.0 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 2532 None 43 Mouse Binding pKi = 8.1 8.1 -3 58
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2470 3653 None 50 Mouse Binding pKi = 8.1 8.1 -194 59
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 None 50 Mouse Binding pKi = 8.1 8.1 -194 59
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 None 50 Mouse Binding pKi = 8.1 8.1 -194 59
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 None 50 Mouse Binding pKi = 8.1 8.1 -194 59
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 None 50 Mouse Binding pKi = 8.1 8.1 -194 59
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
102 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969.0 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 4127 None 48 Mouse Binding pKi = 8.1 8.1 -186 49
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2865 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854.0 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 4143 None 73 Human Binding pKi = 8.1 8.1 -12 53
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1588 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864.0 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 2325 None 27 Rat Binding pKi = 8.1 8.1 -58 44
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3036780.0 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970.0 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 107531 None 20 Human Binding pKi = 8.1 8.1 -32 53
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1884 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440.0 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
11954224 215953 None 0 Human Binding pKi = 8.1 8.1 -32 58
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
3251.0 215953 None 0 Human Binding pKi = 8.1 8.1 -32 58
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
CHEMBL1982133 215953 None 0 Human Binding pKi = 8.1 8.1 -32 58
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
DB00696 215953 None 0 Human Binding pKi = 8.1 8.1 -32 58
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1042 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884.0 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 1581 None 23 Rat Binding pKi = 8.1 8.1 -5 17
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
151 2416 UNDEFINED 44 Human Binding pKi = 7.1 7.1 -89 4
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
20 2416 UNDEFINED 44 Human Binding pKi = 7.1 7.1 -89 4
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
5311258 2416 UNDEFINED 44 Human Binding pKi = 7.1 7.1 -89 4
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
CHEMBL101690 2416 UNDEFINED 44 Human Binding pKi = 7.1 7.1 -89 4
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
242 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
155 728 3H-5HT 25 Rat Binding pKi = 6.1 6.1 -263 13
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 728 3H-5HT 25 Rat Binding pKi = 6.1 6.1 -263 13
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 728 3H-5HT 25 Rat Binding pKi = 6.1 6.1 -263 13
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 728 3H-5HT 25 Rat Binding pKi = 6.1 6.1 -263 13
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 728 3H-5HT 25 Rat Binding pKi = 6.1 6.1 -263 13
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
104911 216019 3H-8-OH-DPAT 0 Human Binding pKi = 5.1 5.1 -38018 37
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
119570 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570.0 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 3H-GR-125743 96 Human Binding pKi = 5.1 5.1 -660 40
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
242 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795.0 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 470 3H-GR-125743 124 Human Binding pKi = 6.1 6.1 -380 51
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
115 3791 125I-ICYP 80 Rat Binding pKi = 7.1 7.1 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 3791 125I-ICYP 80 Rat Binding pKi = 7.1 7.1 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 3791 125I-ICYP 80 Rat Binding pKi = 7.1 7.1 1 27
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
180 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160.0 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 401 3H-5HT 56 Rat Binding pKi = 6.1 6.1 -389 40
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
277 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913.0 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 1301 3H-5HT 62 Rat Binding pKi = 6.1 6.1 -501 50
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
62787 206188 3H-5HT 21 Rat Binding pKi = 5.1 5.1 -85 10
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 206188 3H-5HT 21 Rat Binding pKi = 5.1 5.1 -85 10
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
165193 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 3H-5-CT 0 Human Binding pKi = 7.1 7.1 -1000 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
165193 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4946.0 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
CHEMBL27 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
DB00571 215945 125I-CYP 0 Rat Binding pKi = 7.1 7.1 -154 30
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
1574 81 3H-5HT 60 Human Binding pKi = 6.1 6.1 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 3H-5HT 60 Human Binding pKi = 6.1 6.1 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 3H-5HT 60 Human Binding pKi = 6.1 6.1 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1150 3878 3H-5HT 121 Human Binding pKi = 7.1 7.1 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 3878 3H-5HT 121 Human Binding pKi = 7.1 7.1 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 3878 3H-5HT 121 Human Binding pKi = 7.1 7.1 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 3878 3H-5HT 121 Human Binding pKi = 7.1 7.1 -7 25
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
2142 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775.0 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 3096 125I-ICYP 58 Rat Binding pKi = 6.1 6.1 -741 36
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
138107169 215952 125I-ICYP 0 Rat Binding pKi = 5.1 5.1 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 215952 125I-ICYP 0 Rat Binding pKi = 5.1 5.1 -19054 22
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
1353 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559.0 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 1911 125I-CYP 93 Rat Binding pKi = 5.1 5.1 -5248 83
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360.0 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 3H-5HT 111 Human Binding pKi = 7.1 7.1 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
7153 98020 3H-5HT 77 Human Binding pKi = 7.1 7.1 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Human Binding pKi = 7.1 7.1 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5 139 3H-GR-125743 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 139 125I-ICYP 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 3H-GR-125743 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 139 125I-ICYP 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 3H-GR-125743 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 139 125I-ICYP 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 3H-GR-125743 72 Human Binding pKi = 8.1 8.1 -11 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 139 125I-ICYP 72 Rat Binding pKi = 8.1 8.1 -13 54
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
124 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 None 47 Rat Binding pKi = 8.0 8.0 -2 33
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2543 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 UNDEFINED 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
10531 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
10531.0 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
121 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
888 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
CHEMBL1732 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
DB00320 1420 None 21 Human Binding pKi = 8.0 8.0 -12 23
NoneNone
Drug Central 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 None
2543 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358.0 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 3707 3H-5HT 68 Human Binding pKi = 8.0 8.0 -3 32
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
133 2496 3H-GR-125743 52 Human Binding pKi = 8.0 8.0 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 2496 3H-GR-125743 52 Human Binding pKi = 8.0 8.0 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 2496 3H-GR-125743 52 Human Binding pKi = 8.0 8.0 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 2496 3H-GR-125743 52 Human Binding pKi = 8.0 8.0 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 2496 3H-GR-125743 52 Human Binding pKi = 8.0 8.0 -23 42
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1884 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440.0 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 2735 3H-GR-125743 58 Human Binding pKi = 8.0 8.0 -3 5
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
10531 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
10531.0 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
121 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
888 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
CHEMBL1732 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
DB00320 1420 None 21 Rat Binding pKi = 8.0 8.0 -5 23
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 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 None
124 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636.0 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 2981 None 47 Human Binding pKi = 8.0 8.0 1 33
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2389 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073.0 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 3331 3H-Alniditan 118 Human Binding pKi = 8.0 8.0 -93 67
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
7153 98020 3H-5HT 77 Human Binding pKi = 7.1 7.1 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 3H-5HT 77 Human Binding pKi = 7.1 7.1 -11 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
10257 738 125I-CYP 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
10257 738 3H-5HT 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 125I-CYP 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 738 3H-5HT 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 125I-CYP 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 738 3H-5HT 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 125I-CYP 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 738 3H-5HT 31 Rat Binding pKi = 6.0 6.0 -141 19
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
None 216135 3H-GR-125743 0 Rat Binding pKi = 6.0 6.0 -3162 24
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
1574 81 3H-5HT 60 Human Binding pKi = 6.0 6.0 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 81 3H-5HT 60 Human Binding pKi = 6.0 6.0 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 81 3H-5HT 60 Human Binding pKi = 6.0 6.0 -8 21
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2176 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828.0 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 3127 125I-CYP 68 Rat Binding pKi = 5.0 5.0 -741 27
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
107992 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
3012003 216145 3H-5HT 0 Rat Binding pKi = 5.0 5.0 -371 12
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
107992 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 2553 125I-CYP 49 Rat Binding pKi = 5.0 5.0 -12 10
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
103 4153 3H-5HT 61 Rat Binding pKi = 6.0 6.0 -776 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 4153 3H-5HT 61 Rat Binding pKi = 6.0 6.0 -776 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 4153 3H-5HT 61 Rat Binding pKi = 6.0 6.0 -776 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 4153 3H-5HT 61 Rat Binding pKi = 6.0 6.0 -776 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 4153 3H-5HT 61 Rat Binding pKi = 6.0 6.0 -776 53
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
4106 2502 125I-ICYP 22 Rat Binding pKi = 7.0 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 2502 125I-ICYP 22 Rat Binding pKi = 7.0 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 2502 125I-ICYP 22 Rat Binding pKi = 7.0 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 2502 125I-ICYP 22 Rat Binding pKi = 7.0 7.0 -102 34
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
7153 98020 125I-ICYP 77 Rat Binding pKi = 7.0 7.0 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 98020 125I-ICYP 77 Rat Binding pKi = 7.0 7.0 -10 34
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
3294 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360.0 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 2006 3H-5CT 111 Human Binding pKi = 7 7.0 -57 45
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 3653 3H-5HT 50 Human Binding pKi = 6 6.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 3653 3H-5HT 50 Human Binding pKi = 6 6.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 3653 3H-5HT 50 Human Binding pKi = 6 6.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 3653 3H-5HT 50 Human Binding pKi = 6 6.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 3653 3H-5HT 50 Human Binding pKi = 6 6.0 -95499 59
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2393 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
5078 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
5078.0 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
51 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
CHEMBL905 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
DB00953 3334 None 82 Human Binding pKi = 6.9 6.9 -1 5
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
2389 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
2389 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
2389 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
5073 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
5073 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
5073 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
5073.0 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
5073.0 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
5073.0 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
96 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
96 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
96 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
CHEMBL85 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
CHEMBL85 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
CHEMBL85 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
DB00734 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
DB00734 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
DB00734 3331 None 118 Human Binding pKi = 7.0 7.0 -93 67
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
2543 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
5358 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
5358.0 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
54 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
CHEMBL128 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
DB00669 3707 None 68 Human Binding pKi = 7.3 7.3 -3 32
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
10446 530 None 0 Rat Binding pKi = 7.4 7.4 -8 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
133081 530 None 0 Rat Binding pKi = 7.4 7.4 -8 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
CHEMBL2110755 530 None 0 Rat Binding pKi = 7.4 7.4 -8 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
4806 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
71768094.0 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051.0 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 4008 None 88 Human Binding pKi = 7.5 7.5 -2 13
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
113 1852 None 14 Human Binding pKi = 7.5 7.5 39 3
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
128018 1852 None 14 Human Binding pKi = 7.5 7.5 39 3
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
CHEMBL119264 1852 None 14 Human Binding pKi = 7.5 7.5 39 3
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
10446 530 None 0 Human Binding pKi = 7.7 7.7 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
133081 530 None 0 Human Binding pKi = 7.7 7.7 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
CHEMBL2110755 530 None 0 Human Binding pKi = 7.7 7.7 -4 4
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
2869 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
60 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
60857 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
60857.0 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
CHEMBL1185 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
DB00315 4152 None 89 Human Binding pKi = 7.7 7.7 -8 7
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
1251 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
7191 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
77992 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
77992.0 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
CHEMBL1279 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
DB00998 1692 None 30 Human Binding pKi = 8.0 8.0 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
40 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
77993 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
77993.0 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
995 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
CHEMBL1510 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
DB00216 1547 None 58 Human Binding pKi = 8 8.0 -2 5
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
5 139 None 72 Mouse Binding pKi = 8.1 8.1 -41 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
5202 139 None 72 Mouse Binding pKi = 8.1 8.1 -41 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
CHEMBL39 139 None 72 Mouse Binding pKi = 8.1 8.1 -41 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
DB08839 139 None 72 Mouse Binding pKi = 8.1 8.1 -41 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
1884 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
4440 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
4440.0 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
45 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
CHEMBL1278 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
DB00952 2735 None 58 Human Binding pKi = 8.1 8.1 -3 5
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
5 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
5202 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
CHEMBL39 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
DB08839 139 None 72 Human Binding pKi = 8.2 8.2 -11 54
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
3231 3505 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
5311426 3505 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
CHEMBL1628625 3505 None 0 Human Binding pKi = 8.2 8.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
130 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
130 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
130 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
3378093 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
3378093 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
3378093 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
CHEMBL281350 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
CHEMBL281350 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
CHEMBL281350 3500 None 47 Human Binding pKi = 8.4 8.4 -1 13
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
3221 1188 None 0 Human Binding pKi = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
4029677 1188 None 0 Human Binding pKi = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
CHEMBL1570196 1188 None 0 Human Binding pKi = 8.7 8.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
132059 2235 None 57 Human Binding pKi = 9.2 9.2 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
15 2235 None 57 Human Binding pKi = 9.2 9.2 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
CHEMBL39317 2235 None 57 Human Binding pKi = 9.2 9.2 -1 3
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
202 1508 None 77 Human Binding pKi None 8.3 8.3 -1 30
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 1508 None 77 Human Binding pKi None 8.3 8.3 -1 30
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 1508 None 77 Human Binding pKi None 8.3 8.3 -1 30
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 1508 None 77 Human Binding pKi None 8.3 8.3 -1 30
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 1508 None 77 Human Binding pKi None 8.3 8.3 -1 30
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
119570 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
119570.0 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 3159 None 96 Human Binding pKi None 8.3 8.3 -660 40
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
228 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005.0 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 445 None 28 Human Binding pKi None 8.3 8.3 1 24
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
3337 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
3337.0 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 206367 None 27 Human Binding pKi None 8.2 8.2 -74 40
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
179 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159.0 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 400 None 115 Human Binding pKi None 8.2 8.2 -43 49
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2995 204405 None 53 Human Binding pKi None 8.2 8.2 -3 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
2995.0 204405 None 53 Human Binding pKi None 8.2 8.2 -3 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 204405 None 53 Human Binding pKi None 8.2 8.2 -3 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 204405 None 53 Human Binding pKi None 8.2 8.2 -3 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 204405 None 53 Human Binding pKi None 8.2 8.2 -3 23
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
29 792 None 0 Human Binding pKi None 5.3 5.3 -7943 9
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 792 None 0 Human Binding pKi None 5.3 5.3 -7943 9
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 792 None 0 Human Binding pKi None 5.3 5.3 -7943 9
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
126 4070 None 8 Human Binding pKi None 5.8 5.8 -1258 5
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
6604840 4070 None 8 Human Binding pKi None 5.8 5.8 -1258 5
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
CHEMBL38288 4070 None 8 Human Binding pKi None 5.8 5.8 -1258 5
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
219050 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
219050 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
52 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
CHEMBL431367 3373 None 25 Human Binding pKi None 5.9 5.9 -7762 21
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
1574 81 None 60 Human Binding pKi None 6.1 6.1 -8 21
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
218 81 None 60 Human Binding pKi None 6.1 6.1 -8 21
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
CHEMBL266591 81 None 60 Human Binding pKi None 6.1 6.1 -8 21
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
242 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
34 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
60795 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
60795.0 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
CHEMBL1112 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
DB01238 470 None 124 Human Binding pKi None 6.1 6.1 -380 51
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
10 723 None 28 Human Binding pKi None 6.1 6.1 -63 9
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 723 None 28 Human Binding pKi None 6.1 6.1 -63 9
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 723 None 28 Human Binding pKi None 6.1 6.1 -63 9
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
65 2070 None 0 Human Binding pKi None 6.1 6.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
9995893 2070 None 0 Human Binding pKi None 6.1 6.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
CHEMBL418834 2070 None 0 Human Binding pKi None 6.1 6.1 -2 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
129 3440 None 10 Human Binding pKi None 6.1 6.1 -2818 9
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
9868452 3440 None 10 Human Binding pKi None 6.1 6.1 -2818 9
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
CHEMBL65280 3440 None 10 Human Binding pKi None 6.1 6.1 -2818 9
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
135398737 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
135398737.0 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
38 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
722 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
CHEMBL42 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
DB00363 958 None 93 Human Binding pKi None 6.2 6.2 -151 89
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
2181 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
4830 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
4830.0 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
92 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
CHEMBL440294 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
DB09286 3128 None 46 Human Binding pKi None 6.2 6.2 -70 35
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
37 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746.0 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 778 None 60 Human Binding pKi None 6.3 6.3 -22 17
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
18971832 2418 None 0 Human Binding pKi None 6.3 6.3 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
21 2418 None 0 Human Binding pKi None 6.3 6.3 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
CHEMBL3186179 2418 None 0 Human Binding pKi None 6.3 6.3 -85 13
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
135398745 2914 None 112 Human Binding pKi None 6.3 6.3 -199 65
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
135398745.0 2914 None 112 Human Binding pKi None 6.3 6.3 -199 65
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
47 2914 None 112 Human Binding pKi None 6.3 6.3 -199 65
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
CHEMBL715 2914 None 112 Human Binding pKi None 6.3 6.3 -199 65
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
DB00334 2914 None 112 Human Binding pKi None 6.3 6.3 -199 65
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
1150 3878 None 121 Human Binding pKi None 6.3 6.3 -7 25
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
125 3878 None 121 Human Binding pKi None 6.3 6.3 -7 25
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
CHEMBL6640 3878 None 121 Human Binding pKi None 6.3 6.3 -7 25
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
DB08653 3878 None 121 Human Binding pKi None 6.3 6.3 -7 25
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
31101 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
31101.0 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 729 None 40 Human Binding pKi None 6.5 6.5 -128 36
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
10358392 2084 None 0 Human Binding pKi None 6.5 6.5 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
66 2084 None 0 Human Binding pKi None 6.5 6.5 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
CHEMBL326418 2084 None 0 Human Binding pKi None 6.5 6.5 -10 2
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
115 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
115 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
4296 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
4296 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
CHEMBL274866 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
CHEMBL274866 3791 None 80 Human Binding pKi None 6.6 6.6 -2 27
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
114 2254 None 14 Human Binding pKi None 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
6426760 2254 None 14 Human Binding pKi None 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
CHEMBL292779 2254 None 14 Human Binding pKi None 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
2105 3054 None 37 Human Binding pKi None 6.6 6.6 -436 33
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 3054 None 37 Human Binding pKi None 6.6 6.6 -436 33
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 3054 None 37 Human Binding pKi None 6.6 6.6 -436 33
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 3054 None 37 Human Binding pKi None 6.6 6.6 -436 33
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 3054 None 37 Human Binding pKi None 6.6 6.6 -436 33
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2601 3780 None 33 Human Binding pKi None 6.6 6.6 -87 21
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 3780 None 33 Human Binding pKi None 6.6 6.6 -87 21
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 3780 None 33 Human Binding pKi None 6.6 6.6 -87 21
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 3780 None 33 Human Binding pKi None 6.6 6.6 -87 21
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 3780 None 33 Human Binding pKi None 6.6 6.6 -87 21
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
10287730 3536 None 40 Human Binding pKi None 6.7 6.7 -251 12
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
77 3536 None 40 Human Binding pKi None 6.7 6.7 -251 12
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
CHEMBL425190 3536 None 40 Human Binding pKi None 6.7 6.7 -251 12
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
475100 189 None 0 Human Binding pKi None 6.8 6.8 -158 6
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
67 189 None 0 Human Binding pKi None 6.8 6.8 -158 6
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
CHEMBL3542429 189 None 0 Human Binding pKi None 6.8 6.8 -158 6
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
136 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
136 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
223 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
223 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
643606 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
643606 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
CHEMBL10347 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
CHEMBL10347 3292 None 32 Human Binding pKi None 7.0 7.0 -177 15
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
2435 3590 None 83 Human Binding pKi None 7 7.0 -128 48
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
60149 3590 None 83 Human Binding pKi None 7 7.0 -128 48
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
98 3590 None 83 Human Binding pKi None 7 7.0 -128 48
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
CHEMBL12713 3590 None 83 Human Binding pKi None 7 7.0 -128 48
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
DB06144 3590 None 83 Human Binding pKi None 7 7.0 -128 48
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
134 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
134 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
1775 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
1775 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
9681 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
9681 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
9681.0 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
9681.0 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
CHEMBL1065 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
CHEMBL1065 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
DB00247 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
DB00247 2514 None 24 Human Binding pKi None 7.1 7.1 -14 67
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
102 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
102 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
3659 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
3659 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
8969 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
8969 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
8969.0 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
8969.0 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
CHEMBL15245 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
CHEMBL15245 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
DB01392 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
DB01392 4127 None 48 Human Binding pKi None 7.2 7.2 -64 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
133 2496 None 52 Human Binding pKi None 7.2 7.2 -23 42
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
1723 2496 None 52 Human Binding pKi None 7.2 7.2 -23 42
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
28693 2496 None 52 Human Binding pKi None 7.2 7.2 -23 42
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
CHEMBL19215 2496 None 52 Human Binding pKi None 7.2 7.2 -23 42
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
DB13520 2496 None 52 Human Binding pKi None 7.2 7.2 -23 42
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
103 4153 None 61 Human Binding pKi None 7.2 7.2 -48 53
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 4153 None 61 Human Binding pKi None 7.2 7.2 -48 53
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 4153 None 61 Human Binding pKi None 7.2 7.2 -48 53
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 4153 None 61 Human Binding pKi None 7.2 7.2 -48 53
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 4153 None 61 Human Binding pKi None 7.2 7.2 -48 53
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
3652 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809.0 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 4097 None 79 Human Binding pKi None 7.3 7.3 -3 18
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
107 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
107 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
1833 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
1833 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
CHEMBL8165 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
CHEMBL8165 141 None 121 Human Binding pKi None 7.4 7.4 -16 30
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
122 1437 None 9 Human Binding pKi None 7.4 7.4 -5 11
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
156314 1437 None 9 Human Binding pKi None 7.4 7.4 -5 11
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
CHEMBL1332062 1437 None 9 Human Binding pKi None 7.4 7.4 -5 11
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
1588 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864.0 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 2325 None 27 Human Binding pKi None 7.7 7.7 -42 44
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
4106 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
4106 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
4106 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
4106 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
5358812 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
5358812 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
5358812 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
5358812 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
89 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
89 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
89 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
89 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
CHEMBL93240 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
CHEMBL93240 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
CHEMBL93240 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
CHEMBL93240 2502 None 22 Human Binding pKi None 7.8 7.8 -11 34
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
1342 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
1342 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
1342 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
3 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
3 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
3 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
CHEMBL277120 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
CHEMBL277120 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
CHEMBL277120 35 None 49 Human Binding pKi None 7.8 7.8 -4 19
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
108 669 None 0 Human Binding pKi None 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 5 2.9 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(F)cc2 11040052
177836 669 None 0 Human Binding pKi None 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 5 2.9 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(F)cc2 11040052
10296414 3531 None 15 Human Binding pKi None 8 8.0 -7 9
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
76 3531 None 15 Human Binding pKi None 8 8.0 -7 9
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
CHEMBL183460 3531 None 15 Human Binding pKi None 8 8.0 -7 9
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
1809 134 None 32 Mouse Binding pKi None 8.1 8.1 -97 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
4 134 None 32 Mouse Binding pKi None 8.1 8.1 -97 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
CHEMBL18840 134 None 32 Mouse Binding pKi None 8.1 8.1 -97 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
163091 494 None 34 Human Binding pKi None 8.1 8.1 -131 10
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
163091.0 494 None 34 Human Binding pKi None 8.1 8.1 -131 10
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
22 494 None 34 Human Binding pKi None 8.1 8.1 -131 10
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
CHEMBL504548 494 None 34 Human Binding pKi None 8.1 8.1 -131 10
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
DB06216 494 None 34 Human Binding pKi None 8.1 8.1 -131 10
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
132 1275 None 13 Mouse Binding pKi None 8.1 8.1 -125 15
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
155346 1275 None 13 Mouse Binding pKi None 8.1 8.1 -125 15
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
CHEMBL378501 1275 None 13 Mouse Binding pKi None 8.1 8.1 -125 15
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
127 3126 None 52 Mouse Binding pKi None 8.1 8.1 -18 15
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
688095 3126 None 52 Mouse Binding pKi None 8.1 8.1 -18 15
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
CHEMBL117405 3126 None 52 Mouse Binding pKi None 8.1 8.1 -18 15
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
108029 3414 None 57 Human Binding pKi None 8.1 8.1 -7 13
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
23 3414 None 57 Human Binding pKi None 8.1 8.1 -7 13
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
CHEMBL18785 3414 None 57 Human Binding pKi None 8.1 8.1 -7 13
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
75 3514 None 7 Human Binding pKi None 8.1 8.1 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
9870500 3514 None 7 Human Binding pKi None 8.1 8.1 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
CHEMBL191971 3514 None 7 Human Binding pKi None 8.1 8.1 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
123 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
123 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
14987 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
14987 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
CHEMBL39947 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
CHEMBL39947 2430 None 41 Human Binding pKi None 8.2 8.2 -10 3
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
106 148 None 26 Human Binding pKi None 8.2 8.2 4 6
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
1797 148 None 26 Human Binding pKi None 8.2 8.2 4 6
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
CHEMBL97450 148 None 26 Human Binding pKi None 8.2 8.2 4 6
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
1809 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
1809 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
4 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
4 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
CHEMBL18840 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
CHEMBL18840 134 None 32 Human Binding pKi None 8.3 8.3 -15 36
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
1524 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
197 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
3822 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
3822.0 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
88 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
CHEMBL51 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
DB12465 2181 None 96 Mouse Binding pKi None 8.3 8.3 -4 52
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
135 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
1796 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
4184 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
4184.0 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
CHEMBL6437 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
DB06148 2532 None 43 Mouse Binding pKi None 8.3 8.3 -3 58
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
2470 3653 None 50 Mouse Binding pKi None 8.3 8.3 -194 59
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
3300 3653 None 50 Mouse Binding pKi None 8.3 8.3 -194 59
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
5265 3653 None 50 Mouse Binding pKi None 8.3 8.3 -194 59
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
99 3653 None 50 Mouse Binding pKi None 8.3 8.3 -194 59
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
CHEMBL267930 3653 None 50 Mouse Binding pKi None 8.3 8.3 -194 59
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
102 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
3659 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
8969 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
8969.0 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
CHEMBL15245 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
DB01392 4127 None 48 Mouse Binding pKi None 8.3 8.3 -186 49
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
2865 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
59 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
60854 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
60854.0 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
CHEMBL708 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
DB00246 4143 None 73 Human Binding pKi None 8.3 8.3 -12 53
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
109 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
109 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
2689 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
2689 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
CHEMBL27403 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
CHEMBL27403 902 None 31 Human Binding pKi None 8.4 8.4 -1 7
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
128 149 None 11 Mouse Binding pKi None 8.4 8.4 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
172267 149 None 11 Mouse Binding pKi None 8.4 8.4 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
CHEMBL273273 149 None 11 Mouse Binding pKi None 8.4 8.4 -2 8
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
10531 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
10531 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
10531.0 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
10531.0 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
121 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
121 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
888 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
888 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
CHEMBL1732 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
CHEMBL1732 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
DB00320 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8863519
DB00320 1420 None 21 Human Binding pKi None 8.6 8.6 -12 23
UnclassifiedUnclassified
Guide to Pharmacology 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 8967979
14533720 182 None 0 Human Binding pKi None 8.7 8.7 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 2.2 O=C(OCC1OC1)NCC[Si]([Si](C)(C)C)(C)C 9397179
6 182 None 0 Human Binding pKi None 8.7 8.7 -3 3
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 2.2 O=C(OCC1OC1)NCC[Si]([Si](C)(C)C)(C)C 9397179
117 353 None 19 Human Binding pKi None 8.9 8.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
120 353 None 19 Human Binding pKi None 8.9 8.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
66004 353 None 19 Human Binding pKi None 8.9 8.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
CHEMBL88240 353 None 19 Human Binding pKi None 8.9 8.9 -1 2
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
28 3496 None 46 Human Binding pKi None 9 9.0 13 10
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
3292447 3496 None 46 Human Binding pKi None 9 9.0 13 10
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL20963 3496 None 46 Human Binding pKi None 9 9.0 13 10
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
107780 1844 None 54 Human Binding pKi None 9.2 9.2 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
14 1844 None 54 Human Binding pKi None 9.2 9.2 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
CHEMBL15928 1844 None 54 Human Binding pKi None 9.2 9.2 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
107780 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
107780 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
107780 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
107780 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
107780 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
14 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
14 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
14 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
14 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
CHEMBL15928 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
CHEMBL15928 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
CHEMBL15928 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
CHEMBL15928 1844 None 54 Human Binding pKi None 9.4 9.4 1 17
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
197706 1464 None 0 Human Binding pKi None 9.4 9.4 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1464 None 0 Human Binding pKi None 9.4 9.4 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1464 None 0 Human Binding pKi None 9.4 9.4 -1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
124 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
2032 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
4636 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
4636.0 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
CHEMBL762 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
DB00935 2981 None 47 Human Binding pKi None 9.5 9.5 1 33
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
197706 1464 None 0 Rat Binding pKi None 9.7 9.7 1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 1464 None 0 Rat Binding pKi None 9.7 9.7 1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 1464 None 0 Rat Binding pKi None 9.7 9.7 1 10
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763