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 36098 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 36098 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 118996 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 118996 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 35806 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 35806 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 39997 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 39997 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 121336 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 121336 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 38888 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 38888 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 121049 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 121049 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 121189 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 121189 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 40053 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 40053 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 52331 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 52331 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 165628 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 165628 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 40204 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 40204 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 39819 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 39819 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 205469 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 205469 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
125181385 195322 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@@H](C)Cc1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5400905 195322 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@@H](C)Cc1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
40 1547 None 36 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 36 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 36 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 36 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 36 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 36 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 101083 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 101083 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 55 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 4008 None 55 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 55 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 55 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 55 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 55 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 55 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 55 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
163585306 195142 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5397369 195142 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
11796806 102772 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 102772 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
125181384 196110 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@H](C)Cc1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5417081 196110 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@H](C)Cc1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
2869 4152 None 54 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 54 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 54 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 54 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 54 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 54 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 179100 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 179100 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 205838 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 205838 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
121493472 195370 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@@H](C)Cc1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5402187 195370 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@@H](C)Cc1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
10600213 205567 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 205567 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
163757283 195169 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CC[C@@H](Cc1ccc2ccoc2c1)NC 10.1021/acsmedchemlett.3c00358
CHEMBL5397993 195169 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CC[C@@H](Cc1ccc2ccoc2c1)NC 10.1021/acsmedchemlett.3c00358
145975946 164015 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 164015 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
163757284 195497 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CCC(Cc1ccc2ccoc2c1)NC 10.1021/acsmedchemlett.3c00358
CHEMBL5404902 195497 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CCC(Cc1ccc2ccoc2c1)NC 10.1021/acsmedchemlett.3c00358
24762221 19326 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 19326 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 40538 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 40538 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 14430 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 14430 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 14430 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 18968 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 18968 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 19477 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 19477 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 178943 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 178943 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 44 Human Functional pEC50 = 6.6 6.6 -95 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 44 Human Functional pEC50 = 6.6 6.6 -95 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 44 Human Functional pEC50 = 6.6 6.6 -95 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 44 Human Functional pEC50 = 6.6 6.6 -95 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 78807 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 78807 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
163982955 195154 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5397645 195154 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
145964150 164401 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 164401 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 205457 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 205457 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 35701 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 35701 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 116900 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 116900 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
121490990 196954 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CC[C@@H](Cc1ccc2occc2c1)NC 10.1021/acsmedchemlett.3c00358
CHEMBL5435545 196954 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CC[C@@H](Cc1ccc2occc2c1)NC 10.1021/acsmedchemlett.3c00358
52946290 19109 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 19109 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 46 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 46 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 46 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 46 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 46 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 46 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 19327 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 19327 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 119260 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 119260 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 15 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 15 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 15 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 205535 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 205535 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 168152 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 168152 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 101767 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 101767 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 19089 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 19089 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 206179 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 206179 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 168261 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 168261 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
163982955 195154 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5397645 195154 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2ccoc2c1 10.1021/acsmedchemlett.3c00358
11 1187 None 17 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 17 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 17 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
139033209 197173 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CCC(Cc1ccc2occc2c1)NC 10.1021/acsmedchemlett.3c00358
CHEMBL5440408 197173 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 4 1 2 3.0 CCC(Cc1ccc2occc2c1)NC 10.1021/acsmedchemlett.3c00358
44592208 179285 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 179285 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 19090 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 19090 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 178942 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 178942 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 101112 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 101112 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
163585306 195142 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5397369 195142 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 203 3 1 3 2.2 CNC(C)C(=O)c1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
2543 3707 None 46 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 46 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 46 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 46 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 46 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 46 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 205497 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 205497 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
121493473 196775 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@H](C)Cc1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
CHEMBL5431933 196775 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assayAgonist activity at 5HT1B receptor in forskolin induced CHO-K1 cells incubated for 60 mins by DiscoverX HitHunter cAMP assay
ChEMBL 189 3 1 2 2.6 CN[C@H](C)Cc1ccc2occc2c1 10.1021/acsmedchemlett.3c00358
10621021 205842 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 205842 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 101112 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 101112 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 101083 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 101083 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 164015 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 164015 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 164401 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 164401 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 189166 None 19 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 189166 None 19 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 132866 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 132866 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
13339 1207 None 7 Human Functional pIC50 = 6.1 6.1 -3311 3
Antagonist activity at 5-HT1B (unknown origin)Antagonist activity at 5-HT1B (unknown origin)
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
146361282 1207 None 7 Human Functional pIC50 = 6.1 6.1 -3311 3
Antagonist activity at 5-HT1B (unknown origin)Antagonist activity at 5-HT1B (unknown origin)
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
CHEMBL5414447 1207 None 7 Human Functional pIC50 = 6.1 6.1 -3311 3
Antagonist activity at 5-HT1B (unknown origin)Antagonist activity at 5-HT1B (unknown origin)
ChEMBL 613 8 1 6 5.1 CCOC1=C(C=CC=C1)C2=CC=C(N3CCN(C[C@H]3CC)C(=O)C4(CCC4)C(F)(F)F)C(=N2)C(=O)N[C@@H]5CN6CCC5CC6 10.1021/acsmedchemlett.3c00514
11662592 72368 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 72368 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 16651 None 7 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 16651 None 7 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 1 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 1 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 1 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 11722 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 11722 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 11722 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 11725 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 11725 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 11725 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 2 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 2 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 2 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 12237 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 12237 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 12237 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 35701 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 35701 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 169022 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 169022 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 39997 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 39997 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 121189 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 121189 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 40053 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 40053 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 39819 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 39819 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 121336 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 121336 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 35806 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 35806 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 121049 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 121049 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 36098 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 36098 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 72654 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 72654 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 40204 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 40204 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 38888 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 38888 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 118996 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 118996 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 71995 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 71995 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 165628 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 165628 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 71859 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 71859 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 72473 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 72473 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 72898 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 72898 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 133656 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 133656 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 16659 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 16659 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 16646 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 16646 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 16661 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 16661 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 19307 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 19307 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 16645 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 16645 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 19143 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 19143 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 19308 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 19308 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 19350 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 19350 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 72605 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 72605 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 16640 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 16640 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 16641 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 16641 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 16643 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 16643 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 16676 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 16676 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 16691 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 16691 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 189581 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 189581 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 189581 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 189581 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 189581 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 189581 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 71881 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 71881 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 72459 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 72459 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 72519 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 72519 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 16639 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 16639 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 16650 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 16650 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 71841 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 71841 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 72539 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 72539 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 16633 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 16633 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 16647 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 16647 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 16651 None 7 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 16651 None 7 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 16667 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 16667 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 16671 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 16671 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 16683 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 16683 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 16703 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 16703 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 178938 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 178938 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 40538 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 40538 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 71955 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 71955 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 72425 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 72425 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 16634 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 16634 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 16666 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 16666 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 193091 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 193091 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 19349 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 19349 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 189599 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 189599 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 193091 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 193091 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 116812 None 30 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 116812 None 30 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 116511 None 3 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 116511 None 3 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 71902 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 71902 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 30418 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 30418 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 71868 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 71868 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 30115 None 1 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 30115 None 1 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 27619 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 27619 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 30044 None 2 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 30044 None 2 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 179115 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 179115 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 189303 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 189303 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 179031 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 179031 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 35202 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 35202 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 119260 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 119260 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 71866 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 71866 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 132866 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 132866 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 16632 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 16632 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 16644 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 16644 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 16655 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 16655 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 178941 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 178941 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 189372 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 189372 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 29761 None 1 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 29761 None 1 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 46 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 187074 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 187074 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 187074 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 187074 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 29129 None 0 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 29129 None 0 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 30107 None 22 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 30107 None 22 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 31592 None 7 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 31592 None 7 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 40 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 40 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 40 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 40 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 40 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 40 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 115265 None 0 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 115265 None 0 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 35395 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 35395 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 119155 None 24 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 119155 None 24 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 113141 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 113141 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 71869 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 71869 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 71907 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 71907 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 72031 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 72031 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 178938 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 178938 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 178938 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 178938 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 179286 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 179286 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 19108 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 19108 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 189472 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 189472 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 78849 None 8 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 78849 None 8 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 19160 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 19160 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 71856 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 71856 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 29548 None 38 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 29548 None 38 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 73048 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 73048 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 35199 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 35199 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 18985 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 18985 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 71989 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 71989 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 44 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 44 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 44 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 44 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 44 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 44 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 44 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 44 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 73046 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 73046 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 31590 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 31590 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 27012 None 0 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 27012 None 0 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 178957 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 178957 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 178958 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 178958 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 73047 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 73047 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 133634 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 133634 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 71882 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 71882 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 26831 None 47 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 26831 None 47 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 179013 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 179013 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 45 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 45 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 45 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 45 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 26740 None 0 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 26740 None 0 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 16638 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 16638 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 72367 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 72367 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 31595 None 0 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 31595 None 0 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 30881 None 9 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 30881 None 9 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 178963 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 178963 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 35629 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 35629 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 72368 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 72368 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 30272 None 3 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 30272 None 3 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 28 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 28 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 28 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 28 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 28 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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 57 Rat Functional pIC50 = 8.3 8.3 -707 17
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 44 Human Functional pIC50 = 6.2 6.2 -95 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
31 187 None 44 Human Functional pIC50 = 6.2 6.2 -95 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
7 187 None 44 Human Functional pIC50 = 6.2 6.2 -95 9
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
CHEMBL56 187 None 44 Human Functional pIC50 = 6.2 6.2 -95 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 61 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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 53 Human Functional pIC50 None 6.3 6.3 -33 10
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 10 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 10 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 10 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 16 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 16 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 16 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 12 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 12 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 12 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 12093 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 12093 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 12093 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 11390 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 11390 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 11390 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 45 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 45 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 45 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 45 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 217023 None 9 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 45 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 45 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 45 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 45 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 156341 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 156341 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 70585 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 70585 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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 6 Rat Binding pIC50 = 9.7 9.7 4 27
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 52688 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 52688 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 39691 None 14 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 39691 None 14 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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 46 Human Binding pIC50 = 9.3 9.3 -3 31
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 96714 None 18 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 96714 None 18 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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 13 Rat Binding pIC50 = 9.1 9.1 -5 30
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 38910 None 18 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 38910 None 18 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 96712 None 14 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 96712 None 14 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 101302 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 101302 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 101302 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 101302 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 39295 None 16 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 39295 None 16 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 101302 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 101302 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 35 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 35 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 35 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 35 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 35 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 35 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 97346 None 33 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 97346 None 33 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 46 Human Binding pIC50 = 8 8.0 -3 31
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 46 Human Binding pIC50 = 8 8.0 -3 31
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 46 Human Binding pIC50 = 8 8.0 -3 31
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 46 Human Binding pIC50 = 8 8.0 -3 31
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 46 Human Binding pIC50 = 8 8.0 -3 31
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 46 Human Binding pIC50 = 8 8.0 -3 31
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 21 Rat Binding pIC50 = 8 8.0 -58 43
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 121203 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 121203 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 44055 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 44055 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 40001 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 40001 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 106491 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 106491 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 106491 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 41990 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 41990 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 168410 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 168410 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 10224 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 10224 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 205184 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 205184 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 123046 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 123046 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 40 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 40 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 40 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 40 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 40 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 13736 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 13736 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 13736 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 99523 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 99523 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 99523 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 99613 None 5 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 99613 None 5 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 199931 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 199931 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 199931 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 205469 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 205469 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 205497 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 205497 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 205828 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 205828 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 11249 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 11249 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 11249 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 97443 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 97443 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 97443 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 101926 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 101926 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 67974 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 67974 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 99802 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 99802 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 56573 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 56573 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 197236 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 197236 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 197236 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 197236 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 205890 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 205890 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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 28 Rat Binding pIC50 = 7.0 7.0 -48 35
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 113153 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 113153 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 205794 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 205794 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 205842 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 205842 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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 205842 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 205842 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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 46 Human Binding pIC50 = 8.0 8.0 -3 31
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 165436 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 165436 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 205842 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 205842 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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 46 Rat Binding pIC50 = 7.0 7.0 -17 31
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 11411 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 11411 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 54608 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 54608 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 40060 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 40060 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 18 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 18 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 18 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 125456 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 125456 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 165022 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 165022 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 78403 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 78403 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 115271 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 115271 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 89304 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 89304 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 205924 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 205924 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 98367 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 98367 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 11411 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 11411 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 45 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 45 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 45 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 45 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 89735 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 89735 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 119968 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 119968 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 119204 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 119204 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 99058 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 99058 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 10145 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 10145 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 10656 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 10656 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 10145 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 10145 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 119452 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 119452 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 162555 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 162555 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 205497 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 205497 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 89311 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 89311 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 10656 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 10656 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 119930 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 119930 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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 38 Rat Binding pIC50 = 4.9 4.9 -16 28
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 194821 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 194821 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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 59 Rat Binding pIC50 = 5.9 5.9 -120 22
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 56031 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 56031 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 56514 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 56514 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 120211 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 120211 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 39961 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 39961 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 79561 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 79561 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 102082 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 102082 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 102082 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 102082 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 119801 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 119801 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 9625 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 9625 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 118825 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 118825 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 205566 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 205566 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 194849 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 194849 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 120032 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 120032 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 98963 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 98963 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 119929 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 119929 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 50235 None 31 Rat Binding pIC50 = 4.9 4.9 -38 11
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 50235 None 31 Rat Binding pIC50 = 4.9 4.9 -38 11
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 50235 None 31 Rat Binding pIC50 = 4.9 4.9 -38 11
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 34 Rat Binding pIC50 = 5.9 5.9 -3 43
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 55 Rat Binding pIC50 = 5.9 5.9 -35 41
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 55 Rat Binding pIC50 = 5.9 5.9 -35 41
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 55 Rat Binding pIC50 = 5.9 5.9 -35 41
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 55 Rat Binding pIC50 = 5.9 5.9 -35 41
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 55 Rat Binding pIC50 = 5.9 5.9 -35 41
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 161661 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 161661 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 119322 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 119322 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 205457 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 205457 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 16 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 16 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 16 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 38153 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 38153 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 89736 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 89736 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 38902 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 38902 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 39096 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 39096 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 39732 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 39732 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 40550 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 40550 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 102772 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 102772 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 165377 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 165377 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 102772 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 102772 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 47754 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 47754 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 103517 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 103517 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 163372 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 163372 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 162542 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 162542 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 102772 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 102772 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 98238 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 98238 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 164127 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 164127 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 164127 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 164127 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 205279 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 205279 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 113391 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 113391 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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 14 Rat Binding pIC50 = 7.8 7.8 -6 15
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 101112 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 101112 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 113391 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 113391 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 53016 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 53016 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 101112 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 101112 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 17 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 17 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 17 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 38769 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 38769 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 10 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 10 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 10 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 121053 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 121053 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 26 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 26 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 26 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 194835 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 194835 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 55123 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 55123 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 9857 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 9857 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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 46 Human Binding pIC50 = 7.8 7.8 -3 31
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 206139 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 206139 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 45 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 45 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 45 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 45 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 71662 None 11 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 71662 None 11 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 38154 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 38154 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 102848 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 102848 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 78403 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 78403 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 119983 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 119983 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 120206 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 120206 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 11046 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 11046 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 14535 None 5 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 14535 None 5 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 119938 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 119938 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 38609 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 38609 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 38020 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 38020 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 11046 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 11046 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 114416 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 114416 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 79558 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 79558 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 19 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 19 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 19 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 19 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 19 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 19 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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 46 Rat Binding pIC50 = 7.8 7.8 -17 31
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 56280 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 56280 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 56528 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 56528 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 120289 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 120289 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 37971 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 37971 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 78402 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 78402 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 102708 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 102708 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 18 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 18 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 18 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 168261 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 168261 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 167141 None 1 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 167141 None 1 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 10 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 10 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 10 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 44 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 44 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 44 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 44 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 44 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 205526 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 205526 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 10292 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 10292 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 39 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 39 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 39 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 39 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 39 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 101083 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 101083 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 101083 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 101083 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 205398 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 205398 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 101789 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 101789 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 37 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 37 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 37 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 37 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 37 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 37 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 205788 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 205788 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 101703 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 101703 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
141 1427 None 18 Human Binding pIC50 = 5.7 5.7 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 5.7 5.7 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 5.7 5.7 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 5.7 5.7 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
124 2981 None 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -2 32
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 32 Rat Binding pIC50 = 8.7 8.7 -8 21
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 32 Rat Binding pIC50 = 8.7 8.7 -8 21
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 32 Rat Binding pIC50 = 8.7 8.7 -8 21
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 45 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 45 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 45 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 52651 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 52651 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 54735 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 54735 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 119870 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 119870 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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 13 Rat Binding pIC50 = 8.6 8.6 -5 16
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 67820 None 12 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 67820 None 12 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 204555 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 204555 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 55161 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 55161 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 119951 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 119951 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 205607 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 205607 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 205783 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 205783 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 165356 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 165356 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 89728 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 89728 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 40276 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 40276 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 99137 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 99137 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 99137 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 11249 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 11249 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 11249 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 11257 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 11257 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 11257 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 12372 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 12372 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 12372 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 96150 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 96150 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 96150 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 98600 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 98600 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 98600 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 99613 None 5 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 99613 None 5 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 99613 None 5 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 99613 None 5 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 89306 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 89306 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 89310 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 89310 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 101720 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 101720 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 209380 None 58 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 209380 None 58 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 209380 None 58 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 110441 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 110441 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 99306 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 99306 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 35537 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 35537 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 37784 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 37784 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 165467 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 165467 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 110441 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 110441 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 78891 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 78891 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 206121 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 206121 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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 57 Rat Binding pIC50 = 5.7 5.7 -691 91
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 184868 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 184868 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 165015 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 165015 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 205535 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 205535 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 79559 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 79559 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 79680 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 79680 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 209480 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 209480 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 83572 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 83572 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 207971 None 50 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 207971 None 50 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 207971 None 50 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 165004 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 165004 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 52979 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 52979 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 9613 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 9613 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 98656 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 98656 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 56287 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 56287 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 38330 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 38330 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 102913 None 65 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 102913 None 65 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 102913 None 65 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 102913 None 65 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 111460 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 111460 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 99003 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 99003 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 102187 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 102187 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 203402 None 16 Rat Binding pIC50 = 7.6 7.6 -22 21
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 203402 None 16 Rat Binding pIC50 = 7.6 7.6 -22 21
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 203402 None 16 Rat Binding pIC50 = 7.6 7.6 -22 21
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 39805 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 39805 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 121135 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 121135 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 104370 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 104370 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
141 1427 None 18 Human Binding pIC50 = 5.6 5.6 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pIC50 = 5.6 5.6 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pIC50 = 5.6 5.6 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pIC50 = 5.6 5.6 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
19978038 197266 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 197266 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 121114 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 121114 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 100920 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 100920 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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 57 Rat Binding pIC50 = 5.6 5.6 -691 91
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 14106 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 14106 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 205191 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 205191 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 14106 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 14106 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 54753 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 54753 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 39937 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 39937 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 118830 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 118830 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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 38 Rat Binding pIC50 = 4.6 4.6 -16 28
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 41 Rat Binding pIC50 = 4.6 4.6 -1778 17
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 41 Rat Binding pIC50 = 4.6 4.6 -1778 17
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 41 Rat Binding pIC50 = 4.6 4.6 -1778 17
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 120090 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 120090 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 193537 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 193537 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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 38 Rat Binding pIC50 = 5.6 5.6 -39 32
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 167717 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 167717 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 11680 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 11680 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 11680 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 115362 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 115362 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 9466 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 9466 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 10204 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 10204 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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 46 Human Binding pIC50 = 7.6 7.6 -3 31
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 56585 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 56585 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 114510 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 114510 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 36 Rat Binding pIC50 = 7.6 7.6 1 26
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 36 Rat Binding pIC50 = 7.6 7.6 1 26
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 36 Rat Binding pIC50 = 7.6 7.6 1 26
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 169376 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 169376 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 23515 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 23515 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 4781 None 63 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 4781 None 63 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 168562 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 168562 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 89308 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 89308 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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 39 Rat Binding pIC50 = 5.6 5.6 -501 49
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 114510 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 114510 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 10246 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 10246 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 10246 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 10246 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 10246 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 10246 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 35540 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 35540 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 206179 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 206179 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 205720 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 205720 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 164127 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 164127 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 40290 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 40290 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 205838 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 205838 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 56294 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 56294 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 56509 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 56509 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 89729 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 89729 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 45 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 45 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 45 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 45 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 125454 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 125454 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 211058 None 19 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 205904 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 205904 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 98530 None 39 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 98530 None 39 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 121372 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 121372 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 99501 None 3 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 99501 None 3 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 99549 None 14 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 99549 None 14 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 98820 None 45 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 98820 None 45 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 98820 None 45 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 111380 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 111380 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 113456 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 113456 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 29624 None 14 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 29624 None 14 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 10246 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 10246 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 10246 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 10246 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 100975 None 22 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 100975 None 22 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 202610 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 339 4 1 5 3.4 Oc1nc2ccc(CCN3CCN(c4ccccc4)CC3)cc2s1 10.1021/jm970298c
CHEMBL59637 202610 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 339 4 1 5 3.4 Oc1nc2ccc(CCN3CCN(c4ccccc4)CC3)cc2s1 10.1021/jm970298c
10501785 205185 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 205185 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 52467 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 52467 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 35544 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 35544 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 79679 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 79679 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 203598 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 203598 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 99041 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 99041 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 99041 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 165512 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 165512 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 165512 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 102808 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 102808 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 11249 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 11249 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 11249 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 12050 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 12050 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 12050 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 97193 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 97193 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 97193 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 98756 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 98756 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 193433 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 193433 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 67821 None 11 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 67821 None 11 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 162466 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 162466 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 110568 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 110568 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 165638 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 165638 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 10877 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 10877 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 205533 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 205533 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 203821 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 203821 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 125453 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 125453 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 110568 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 110568 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 205567 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 205567 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 70310 None 0 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 70310 None 0 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 9625 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 9625 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 52778 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 52778 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 11199 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 11199 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 101771 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 101771 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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 32 Rat Binding pIC50 = 5.5 5.5 -13 29
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 9593 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 9593 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 11041 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 11041 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 89305 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 89305 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 40507 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 40507 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 98164 None 3 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 98164 None 3 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 98164 None 3 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 55833 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 55833 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 11041 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 11041 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 55178 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 55178 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 26 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 26 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 26 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 26 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 26 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 26 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 205846 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 205846 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 38304 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 38304 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 10101 None 0 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 10101 None 0 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 18557 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 18557 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 194829 None 40 Rat Binding pIC50 = 4.5 4.5 -48 3
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 194829 None 40 Rat Binding pIC50 = 4.5 4.5 -48 3
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 194829 None 40 Rat Binding pIC50 = 4.5 4.5 -48 3
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 113553 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 113553 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 38023 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 38023 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 113553 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 113553 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 38175 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 38175 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 162088 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 162088 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 98462 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 98462 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 10469 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 10469 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 27 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 27 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 27 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 27 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 27 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 27 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 56929 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 56929 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 101111 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 101111 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 102672 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 102672 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 164195 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 164195 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 118568 None 0 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 118568 None 0 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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 38 Rat Binding pIC50 = 5.4 5.4 -389 39
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 102768 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 102768 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 58 Rat Binding pIC50 = 6.4 6.4 -2 22
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 58 Rat Binding pIC50 = 6.4 6.4 -2 22
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 58 Rat Binding pIC50 = 6.4 6.4 -2 22
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 9625 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 9625 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 26424 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 26424 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 44 Rat Binding pIC50 = 5.4 5.4 -7413 43
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 44 Rat Binding pIC50 = 5.4 5.4 -7413 43
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 44 Rat Binding pIC50 = 5.4 5.4 -7413 43
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 44 Rat Binding pIC50 = 5.4 5.4 -7413 43
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 89309 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 89309 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 9625 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 9625 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 195880 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 195880 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 52856 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 52856 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 56577 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 56577 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 55450 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 55450 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 16421 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 16421 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 54588 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 54588 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 119789 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 119789 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 205776 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 205776 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 99544 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 99544 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 99544 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 40128 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 40128 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 99480 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 99480 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 99480 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 48 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 48 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 48 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 48 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 48 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 48 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 205401 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 205401 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 46 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 46 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 46 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 46 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 46 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 46 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 53095 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 53095 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 40446 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 40446 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 39982 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 39982 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 189282 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 189282 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 189282 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 189282 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 35664 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 35664 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 4 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 4 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 4 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 102183 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 102183 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 10877 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 10877 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 196468 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 196468 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 51973 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 51973 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 28568 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 28568 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 56248 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 56248 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 38390 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 38390 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 56371 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 56371 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 203223 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 203223 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 38152 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 38152 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 44041 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 44041 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 101055 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 101055 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 110961 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 110961 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 164195 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 164195 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 164195 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 164195 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 53161 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 53161 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 164195 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 164195 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 10291 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 10291 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 210300 None 60 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 210300 None 60 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 120048 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 120048 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 35602 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 35602 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 98504 None 30 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 98504 None 30 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 188329 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 188329 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 52793 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 52793 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 52793 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 52793 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 53439 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 53439 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 100938 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 100938 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 125455 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 125455 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 205894 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 205894 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 53439 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 53439 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 53161 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 53161 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 51874 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 51874 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 52934 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 52934 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 18562 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 18562 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 57 Rat Binding pIC50 = 5.3 5.3 - 17
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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 162594 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 162594 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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 41 Rat Binding pIC50 = 4.3 4.3 -1778 17
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 15269 None 0 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 15269 None 0 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 36 Rat Binding pIC50 = 7.3 7.3 1 26
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 36 Rat Binding pIC50 = 7.3 7.3 1 26
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 36 Rat Binding pIC50 = 7.3 7.3 1 26
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 99613 None 5 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 99613 None 5 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 164990 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 164990 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 28382 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 28382 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 100724 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 100724 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 35199 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 35199 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 102367 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 102367 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 9603 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 9603 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 56514 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 56514 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 16 Human Binding pIC50 = 6.3 6.3 -8 29
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 16 Human Binding pIC50 = 6.3 6.3 -8 29
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 16 Human Binding pIC50 = 6.3 6.3 -8 29
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 16 Human Binding pIC50 = 6.3 6.3 -8 29
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 98567 None 1 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 98567 None 1 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 56383 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 56383 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 78403 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 78403 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 193545 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 193545 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 51297 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 51297 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 112895 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 112895 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 113120 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 113120 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 89732 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 89732 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 112895 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 112895 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 52681 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 52681 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 53069 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 53069 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 205261 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 205261 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 38459 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 38459 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 24191 None 0 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 24191 None 0 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 206225 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 206225 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 194462 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 194462 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 55127 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 55127 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 52980 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 52980 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 45 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 45 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 45 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 54 Human Binding pIC50 = 8.2 8.2 -5 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 39393 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 39393 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 122084 None 13 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 122084 None 13 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 45 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 45 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 45 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 45 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 35612 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 35612 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 44466 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 44466 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 202766 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 202766 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 10168 None 5 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 97113 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 97113 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 97113 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 10074 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 10074 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 100829 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 100829 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 111729 None 5 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 111729 None 5 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 55235 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 55235 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 55235 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 55235 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 119585 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 119585 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 168152 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 168152 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 53731 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 53731 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 35610 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 35610 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 15453 None 12 Rat Binding pIC50 = 6.2 6.2 -1 3
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 15453 None 12 Rat Binding pIC50 = 6.2 6.2 -1 3
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 89307 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 89307 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 205752 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 205752 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 99098 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 99098 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 96471 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 96471 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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 61 Human Binding pIC50 = 5.2 5.2 -2344 51
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 39725 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 39725 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 119329 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 119329 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 35629 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 35629 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 9625 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 9625 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 100966 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 100966 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 79557 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 79557 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 120075 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 120075 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 28363 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 28363 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 9883 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 9883 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 194858 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 194858 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 165045 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 165045 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 56296 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 56296 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 163338 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 163338 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 169781 None 14 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 169781 None 14 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 14547 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 14547 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 44259 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 44259 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 12046 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 12046 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 12046 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 65 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 65 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 65 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 65 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 65 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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 100793 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 100793 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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 58 Rat Binding pIC50 = 5.2 5.2 -2 22
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 205549 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 205549 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 101644 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 101644 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 10093 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 10093 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 118999 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 118999 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 15 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 15 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 15 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 15 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 15 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 15 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 102500 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 102500 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 54950 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 54950 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 39210 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 39210 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 205542 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 205542 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 163137 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 163137 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 15 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 15 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 15 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 89727 None 0 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 89727 None 0 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 15 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 15 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 15 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 37992 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 37992 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 51647 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 51647 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 188820 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 188820 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 40261 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 40261 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 55453 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 55453 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 121180 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 121180 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 40155 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 40155 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 15279 None 0 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 15279 None 0 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 205842 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 205842 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 18 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 18 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 18 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 18 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 38393 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 38393 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 40102 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 40102 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 98909 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 98909 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 67477 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 67477 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 96150 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 96150 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 96150 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 38466 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 38466 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 56019 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 56019 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 110539 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 110539 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 13962 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 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
CHEMBL119668 13962 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 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
9881324 28380 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 28380 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 120132 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 120132 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 9818 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 9818 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 40312 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 40312 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 77282 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 77282 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 120284 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 120284 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 111206 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 111206 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 37819 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 37819 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 47 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 47 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 47 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 47 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 47 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 47 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 28 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 28 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 28 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 28 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 28 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 52806 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 52806 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 119932 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 119932 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 111206 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 111206 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 9897 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 9897 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 119261 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 119261 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 168437 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 168437 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 48119 None 21 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 48119 None 21 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 20340 None 41 Rat Binding pIC50 = 4.1 4.1 -74 17
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 20340 None 41 Rat Binding pIC50 = 4.1 4.1 -74 17
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 38581 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 38581 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 56511 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 56511 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 89303 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 89303 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 96150 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 96150 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 96150 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 205885 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 205885 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 120208 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 120208 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 52960 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 52960 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 120000 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 120000 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 102797 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 102797 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 40281 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 40281 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 9994 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 9994 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 89302 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 89302 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 89306 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 89306 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 189002 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 189002 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 40406 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 40406 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 35395 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 35395 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 10224 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 10224 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 13962 None 0 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 13962 None 0 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 193134 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 193134 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 193134 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 54 Human Binding pKd = 8.8 8.8 -5 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 54 Human Binding pKd = 8.8 8.8 -5 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 54 Human Binding pKd = 8.8 8.8 -5 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 54 Human Binding pKd = 8.8 8.8 -5 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 54 Human Binding pKd = 8.8 8.8 -5 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 54 Human Binding pKd = 8.8 8.8 -5 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 193134 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 193134 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 193134 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 6 Rat Binding pKi = 10.0 10.0 4 27
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 6 Rat Binding pKi = 10.0 10.0 4 27
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 6 Rat Binding pKi = 10.0 10.0 4 27
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 6 Rat Binding pKi = 10.0 10.0 4 27
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 6 Rat Binding pKi = 10.0 10.0 4 27
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 6 Rat Binding pKi = 10.0 10.0 4 27
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 35701 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 35701 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 137289 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 137289 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 35 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 35 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 35 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 35 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 35 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 35 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 117162 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 117162 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 93822 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 93822 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 187074 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 187074 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 119385 None 30 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 119385 None 30 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 78809 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 78809 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 72552 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 72552 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 125751 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 125751 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 32 Human Binding pKi = 9.5 9.5 1 32
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 32 Human Binding pKi = 9.5 9.5 1 32
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 32 Human Binding pKi = 9.5 9.5 1 32
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 32 Human Binding pKi = 9.5 9.5 1 32
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 32 Human Binding pKi = 9.5 9.5 1 32
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 32 Human Binding pKi = 9.5 9.5 1 32
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 118208 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 118208 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 49 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 49 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 49 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 184402 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 184402 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 133602 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 133602 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 78807 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 78807 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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 13 Rat Binding pKi = 9.4 9.4 -5 30
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 170233 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 170233 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 187991 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 187991 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
2869 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
60 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
60857 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
60857.0 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
CHEMBL1185 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
DB00315 4152 None 54 Human Binding pKi = 9.4 9.4 -5 7
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1039/d3md00677h
45104767 204067 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 204067 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 204067 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 204067 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 19477 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 19477 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 78808 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 78808 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 116900 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 116900 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 126276 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 126276 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 12103 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 12103 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 12103 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
2543 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
5358 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
5358.0 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
54 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
CHEMBL128 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
DB00669 3707 None 46 Human Binding pKi = 9.3 9.3 -3 31
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1039/d3md00677h
24881204 188529 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 188529 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 99386 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 99386 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 56402 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 56402 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 56474 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 56474 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 187074 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 187074 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 188193 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 188193 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 192708 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 192708 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 193091 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 193091 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 187074 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 187074 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 70510 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 70510 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 125746 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 125746 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 125767 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 125767 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 188399 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 188399 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 71838 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 71838 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 184430 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 184430 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 186904 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 186904 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 187243 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 187243 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 72514 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 72514 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 52331 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 52331 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 52331 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 52331 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 99494 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 99494 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 125761 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 125761 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 105568 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 105568 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 105568 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 105568 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 170235 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 170235 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 173334 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 173334 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 16651 None 7 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 16651 None 7 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 91988 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 91988 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 56405 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 56405 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 186938 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 186938 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 187052 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 187052 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 193269 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 193269 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 133512 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 133512 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 14430 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 14430 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 14430 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 188414 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 188414 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 125755 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 125755 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 125753 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 125753 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 85086 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 85086 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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 32 Rat Binding pKi = 9.0 9.0 -2 32
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 203291 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 203291 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 203291 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 203291 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 35 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 35 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 35 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 35 Human Binding pKi = 9 9.0 13 17
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 35 Human Binding pKi = 9 9.0 13 17
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 35 Human Binding pKi = 9 9.0 13 17
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 108592 None 0 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 108592 None 0 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 111368 None 0 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 111368 None 0 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 56403 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 56403 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 186939 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 186939 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 125771 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 125771 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 72177 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 72177 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 135370 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 135370 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 140448 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 140448 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 45 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 109035 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 109035 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 45 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 45 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 45 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 45 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 125745 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 125745 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
28 3496 None 35 Human Binding pKi = 8.9 8.9 13 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
3292447 3496 None 35 Human Binding pKi = 8.9 8.9 13 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
CHEMBL20963 3496 None 35 Human Binding pKi = 8.9 8.9 13 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.6019/CHEMBL5442175
106 148 None 19 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 19 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 19 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 25 Human Binding pKi = 8.9 8.9 -18 37
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 25 Human Binding pKi = 8.9 8.9 -18 37
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 25 Human Binding pKi = 8.9 8.9 -18 37
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 56408 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 56408 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 56475 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 56475 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 56485 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 56485 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 56488 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 56488 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 187868 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 187868 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 187799 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 187799 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 70580 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 70580 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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 13 Rat Binding pKi = 8.9 8.9 -5 16
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 11390 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 11390 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 11390 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 171862 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 171862 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 172689 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 172689 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 126280 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 126280 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 67820 None 12 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 67820 None 12 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 125766 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 125766 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 126286 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 126286 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 18968 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 18968 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
1884 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
4440 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
4440.0 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
45 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
CHEMBL1278 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
DB00952 2735 None 40 Human Binding pKi = 8.8 8.8 -2 5
Binding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5-HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1039/d3md00677h
44342784 9829 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 9829 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 10127 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 10127 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 71758 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 71758 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 82421 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 82421 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 56415 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 56415 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 56476 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 56476 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 56483 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 56483 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 93863 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 93863 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 169587 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 169587 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 187960 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 187960 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 166254 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 166254 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 9376 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 9376 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 126278 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 126278 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 203517 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 203517 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 203517 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 203517 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 12093 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 12093 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 12093 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 125747 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 125747 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 125752 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 125752 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 135303 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 135303 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 121143 None 1 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 121143 None 1 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 70912 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 70912 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 71432 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 71432 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 56412 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 56412 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 56416 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 56416 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 56477 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 56477 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 56487 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 56487 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 56489 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 56489 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 188190 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 188190 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 176159 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 176159 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 187869 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 187869 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 188190 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 188190 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 190137 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 190137 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 188190 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 188190 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 72576 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 72576 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 140978 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 140978 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 32 Human Binding pKi = 8 8.0 -1 21
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 32 Human Binding pKi = 8 8.0 -1 21
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 32 Human Binding pKi = 8 8.0 -1 21
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 72 Human Binding pKi = 8 8.0 -91 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 72 Human Binding pKi = 8 8.0 -91 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 72 Human Binding pKi = 8 8.0 -91 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 72 Human Binding pKi = 8 8.0 -91 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 72 Human Binding pKi = 8 8.0 -91 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 72 Human Binding pKi = 8 8.0 -91 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 46 Human Binding pKi = 8 8.0 -3 31
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 46 Human Binding pKi = 8 8.0 -3 31
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 46 Human Binding pKi = 8 8.0 -3 31
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 46 Human Binding pKi = 8 8.0 -3 31
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 46 Human Binding pKi = 8 8.0 -3 31
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 46 Human Binding pKi = 8 8.0 -3 31
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 9362 None 10 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 9362 None 10 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 14 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 32 Human Binding pKi = 8 8.0 -1 21
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 32 Human Binding pKi = 8 8.0 -1 21
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 32 Human Binding pKi = 8 8.0 -1 21
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 125762 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 125762 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 46 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 46 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 46 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 46 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 46 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 46 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 37 Human Binding pKi = 8 8.0 -4 18
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 37 Human Binding pKi = 8 8.0 -4 18
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 37 Human Binding pKi = 8 8.0 -4 18
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
23642275 482 None 26 Human Binding pKi = 8.0 8.0 -5 8
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.6019/CHEMBL5442175
8433 482 None 26 Human Binding pKi = 8.0 8.0 -5 8
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.6019/CHEMBL5442175
CHEMBL2164327 482 None 26 Human Binding pKi = 8.0 8.0 -5 8
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 283 2 0 3 3.1 CN([C@H]1CCc2c(C1)cccc2c1c(C)nn(c1C)C)C 10.6019/CHEMBL5442175
1251 1692 None 20 Human Binding pKi = 8.0 8.0 -1 8
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 20 Human Binding pKi = 8.0 8.0 -1 8
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 20 Human Binding pKi = 8.0 8.0 -1 8
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 20 Human Binding pKi = 8.0 8.0 -1 8
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 20 Human Binding pKi = 8.0 8.0 -1 8
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 20 Human Binding pKi = 8.0 8.0 -1 8
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 169277 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 169277 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 37 Human Binding pKi = 8.0 8.0 -4 18
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 37 Human Binding pKi = 8.0 8.0 -4 18
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 37 Human Binding pKi = 8.0 8.0 -4 18
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 210467 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 210467 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 102035 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 102035 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 102035 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 68707 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 68707 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 94023 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 94023 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 188433 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 188433 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 184429 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 184429 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 188070 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 188070 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 178677 None 4 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 178677 None 4 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 178677 None 4 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 178677 None 4 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 119761 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 119761 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 102537 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 102537 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 102537 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 24 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 24 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 24 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 67234 None 25 Rat Binding pKi = 6 6.0 -1023 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 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 10.1021/jm00384a001
CHEMBL18786 67234 None 25 Rat Binding pKi = 6 6.0 -1023 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 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 10.1021/jm00384a001
10257042 206819 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 206819 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 70 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 70 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 70 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 70 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 70 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 70 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 57 Human Binding pKi = 6 6.0 -151 91
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 57 Human Binding pKi = 6 6.0 -151 91
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 57 Human Binding pKi = 6 6.0 -151 91
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 57 Human Binding pKi = 6 6.0 -151 91
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 57 Human Binding pKi = 6 6.0 -151 91
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 57 Human Binding pKi = 6 6.0 -151 91
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 65 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 65 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 65 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 65 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 65 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 28 Human Binding pKi = 6 6.0 -977 17
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 28 Human Binding pKi = 6 6.0 -977 17
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 28 Human Binding pKi = 6 6.0 -977 17
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 28 Human Binding pKi = 6 6.0 -977 17
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 28 Human Binding pKi = 6 6.0 -977 17
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 10465 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 10465 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 90330 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 90330 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 90805 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 90805 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
CHEMBL4558518 216481 None 0 Human Binding pKi = 6 6.0 -45 14
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CNC1CCC(c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 10.6019/CHEMBL4507288
11046087 4949 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 4949 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 5132 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 5132 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 27012 None 0 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 27012 None 0 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 29129 None 0 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 29129 None 0 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 207971 None 50 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 207971 None 50 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 207971 None 50 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 186591 None 0 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 186591 None 0 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 72 Rat Binding pKi = 5.0 5.0 -204 24
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 72 Rat Binding pKi = 5.0 5.0 -204 24
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 72 Rat Binding pKi = 5.0 5.0 -204 24
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 72 Rat Binding pKi = 5.0 5.0 -204 24
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 66084 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 66084 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 172849 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 172849 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 145325 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 145325 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
9893924 4750 None 24 Human Binding pKi = 6.0 6.0 -42 22
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442175
CHEMBL103769 4750 None 24 Human Binding pKi = 6.0 6.0 -42 22
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 554 11 3 4 5.4 S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1 10.6019/CHEMBL5442175
11297 67366 None 11 Rat Binding pKi = 6.0 6.0 -26 5
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 67366 None 11 Rat Binding pKi = 6.0 6.0 -26 5
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 117551 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 117551 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 59947 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 59947 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
10531 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
10531.0 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
121 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
888 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
CHEMBL1732 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
DB00320 1420 None 13 Human Binding pKi = 7.0 7.0 -35 30
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
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 10.6019/CHEMBL5442175
4431 2729 None 18 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 18 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 18 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 19 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 19 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 19 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 19 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 19 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 19 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 206775 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 206775 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 103145 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 103145 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 22615 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 22615 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 107586 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 107586 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 11383 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 11383 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 11383 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 209578 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 209578 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 113873 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 113873 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 39 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 39 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 39 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 39 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 39 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 203402 None 16 Rat Binding pKi = 8.0 8.0 -22 21
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 203402 None 16 Rat Binding pKi = 8.0 8.0 -22 21
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 203402 None 16 Rat Binding pKi = 8.0 8.0 -22 21
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 102933 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 102933 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 206626 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 206626 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 126294 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 126294 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
1809 134 None 25 Human Binding pKi = 8.0 8.0 -18 37
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
4 134 None 25 Human Binding pKi = 8.0 8.0 -18 37
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
CHEMBL18840 134 None 25 Human Binding pKi = 8.0 8.0 -18 37
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.6019/CHEMBL5442175
44404394 132883 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 132883 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 210651 None 52 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 210651 None 52 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 209864 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 209864 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 120050 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 120050 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 4872 None 0 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 4872 None 0 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 5018 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 5018 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 30044 None 2 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 30044 None 2 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 60286 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 60286 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 133542 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 133542 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 165369 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 165369 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
42611190 3156 None 14 Human Binding pKi = 5.9 5.9 -2884 22
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
5802 3156 None 14 Human Binding pKi = 5.9 5.9 -2884 22
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
CHEMBL1800685 3156 None 14 Human Binding pKi = 5.9 5.9 -2884 22
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 475 4 2 2 7.4 OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F 10.6019/CHEMBL5442175
115 3791 None 36 Rat Binding pKi = 6.9 6.9 1 26
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 36 Rat Binding pKi = 6.9 6.9 1 26
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 36 Rat Binding pKi = 6.9 6.9 1 26
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 72368 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 72368 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 101924 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 101924 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 63053 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 63053 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 217362 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 203549 None 5 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 203549 None 5 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 127621 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 127621 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 12 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 12 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 12 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 203549 None 5 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 203549 None 5 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 71694 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 71694 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 71694 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 133615 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 133615 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 94455 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 94455 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 77160 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 77160 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 56409 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 56409 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 190034 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 190034 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 187762 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 187762 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 193222 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 193222 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 67939 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 67939 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 63071 None 5 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 63071 None 5 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 151425 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 151425 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 4707 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 4707 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 172734 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 172734 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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 38 Rat Binding pKi = 5.9 5.9 -39 32
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 166939 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 166939 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 206778 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 206778 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 62102 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 62102 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 104516 None 3 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 104516 None 3 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 104516 None 3 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 104516 None 3 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 4781 None 63 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 4781 None 63 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
4223 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
6918314 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
6918314.0 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
7427 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
CHEMBL439849 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
DB06684 3992 None 57 Human Binding pKi = 5.9 5.9 -457 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 10.6019/CHEMBL5442175
62597539 106268 None 1 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 106268 None 1 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 106268 None 1 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 80243 None 0 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 80243 None 0 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 175600 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 175600 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 175798 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 175798 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 188192 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 188192 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 210441 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 210441 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 161935 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 161935 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 90804 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 90804 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 187782 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 187782 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 188895 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 188895 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 189146 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 189146 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 39 Rat Binding pKi = 5.9 5.9 -501 49
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 39 Rat Binding pKi = 5.9 5.9 -501 49
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 39 Rat Binding pKi = 5.9 5.9 -501 49
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 39 Rat Binding pKi = 5.9 5.9 -501 49
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 39 Rat Binding pKi = 5.9 5.9 -501 49
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 39 Rat Binding pKi = 5.9 5.9 -501 49
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
11154555 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
11154555.0 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
5037 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
7671 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
CHEMBL2028019 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
CHEMBL3085826 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
DB06016 800 None 50 Human Binding pKi = 6.9 6.9 -457 24
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.6019/CHEMBL5442175
50878551 90779 None 28 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 90779 None 28 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 90779 None 28 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 90779 None 28 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 9821 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 9821 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 38 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 38 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 38 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 38 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 38 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 38 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 19 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 19 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 19 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 17928 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 17928 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 14116 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 14116 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 72021 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 72021 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 98225 None 38 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 98225 None 38 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 56278 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 56278 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 85216 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 85216 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 102529 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 102529 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 10 Rat Binding pKi = 4.9 4.9 -7585 24
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 10 Rat Binding pKi = 4.9 4.9 -7585 24
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 10 Rat Binding pKi = 4.9 4.9 -7585 24
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 114142 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 114142 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 207809 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 207809 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 33752 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 33752 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 33752 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 60318 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 60318 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 137501 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 137501 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 104514 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 104514 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
CHEMBL4535474 216454 None 39 Human Binding pKi = 5.9 5.9 -11 22
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
10498633 163398 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 163398 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 211058 None 19 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 120224 None 1 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 120224 None 1 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 77263 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 77263 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 104514 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 104514 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 67821 None 11 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 67821 None 11 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 184975 None 0 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 184975 None 0 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 63088 None 24 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 63088 None 24 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 102142 None 0 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 102142 None 0 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 102142 None 0 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 102142 None 0 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 209987 None 0 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 209987 None 0 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 12 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 12 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 12 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 10173 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 10173 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 110170 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 110170 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 38 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 38 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 38 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 38 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 38 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 38 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 35202 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 35202 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 45 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 45 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 45 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 45 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 9356 None 0 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 9356 None 0 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 63052 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 63052 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 109843 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 109843 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 126290 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 126290 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 101905 None 9 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 101905 None 9 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 119967 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 119967 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 120016 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 120016 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 126293 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 126293 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 201843 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 201843 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
CHEMBL4535474 216454 None 39 Human Binding pKi = 5.9 5.9 -11 22
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CNCc1ccccc1-c1csc([C@@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL4507273
10066481 18483 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 18483 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 116204 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 116204 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 102913 None 65 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 102913 None 65 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 102913 None 65 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 102913 None 65 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 206632 None 0 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 206632 None 0 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 65293 None 1 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 65293 None 1 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 162330 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 162330 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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 32 Rat Binding pKi = 5.8 5.8 -13 29
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 106306 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 106306 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 106306 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 147228 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 147228 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 145329 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 145329 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 204187 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 204187 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 103856 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 103856 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 188216 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 188216 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 79049 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 79049 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 191035 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 191035 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 188232 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 188232 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 70543 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 70543 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 71932 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 71932 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 210702 None 3 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 210702 None 3 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 11384 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 11384 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 11384 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 5006 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 5006 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 100230 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 100230 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 30272 None 3 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 30272 None 3 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 102176 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 102176 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 22887 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 22887 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 77893 None 7 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 77893 None 7 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
141 1427 None 18 Human Binding pKi = 5.8 5.8 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
6089 1427 None 18 Human Binding pKi = 5.8 5.8 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
CHEMBL12420 1427 None 18 Human Binding pKi = 5.8 5.8 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
DB01488 1427 None 18 Human Binding pKi = 5.8 5.8 -44 28
Displacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysisDisplacement of [3H] GR125743 from human recombinant 5-HT1B receptor expressed in human Chem-1 cells assessed as inhibition constant incubated for 90 mins by spectrophotometric analysis
ChEMBL 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C 10.1021/acsmedchemlett.3c00143
10070281 208019 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 208019 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 201193 None 5 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 201193 None 5 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 63087 None 0 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 63087 None 0 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 207827 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 207827 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 208173 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 208173 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 194829 None 40 Rat Binding pKi = 4.8 4.8 -48 3
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 194829 None 40 Rat Binding pKi = 4.8 4.8 -48 3
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 194829 None 40 Rat Binding pKi = 4.8 4.8 -48 3
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 103130 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 103130 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 103130 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 103130 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 17769 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 17769 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 13713 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 13713 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 13713 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 84423 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 84423 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 84423 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 79020 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 79020 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 92014 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 92014 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 176163 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 176163 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 189607 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 189607 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 187752 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 187752 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 96459 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 96459 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 18002 None 4 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 18002 None 4 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 114652 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 114652 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 90329 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 90329 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 187783 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 187783 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 26595 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 26595 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 186955 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 186955 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 125758 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 125758 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 12064 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 12064 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 72132 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 72132 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 217394 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 217989 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 4720 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 4720 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 123089 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 123089 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 77850 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 77850 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 77850 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 187079 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 187079 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 206656 None 1 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 206656 None 1 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 190079 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 190079 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 206670 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 206670 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 60107 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 60107 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 60107 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
3038495 708 None 33 Human Binding pKi = 6.8 6.8 -107 27
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
7625 708 None 33 Human Binding pKi = 6.8 6.8 -107 27
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
CHEMBL25236 708 None 33 Human Binding pKi = 6.8 6.8 -107 27
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 417 8 1 4 4.2 COc1ccccc1N1CCN(CC1)CCCCNC(=O)c1ccc2c(c1)cccc2 10.6019/CHEMBL5442175
9901086 187737 None 28 Human Binding pKi = 5.8 5.8 -549 15
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442175
CHEMBL4743049 187737 None 28 Human Binding pKi = 5.8 5.8 -549 15
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442175
CHEMBL494947 187737 None 28 Human Binding pKi = 5.8 5.8 -549 15
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 304 4 1 5 2.1 Clc1cccc(COc2cncc(N3CCNCC3)n2)c1 10.6019/CHEMBL5442175
14547415 100725 None 0 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 100725 None 0 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
3233 3512 None 28 Human Binding pKi = 5.8 5.8 -977 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
3247 3512 None 28 Human Binding pKi = 5.8 5.8 -977 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
6604889 3512 None 28 Human Binding pKi = 5.8 5.8 -977 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
CHEMBL282199 3512 None 28 Human Binding pKi = 5.8 5.8 -977 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
DB13988 3512 None 28 Human Binding pKi = 5.8 5.8 -977 17
PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity.
ChEMBL 352 5 1 4 2.7 CC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1cccc(c1)O 10.6019/CHEMBL5442175
180 401 None 38 Rat Binding pKi = 5.8 5.8 -389 39
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 38 Rat Binding pKi = 5.8 5.8 -389 39
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 38 Rat Binding pKi = 5.8 5.8 -389 39
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 38 Rat Binding pKi = 5.8 5.8 -389 39
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 38 Rat Binding pKi = 5.8 5.8 -389 39
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 38 Rat Binding pKi = 5.8 5.8 -389 39
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 59457 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 59457 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 10531 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 10531 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 125773 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 125773 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 38 Rat Binding pKi = 7.8 7.8 -16 28
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 38 Rat Binding pKi = 7.8 7.8 -16 28
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 38 Rat Binding pKi = 7.8 7.8 -16 28
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