Ligand source activities (1 row/activity)



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

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 Assay
Type

 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 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


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Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name		 GPCRdb
ID		 Reference
ligand		 Vendors

 Species

 Assay
Type		 Activity
Type		 Activity
Relation		 Activity
Value		 p-value
(-log)		 Fold
selectivity		 Tested
GPCRs		 Assay
Description		 Source

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 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