Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
10696930 42862 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL144397 42862 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9897637 125710 0 None - 1 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
CHEMBL342323 125710 0 None - 1 Human 10.0 pEC50 = 10 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
10791244 42571 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL144128 42571 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10720301 46758 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL147851 46758 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10531639 128050 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
CHEMBL357830 128050 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
9984109 45651 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL146720 45651 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
11800592 127763 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL356277 127763 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10008868 127903 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
CHEMBL357478 127903 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
11797158 46814 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147901 46814 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9832057 59089 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 10.1016/s0960-894x(98)00090-0
CHEMBL158941 59089 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 10.1016/s0960-894x(98)00090-0
10836606 172312 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL424128 172312 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10647387 46965 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
CHEMBL148022 46965 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
10837858 46580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147677 46580 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10671315 209790 0 None -186 2 Human 5.0 pEC50 = 5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
CHEMBL63258 209790 0 None -186 2 Human 5.0 pEC50 = 5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 451 8 1 5 4.6 FC(F)(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(OCc2ccccc2)CC1 10.1021/jm981133m
40 8329 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
77993 8329 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
995 8329 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
CHEMBL1510 8329 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
DB00216 8329 58 None 1 8 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2021.114045
18975369 107806 0 None -120 2 Human 6.9 pEC50 = 6.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
CHEMBL294547 107806 0 None -120 2 Human 6.9 pEC50 = 6.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm981133m
4806 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 10780 88 None 1 3 Human 6.9 pEC50 = 6.9 Functional
Partial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingPartial agonist activity at human 5HT1B receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
11796806 109494 0 None -169 2 Human 5.9 pEC50 = 5.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL304857 109494 0 None -169 2 Human 5.9 pEC50 = 5.9 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
2869 10924 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60 10924 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60857 10924 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
CHEMBL1185 10924 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
DB00315 10924 89 None -3 5 Human 7.8 pEC50 = 7.8 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
44592371 185773 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL470849 185773 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
10766570 210159 0 None -501 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1 10.1021/jm981133m
CHEMBL65321 210159 0 None -501 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1cccc(F)c1 10.1021/jm981133m
10600213 209888 0 None -575 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
CHEMBL64004 209888 0 None -575 2 Human 5.8 pEC50 = 5.8 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.2 CC(CN1CCN(CC(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm981133m
145975946 170699 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 170699 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
24762221 26091 0 None -39 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290596 26091 0 None -39 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
11797999 47299 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL148314 47299 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10385855 21197 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL120055 21197 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL321818 21197 0 None -3 3 Human 8.7 pEC50 = 8.7 Functional
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonistThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor; full agonist
ChEMBL 392 6 2 4 2.7 Cc1ccccc1N1CCN(C(=O)COc2ccc3[nH]cc(CCN)c3c2)CC1 10.1016/S0960-894X(97)10164-0
10791125 25733 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1 10.1021/jm9703552
CHEMBL128699 25733 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1 10.1021/jm9703552
10649124 26242 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL129813 26242 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 502 5 0 7 3.1 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5cccc6c5OCCO6)CC4)cc23)CC1 10.1021/jm9703552
44592333 185617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469376 185617 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
1220 6975 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
31 6975 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
7 6975 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
CHEMBL56 6975 55 None -109 9 Human 6.6 pEC50 = 6.6 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
10838063 85551 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
CHEMBL2112660 85551 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 469 5 0 6 3.2 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(c5ccccc5C#N)CC4)cc23)CC1 10.1021/jm9703552
145964150 171085 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 171085 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Partial agonist activity at 5-HT1B receptor (unknown origin) by Tango assayPartial agonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
10719687 209778 0 None -257 2 Human 6.5 pEC50 = 6.5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL63167 209778 0 None -257 2 Human 6.5 pEC50 = 6.5 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 485 7 1 4 5.7 FC1(Cc2ccccc2C(F)(F)F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
11797998 42466 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL144030 42466 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10601619 123614 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
CHEMBL338015 123614 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
Agonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formationAgonist activity at 5-hydroxytryptamine 1B receptor by measuring the inhibition of forskolin-stimulated cAMP formation
ChEMBL 504 7 0 7 3.3 COc1cccc(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c1OC 10.1021/jm9703552
52946290 25874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 446 4 0 5 4.4 Cc1ccc2c(N3CCN(CCc4c(Cl)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289164 25874 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 446 4 0 5 4.4 Cc1ccc2c(N3CCN(CCc4c(Cl)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
2543 10479 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
5358 10479 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
54 10479 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
CHEMBL128 10479 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
DB00669 10479 68 None 2 14 Human 7.4 pEC50 = 7.4 Functional
Effective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell linesEffective concentration determined by measuring inhibition of forskolin-stimulated c-AMP formation at 5-hydroxytryptamine 1B receptor stably transfected in CHO cell lines
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
24804774 26092 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 428 4 0 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290597 26092 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 428 4 0 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10809674 125974 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL343196 125974 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
5 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5202 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
CHEMBL39 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
DB08839 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full AgonistThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line; Full Agonist
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
5202 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
CHEMBL39 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
DB08839 6927 72 None -19 27 Human 8.3 pEC50 = 8.3 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
114 9034 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
6426760 9034 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
CHEMBL292779 9034 14 None -169 6 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm981133m
10503687 209856 0 None -50 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63799 209856 0 None -50 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 449 8 1 4 5.3 Fc1cccc(CCC2(F)CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10341917 174828 0 None -97 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
CHEMBL432332 174828 0 None -97 2 Human 6.4 pEC50 = 6.4 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.6 FC(Cc1c[nH]c2ccc(-n3cnnc3)cc12)CN1CCC(Cc2ccccc2)CC1 10.1021/jm981133m
10076876 108489 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
CHEMBL29951 108489 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
The intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell lineThe intrinsic activity was evaluated for its ability to inhibit forskolin-stimulated c-AMP formation mediated by cloned 5-hydroxytryptamine 1B receptor in CHO cell line
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
52943811 25854 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289047 25854 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 1 4 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
10551328 210500 0 None -97 2 Human 6.3 pEC50 = 6.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL67684 210500 0 None -97 2 Human 6.3 pEC50 = 6.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 445 8 1 4 5.7 CC(CC1(F)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
10837853 174937 0 None -309 2 Human 5.3 pEC50 = 5.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
CHEMBL433108 174937 0 None -309 2 Human 5.3 pEC50 = 5.3 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 464 8 1 5 4.3 CC(CN1CCN(CC(F)(F)Cc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm981133m
11 7970 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
124007 7970 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL304008 7970 19 None 75 4 Rat 7.3 pEC50 = 7.3 Functional
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
44592208 185958 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL472289 185958 0 None - 1 Human 8.2 pEC50 = 8.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
52948697 25855 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289048 25855 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assayAgonist activity at human 5-HT1B receptor expressed in CHO cells assessed as stimulation of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4c(C)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592332 185616 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 430 5 0 5 3.7 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469375 185616 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
Agonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assayAgonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay
ChEMBL 430 5 0 5 3.7 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
9844873 107835 0 None -48 2 Human 7.2 pEC50 = 7.2 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
CHEMBL294732 107835 0 None -48 2 Human 7.2 pEC50 = 7.2 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm981133m
2543 10479 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
5358 10479 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
54 10479 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
CHEMBL128 10479 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
DB00669 10479 68 None 2 14 Human 7.1 pEC50 = 7.1 Functional
Inhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cellsInhibition of forskolin-stimulated c-AMP formation by human 5-hydroxytryptamine 1B receptor expressed in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
10575553 209818 0 None -245 2 Human 6.1 pEC50 = 6.1 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
CHEMBL63432 209818 0 None -245 2 Human 6.1 pEC50 = 6.1 Functional
Agonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptorAgonist-induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with human 5-hydroxytryptamine 1B receptor
ChEMBL 450 8 1 5 3.6 Fc1cccc(CCN2CCN(CC(F)Cc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm981133m
10621021 210163 0 None -66 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
CHEMBL65367 210163 0 None -66 2 Human 8.0 pIC50 = 8.0 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
9844873 107835 0 None -48 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.7b01788
CHEMBL294732 107835 0 None -48 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 417 7 1 4 4.7 FC1(Cc2ccccc2)CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/acs.jmedchem.7b01788
18975369 107806 0 None -120 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
CHEMBL294547 107806 0 None -120 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assayInhibition of human 5HT1B expressed in CHO cells by [35S]-GTPgammaS binding assay
ChEMBL 399 7 1 4 4.6 c1ccc(CC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/acs.jmedchem.7b01788
145975946 170699 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4207355 170699 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 307 8 1 4 3.9 CCCCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
145964150 171085 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
CHEMBL4212246 171085 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at 5-HT1B receptor (unknown origin) by Tango assayAntagonist activity at 5-HT1B receptor (unknown origin) by Tango assay
ChEMBL 279 6 1 4 3.1 CCCCOc1ccc(C2=N[C@@H](CO)[C@H](C)S2)cc1 10.1021/acs.jnatprod.7b00317
146395245 195836 15 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 400 3 2 3 2.8 CC(=O)N1CCN([C@H]2CCC[C@@H](NC(=O)c3cc4c(F)ccc(C)c4[nH]3)C2)CC1 10.1021/acsmedchemlett.2c00167
CHEMBL5095235 195836 15 None 4 2 Human 5.5 pIC50 = 5.5 Functional
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 400 3 2 3 2.8 CC(=O)N1CCN([C@H]2CCC[C@@H](NC(=O)c3cc4c(F)ccc(C)c4[nH]3)C2)CC1 10.1021/acsmedchemlett.2c00167
11568826 139576 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 139576 0 None 9 2 Human 7.5 pIC50 = 7.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11662592 79119 0 None 15 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198463 79119 0 None 15 2 Human 7.1 pIC50 = 7.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
11655728 23416 8 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 23416 8 None - 0 Human 8.9 pKd = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
10447834 8714 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
4026 8714 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275507 8714 4 None - 3 Human 4.9 pKd = 4.9 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 305 7 2 2 3.7 NCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
44373817 18490 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1181270 18490 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL161046 18490 0 None - 0 Human 5.7 pKd = 5.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 298 2 1 3 3.2 CC(C)n1cc2c3c(cccc31)[C@H]1C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
44373789 18493 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1181275 18493 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL161368 18493 0 None - 0 Human 6.7 pKd = 6.7 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)C1=C[C@@H](CO)CN(C)[C@@H]1C2 10.1021/jm981092u
10403687 9289 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
1205 9289 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
CHEMBL275035 9289 3 None - 2 Human 5.1 pKd = 5.1 Functional
Compound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pigCompound was evaluated for its antagonist affinity towards 5-hydroxytryptamine 1B receptor of guinea pig
ChEMBL 319 8 2 2 3.9 CNCCc1cnc([nH]1)CCC(c1ccccc1)c1ccccc1 10.1021/jm991056a
44373791 19005 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL1184450 19005 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
CHEMBL349405 19005 0 None - 0 Human 6.1 pKd = 6.1 Functional
Affinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac arteryAffinity of compound towards 5-hydroxytryptamine 1B receptor in isolated guinea-pig iliac artery
ChEMBL 296 2 1 3 3.1 CC(C)n1cc2c3c(cccc31)[C@H]1C=C(CO)CN(C)[C@@H]1C2 10.1021/jm981092u
11797998 42466 0 None - 1 Human 10.0 pKi = 10 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL144030 42466 0 None - 1 Human 10.0 pKi = 10 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
44405730 175698 0 None - 0 Human 10.0 pKi = 10 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL438619 175698 0 None - 0 Human 10.0 pKi = 10 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccncc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10720301 46758 0 None - 1 Human 10.0 pKi = 10.0 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL147851 46758 0 None - 1 Human 10.0 pKi = 10.0 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 504 11 4 6 2.3 NCCc1c[nH]c2ccc(OCCN3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
10008868 127903 0 None - 1 Human 9.9 pKi = 9.9 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
CHEMBL357478 127903 0 None - 1 Human 9.9 pKi = 9.9 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 609 12 5 7 3.4 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(N4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)cc3)cc12 10.1021/jm960552l
11797158 46814 0 None - 1 Human 9.8 pKi = 9.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147901 46814 0 None - 1 Human 9.8 pKi = 9.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 11 5 5 2.2 NCCc1c[nH]c2ccc(OCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10837858 46580 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL147677 46580 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 464 12 6 5 2.4 NCCc1c[nH]c2ccc(OCCNC(=O)NCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
10531639 128050 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
CHEMBL357830 128050 0 None - 1 Human 9.7 pKi = 9.7 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 600 11 4 6 3.6 NCCc1c[nH]c2ccc(OCC(=O)N3CCC(C4CCN(C(=O)COc5ccc6[nH]cc(CCN)c6c5)CC4)CC3)cc12 10.1021/jm960552l
10791244 42571 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL144128 42571 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 490 12 4 6 2.7 NCCc1c[nH]c2ccc(OCCN3CCN(CCOc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
11800592 127763 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
CHEMBL356277 127763 0 None - 1 Human 9.6 pKi = 9.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 540 12 6 6 3.7 NCCc1c[nH]c2ccc(OCC(=O)Nc3ccc(NC(=O)COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 10.1021/jm960552l
10696930 42862 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL144397 42862 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 506 14 6 6 1.7 NCCc1c[nH]c2ccc(OCC(=O)NCCCNC(=O)COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
9868889 79404 0 None - 0 Human 9.5 pKi = 9.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL199443 79404 0 None - 0 Human 9.5 pKi = 9.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cccnc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10647387 46965 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
CHEMBL148022 46965 0 None - 1 Human 9.5 pKi = 9.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3cccc(COc4ccc5[nH]cc(CCN)c5c4)c3)cc12 10.1021/jm960552l
9984109 45651 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
CHEMBL146720 45651 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 518 10 4 6 1.8 NCCc1c[nH]c2ccc(OCC(=O)N3CCN(C(=O)COc4ccc5[nH]cc(CCN)c5c4)CC3)cc12 10.1021/jm960552l
9897637 125710 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
CHEMBL342323 125710 0 None - 1 Human 9.4 pKi = 9.4 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 828 25 6 8 7.2 NCCc1c[nH]c2ccc(OCCCCCCNS(=O)(=O)c3ccc(-c4ccc(S(=O)(=O)NCCCCCCOc5ccc6[nH]cc(CCN)c6c5)cc4)cc3)cc12 10.1021/jm960552l
44405669 78746 0 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 465 4 0 8 3.5 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccsc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197344 78746 0 None - 0 Human 9.4 pKi = 9.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 465 4 0 8 3.5 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccsc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10836606 172312 0 None - 1 Human 9.3 pKi = 9.3 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL424128 172312 0 None - 1 Human 9.3 pKi = 9.3 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 434 13 4 4 4.7 NCCc1c[nH]c2ccc(OCCCCCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405725 78610 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1c(Cl)cccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196914 78610 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1c(Cl)cccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464649 79224 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 459 4 0 7 3.4 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198836 79224 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 459 4 0 7 3.4 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405666 79648 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 451 4 0 8 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6c5OCC6)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL200315 79648 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 451 4 0 8 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6c5OCC6)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
9933975 140365 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5nccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL371221 140365 0 None - 0 Human 9.3 pKi = 9.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5nccc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900954 23424 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242081 23424 0 None - 0 Human 9.3 pKi = 9.3 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 6 1 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900776 23411 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241824 23411 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 5 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900956 23426 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242167 23426 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 6 1 7 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
52942551 26072 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 400 4 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290486 26072 0 None - 0 Human 9.2 pKi = 9.2 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 400 4 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
46900459 23410 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241738 23410 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnc(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
52947615 25908 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289394 25908 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
52947414 26073 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 0 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290487 26073 0 None - 0 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 414 4 0 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4CCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
24804775 26115 0 None - 2 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290716 26115 0 None - 2 Human 9.1 pKi = 9.1 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 412 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44405702 79355 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cnccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL199269 79355 0 None - 0 Human 9.1 pKi = 9.1 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6cnccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900455 23405 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241641 23405 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 493 4 0 6 5.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C(F)(F)F)cn4-5)CC3)cccc2n1 10.1021/jm100482n
46900457 23406 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241642 23406 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4cncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900612 23408 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241736 23408 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 467 5 0 7 4.2 CC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46899639 23441 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242533 23441 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 5 0 7 4.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
11720815 23456 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 538 5 0 8 3.5 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCOCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242717 23456 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 538 5 0 8 3.5 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCOCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44138098 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL513715 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1021/jm100482n
44138098 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL513715 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44138098 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513715 196251 0 None - 0 Human 9.0 pKi = 9 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44405573 78632 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 485 5 0 7 3.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5-c5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197007 78632 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 485 5 0 7 3.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5-c5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405574 79210 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 501 6 0 8 4.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Oc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198792 79210 0 None - 0 Human 9.0 pKi = 9.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 501 6 0 8 4.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Oc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
44405575 79269 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 7 0 8 3.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198999 79269 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 7 0 8 3.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCc5ccccc5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900610 23404 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 497 6 0 8 4.2 CCOC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241640 23404 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 497 6 0 8 4.2 CCOC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
11712756 23415 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241912 23415 0 None - 0 Human 8.9 pKi = 8.9 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 482 5 1 7 3.3 CNC(=O)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
22464842 78592 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 434 4 0 8 2.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5C#N)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL196862 78592 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 434 4 0 8 2.1 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5C#N)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
9872238 79289 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 439 5 0 8 2.3 COc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL199049 79289 0 None - 0 Human 8.9 pKi = 8.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 439 5 0 8 2.3 COc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
46900451 23398 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241547 23398 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 439 4 0 6 4.3 Cc1cn2c(n1)COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900778 23412 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 450 4 0 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C#N)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241825 23412 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 450 4 0 7 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C#N)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
11655728 23416 8 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 23416 8 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899637 23432 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242345 23432 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 522 7 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NCC6CC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899638 23436 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242436 23436 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 508 5 0 7 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46899640 23448 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 5 0 7 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242623 23448 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 5 0 7 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)N6CCCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
46900150 23468 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242904 23468 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 425 4 0 6 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nccn4-5)CC3)cccc2n1 10.1021/jm100482n
44138104 185612 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL469345 185612 0 None - 0 Human 8.8 pKi = 8.8 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
11797999 47299 0 None - 1 Human 8.8 pKi = 8.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL148314 47299 0 None - 1 Human 8.8 pKi = 8.8 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccccc3COc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405701 78706 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ncccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL197240 78706 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cccc6ncccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22464720 79176 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 443 4 0 7 2.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Cl)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198696 79176 0 None - 0 Human 8.8 pKi = 8.8 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 443 4 0 7 2.9 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5Cl)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900453 23399 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241548 23399 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 453 4 0 6 4.6 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nc(C)c(C)n4-5)CC3)cccc2n1 10.1021/jm100482n
46900958 23431 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1242257 23431 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 536 6 1 7 4.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC6CCCC6)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
9979309 199761 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL522257 199761 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
52942644 26114 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 398 4 1 4 3.7 Cc1ccc2c(N3CCN(CCc4cccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1290715 26114 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 398 4 1 4 3.7 Cc1ccc2c(N3CCN(CCc4cccc5[nH]c(=O)ccc45)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592297 196269 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL513875 196269 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 4 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
9979309 199761 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL522257 199761 0 None - 0 Human 8.7 pKi = 8.7 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
14519851 123526 39 None - 0 Human 7.0 pKi = 7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 187 3 1 2 2.2 NCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL337539 123526 39 None - 0 Human 7.0 pKi = 7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 187 3 1 2 2.2 NCCOc1cccc2ccccc12 10.1021/jm970507t
2261792 123225 6 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 231 6 2 3 1.8 OCCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL336092 123225 6 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 231 6 2 3 1.8 OCCNCCOc1cccc2ccccc12 10.1021/jm970507t
44405655 78653 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 453 5 0 8 2.6 COc1ccc(C)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197064 78653 0 None - 0 Human 7.9 pKi = 7.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 453 5 0 8 2.6 COc1ccc(C)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10584924 37183 0 None - 0 Human 6.0 pKi = 6.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 218 5 2 2 2.5 CC(C)NCCOc1cccc2[nH]ccc12 10.1021/jm970507t
CHEMBL139230 37183 0 None - 0 Human 6.0 pKi = 6.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 218 5 2 2 2.5 CC(C)NCCOc1cccc2[nH]ccc12 10.1021/jm970507t
22464806 78619 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 6 0 8 3.9 COc1ccc(-c2ccccc2)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196961 78619 0 None - 0 Human 6.9 pKi = 6.9 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 515 6 0 8 3.9 COc1ccc(-c2ccccc2)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10775772 36880 2 None - 0 Human 6.9 pKi = 6.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 1 2 3.2 CC(C)NCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138963 36880 2 None - 0 Human 6.9 pKi = 6.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 1 2 3.2 CC(C)NCCOc1cccc2ccccc12 10.1021/jm970507t
10588458 34384 0 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 275 8 0 2 4.5 CCCN(C)CCCOc1ccccc1C1CCCC1 10.1021/jm970507t
CHEMBL136962 34384 0 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 275 8 0 2 4.5 CCCN(C)CCCOc1ccccc1C1CCCC1 10.1021/jm970507t
6422277 36809 5 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138907 36809 5 None - 0 Human 5.9 pKi = 5.9 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 271 8 0 2 4.3 CCCCN(CC)CCOc1cccc2ccccc12 10.1021/jm970507t
44592295 185788 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL471047 185788 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592252 195973 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 466 6 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC(F)F)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL511279 195973 0 None - 0 Human 7.8 pKi = 7.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 466 6 0 5 3.9 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC(F)F)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592335 185704 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 462 5 0 5 4.2 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL470217 185704 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 462 5 0 5 4.2 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
10518850 41967 0 None - 0 Human 7.8 pKi = 7.8 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143512 41967 0 None - 0 Human 7.8 pKi = 7.8 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 308 4 2 4 1.9 NCCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10809674 125974 0 None - 1 Human 8.6 pKi = 8.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
CHEMBL343196 125974 0 None - 1 Human 8.6 pKi = 8.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 378 9 4 4 3.1 NCCc1c[nH]c2ccc(OCCOc3ccc4[nH]cc(CCN)c4c3)cc12 10.1021/jm960552l
44405586 78617 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 467 6 0 8 3.1 CC(C)Oc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196958 78617 0 None - 0 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 467 6 0 8 3.1 CC(C)Oc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
11568826 139576 0 None 9 2 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 139576 0 None 9 2 Human 8.6 pKi = 8.6 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
46900606 23397 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241546 23397 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 440 4 0 7 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C)nnn4-5)CC3)cccc2n1 10.1021/jm100482n
46900614 23409 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 6 0 8 4.4 CO/N=C(\C)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
CHEMBL1241737 23409 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 496 6 0 8 4.4 CO/N=C(\C)c1ncn2c1COc1c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc1-2 10.1021/jm100482n
46900782 23420 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241998 23420 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 510 6 1 7 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(=O)NC(C)C)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
44592296 185615 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469374 185615 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 434 4 0 5 3.4 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
44592294 196042 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL511815 196042 0 None - 0 Human 8.6 pKi = 8.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 4 0 5 3.7 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2009.02.056
10585509 36526 2 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 6 1 2 3.2 CCCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138683 36526 2 None - 0 Human 6.7 pKi = 6.7 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 6 1 2 3.2 CCCNCCOc1cccc2ccccc12 10.1021/jm970507t
2543 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
5358 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
54 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
CHEMBL128 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
DB00669 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm960552l
2543 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
5358 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
54 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
CHEMBL128 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
DB00669 10479 68 None 2 14 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
9909089 193747 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL490417 193747 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1021/jm100482n
9909089 193747 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL490417 193747 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
23274477 35894 1 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138136 35894 1 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 229 5 0 2 3.2 CN(C)CCCOc1cccc2ccccc12 10.1021/jm970507t
2199302 36872 25 None - 0 Human 7.6 pKi = 7.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.4 CNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL138958 36872 25 None - 0 Human 7.6 pKi = 7.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.4 CNCCOc1cccc2ccccc12 10.1021/jm970507t
1328538 38358 8 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 291 6 0 2 4.4 CN(CCOc1cccc2ccccc12)Cc1ccccc1 10.1021/jm970507t
CHEMBL140416 38358 8 None - 0 Human 6.6 pKi = 6.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 291 6 0 2 4.4 CN(CCOc1cccc2ccccc12)Cc1ccccc1 10.1021/jm970507t
2176 9901 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
4828 9901 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
91 9901 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
CHEMBL500 9901 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
DB00960 9901 68 None - 8 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm970507t
14519863 121979 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL334465 121979 1 None - 0 Human 5.6 pKi = 5.6 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm970507t
9802530 42160 1 None -11 2 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143767 42160 1 None -11 2 Human 7.6 pKi = 7.6 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
14566707 125869 42 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.6 NCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL342704 125869 42 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 201 4 1 2 2.6 NCCCOc1cccc2ccccc12 10.1021/jm970507t
10365683 119855 0 None - 0 Human 8.5 pKi = 8.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 7 3 5 2.4 CC(=O)Nc1ccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)cc1 10.1021/jm960552l
CHEMBL331240 119855 0 None - 0 Human 8.5 pKi = 8.5 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 435 7 3 5 2.4 CC(=O)Nc1ccc(N2CCN(C(=O)COc3ccc4[nH]cc(CCN)c4c3)CC2)cc1 10.1021/jm960552l
44405677 78620 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1cc(Cl)ccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL196962 78620 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1cc(Cl)ccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464831 78658 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 423 4 0 7 2.6 Cc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197078 78658 0 None - 0 Human 8.5 pKi = 8.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 423 4 0 7 2.6 Cc1ccccc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
22464606 78782 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1c(Cl)cc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197445 78782 0 None - 0 Human 8.4 pKi = 8.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1c(Cl)cc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
44138104 185612 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
CHEMBL469345 185612 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1021/jm100482n
44138104 185612 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469345 185612 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 416 4 0 5 3.3 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592209 185959 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
CHEMBL472290 185959 0 None - 0 Human 8.4 pKi = 8.4 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 430 5 0 5 3.7 CCN1C(=O)COc2c(CCN3CCN(c4cccc5nc(C)ccc45)CC3)cccc21 10.1016/j.bmcl.2009.02.056
52943861 25873 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 430 4 0 5 3.9 Cc1ccc2c(N3CCN(CCc4c(F)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289163 25873 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 430 4 0 5 3.9 Cc1ccc2c(N3CCN(CCc4c(F)ccc5c4ccc(=O)n5C)CC3)cccc2n1 10.1016/j.bmcl.2010.09.085
44592207 196142 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL512724 196142 0 None - 0 Human 7.5 pKi = 7.5 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 402 4 1 5 3.2 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
10654938 85593 11 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 179 4 1 2 1.9 CNCCOc1cccc(C)c1C 10.1021/jm970507t
CHEMBL2112766 85593 11 None - 0 Human 6.5 pKi = 6.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 179 4 1 2 1.9 CNCCOc1cccc(C)c1C 10.1021/jm970507t
52947622 25925 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1289510 25925 0 None - 0 Human 6.5 pKi = 6.5 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 444 4 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cc(F)cc2n1 10.1016/j.bmcl.2010.09.085
22464564 78607 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 461 4 0 9 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5ncnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL196907 78607 0 None - 0 Human 6.5 pKi = 6.5 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 461 4 0 9 2.2 CN1CCc2c(sc3ncn(CCN4CCN(c5ncnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22067856 36313 52 None - 0 Human 5.5 pKi = 5.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm970507t
CHEMBL138509 36313 52 None - 0 Human 5.5 pKi = 5.5 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm970507t
22464634 79798 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccc6ccccc6n5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL200951 79798 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccc6ccccc6n5)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
10618751 41964 0 None -25 2 Human 7.4 pKi = 7.4 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143510 41964 0 None -25 2 Human 7.4 pKi = 7.4 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
52944840 25750 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2010.09.085
CHEMBL1287827 25750 0 None - 0 Human 6.4 pKi = 6.4 Functional
Antagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assayAntagonist activity at human 5-HT1B receptor expressed in CHO cells assessed as inhibition of GTPgammaS binding by scintillation proximity assay
ChEMBL 426 4 0 5 4.1 Cc1ccc2c(N3CCN(CCc4cccc5c4ccc(=O)n5C)[C@@H](C)C3)cccc2n1 10.1016/j.bmcl.2010.09.085
44405726 78740 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1cc(Cl)c(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL197338 78740 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.6 COc1cc(Cl)c(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
2303 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
4946 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
564 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
63 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
91536 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
CHEMBL27 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
CHEMBL452861 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
DB00571 9961 68 None - 20 Human 5.4 pKi = 5.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm970507t
44405665 79796 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.3 COc1ccc(C(F)(F)F)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL200949 79796 0 None - 0 Human 7.4 pKi = 7.4 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 507 5 0 8 3.3 COc1ccc(C(F)(F)F)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
10635169 38356 0 None - 0 Human 6.4 pKi = 6.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 261 7 0 2 4.1 CCCN(C)CCOc1ccccc1C1CCCC1 10.1021/jm970507t
CHEMBL140415 38356 0 None - 0 Human 6.4 pKi = 6.4 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 261 7 0 2 4.1 CCCN(C)CCOc1ccccc1C1CCCC1 10.1021/jm970507t
13520547 33777 1 None - 0 Human 6.3 pKi = 6.3 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL136470 33777 1 None - 0 Human 6.3 pKi = 6.3 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CN(C)CCCCOc1cccc2ccccc12 10.1021/jm970507t
44592249 185630 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C(C)C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469567 185630 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 444 5 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C(C)C)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
44592250 185631 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469568 185631 0 None - 0 Human 8.3 pKi = 8.3 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 442 5 0 5 3.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5C4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
22464804 79797 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 489 5 0 8 3.4 COc1ccc2ccccc2c1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL200950 79797 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 489 5 0 8 3.4 COc1ccc2ccccc2c1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
44405587 140343 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 495 6 0 8 3.7 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCC(C)(C)C)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL371094 140343 0 None - 0 Human 8.3 pKi = 8.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 495 6 0 8 3.7 CN1CCc2c(sc3ncn(CCN4CCN(c5ccccc5OCC(C)(C)C)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
22464614 78633 0 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 469 6 0 9 2.3 COc1ccc(OC)c(N2CCN(CCn3cnc4sc5c(c4c3=O)CCN(C)C5)CC2)c1 10.1016/j.bmcl.2005.04.077
CHEMBL197011 78633 0 None - 0 Human 7.3 pKi = 7.3 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 469 6 0 9 2.3 COc1ccc(OC)c(N2CCN(CCn3cnc4sc5c(c4c3=O)CCN(C)C5)CC2)c1 10.1016/j.bmcl.2005.04.077
37732 33596 73 None - 0 Human 5.2 pKi = 5.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 151 4 1 2 1.3 CNCCOc1ccccc1 10.1021/jm970507t
CHEMBL136311 33596 73 None - 0 Human 5.2 pKi = 5.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 151 4 1 2 1.3 CNCCOc1ccccc1 10.1021/jm970507t
44592251 185686 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 456 6 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469995 185686 0 None - 0 Human 8.2 pKi = 8.2 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 456 6 0 5 4.0 Cc1ccc2c(N3CCN(CCc4cccc5c4OCC(=O)N5CC4CC4)CC3)cccc2n1 10.1016/j.bmcl.2009.02.056
5 6927 72 None -19 27 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
5202 6927 72 None -19 27 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
CHEMBL39 6927 72 None -19 27 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
DB08839 6927 72 None -19 27 Human 8.2 pKi = 8.2 Functional
Ability to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cellsAbility to inhibit the forskolin-stimulated c-AMP formation mediated by human 5-hydroxytryptamine 1B receptor in CHO-K1 cells
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm960552l
10560632 33505 1 None - 0 Human 7.2 pKi = 7.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 5 1 2 2.8 CCNCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL136236 33505 1 None - 0 Human 7.2 pKi = 7.2 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 5 1 2 2.8 CCNCCOc1cccc2ccccc12 10.1021/jm970507t
46900608 23403 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 427 4 0 8 2.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnnn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241639 23403 0 None - 0 Human 8.1 pKi = 8.1 Functional
Antagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assayAntagonist activity against human recombinant 5HT1B receptor expressed in CHO cells assessed as inhibition of 5HT-induced [35S]GTPgammaS binding by scintillation proximity assay
ChEMBL 427 4 0 8 2.8 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4nnnn4-5)CC3)cccc2n1 10.1021/jm100482n
22002244 79118 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1ccc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
CHEMBL198462 79118 0 None - 0 Human 7.2 pKi = 7.2 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 473 5 0 8 2.9 COc1ccc(Cl)cc1N1CCN(CCn2cnc3sc4c(c3c2=O)CCN(C)C4)CC1 10.1016/j.bmcl.2005.04.077
14519865 38361 1 None - 0 Human 6.1 pKi = 6.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL140417 38361 1 None - 0 Human 6.1 pKi = 6.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
10263828 37646 17 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 1 2 3.6 CC(C)NCCCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL139737 37646 17 None - 0 Human 5.1 pKi = 5.1 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 243 6 1 2 3.6 CC(C)NCCCOc1cccc2ccccc12 10.1021/jm970507t
44592334 185636 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 5 0 5 3.8 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
CHEMBL469589 185636 0 None - 0 Human 6.1 pKi = 6.1 Functional
Antagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HTAntagonist activity at human 5HT1B assessed as GTPgammaS binding by scintillation proximity assay in presence of 5-HT
ChEMBL 448 5 0 5 3.8 Cc1ccc2c(N3CCN(CCCc4cccc5c4OCC(=O)N5C)CC3)cc(F)cc2n1 10.1016/j.bmcl.2009.02.056
10691904 42394 0 None -3 2 Human 7.1 pKi = 7.1 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143967 42394 0 None -3 2 Human 7.1 pKi = 7.1 Functional
Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.Compound was tested for intrinsic efficacy against human 5-hydroxytryptamine 1D receptor beta measured as the reduction of forskolin-stimulated cAMP.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
11662592 79119 0 None 15 2 Human 8.0 pKi = 8.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL198463 79119 0 None 15 2 Human 8.0 pKi = 8.0 Functional
Inhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPRInhibitory activity against human recombinant 5HT1B receptor co-expressed with G-protein chimera Gqo5 in HEK293 cells by FLIPR
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5ccnc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
3604129 37037 5 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
CHEMBL139103 37037 5 None - 0 Human 7.0 pKi = 7.0 Functional
Agonist activity to the human recombinant 5-hydroxytryptamine 1B receptorAgonist activity to the human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 215 4 0 2 2.8 CN(C)CCOc1cccc2ccccc12 10.1021/jm970507t
2105 9828 37 None 1 24 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 None 1 24 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 None 1 24 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 None 1 24 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 None 1 24 Human 8.2 pEC50 = 8.2 Functional
NoneNone
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
4223 10764 94 None -707 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
6918314 10764 94 None -707 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
7427 10764 94 None -707 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
CHEMBL439849 10764 94 None -707 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
DB06684 10764 94 None -707 15 Rat 8.3 pIC50 = 8.3 Functional
Inhibition of rat hydroxytryptamine 1B receptorInhibition of rat hydroxytryptamine 1B receptor
Drug Central 441 7 2 5 4.0 N#Cc1ccc2c(c1)c(CCCCN1CCN(CC1)c1ccc3c(c1)cc(o3)C(=O)N)c[nH]2 None
1220 6975 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
31 6975 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
7 6975 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
CHEMBL56 6975 55 None -109 9 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 9303569
137 6926 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048565 6926 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
7048566 6926 0 None -1 2 Human 11.9 pIC50 None 11.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9774213
1524 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
1524 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
197 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
197 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
3822 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
3822 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
88 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
88 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
CHEMBL51 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
CHEMBL51 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
DB12465 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9303569
DB12465 8962 96 None -125 18 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 9605573
5074 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
5074 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
97 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
97 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
CHEMBL267777 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
CHEMBL267777 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
DB12693 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9303569
DB12693 10105 80 None -33 8 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F 9605573
16 9033 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
9847194 9033 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
CHEMBL313714 9033 8 None -177 5 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10585208
46 9680 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
71351 9680 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
CHEMBL2104619 9680 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
DB06229 9680 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 420 4 0 6 4.0 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2C 9605573
110 7957 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
132552 7957 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
CHEMBL159332 7957 18 None -1 2 Human 7.6 pIC50 None 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 9303569
113 8633 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
128018 8633 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546
CHEMBL119264 8633 14 None - 1 Human 7.4 pKB = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 11888546




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
19066203 18861 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1183904 18861 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL323986 18861 0 None 47 3 Human 8.7 pEC50 = 8.7 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3ccc(C)cc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
19066163 18158 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL111302 18158 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1180017 18158 0 None 28 3 Human 8.0 pEC50 = 8 Binding
The compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptorThe compound was evaluated for intrinsic activity against human cloned 5-hydroxytryptamine 1B receptor
ChEMBL 437 4 1 5 3.4 COc1ccc(NC(=O)N2CCN(c3c(C)cccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
5 6927 72 None -13 53 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
5202 6927 72 None -13 53 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL39 6927 72 None -13 53 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
DB08839 6927 72 None -13 53 Rat 7.6 pEC50 = 7.6 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigraInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1B receptor of rat substantia nigra
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL5078078 221314 7 None - 0 Human 5.6 pEC50 = 5.6 Binding
Safety47 Scan (DiscoverX - Eurofins)Safety47 Scan (DiscoverX - Eurofins)
ChEMBL None None None CC(C)(O)c1ccc(N2Cc3c(ccnc3-c3ccc(F)cc3OCC(F)(F)F)C2=O)cc1 10.6019/CHEMBL5303768
5 6927 72 None -11 53 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
5202 6927 72 None -11 53 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
CHEMBL39 6927 72 None -11 53 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
DB08839 6927 72 None -11 53 Human 7.5 pEC50 = 7.5 Binding
Inhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampusInhibition of Forskolin-stimulated adenylate cyclase activity against 5-hydroxytryptamine 1A receptor of guinea pig hippocampus
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00170a007
137634921 163029 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 586 3 2 9 4.5 O=C1CCc2cc3cc(c2N1Cc1ccccc1)OC/C=C/CO[C@H]1C[C@@H](CO)N(C1)c1cc(n2ncc(Cl)c2n1)N3 10.1021/acs.jmedchem.7b00359
CHEMBL4064865 163029 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
Agonist activity at 5-HT1B receptor (unknown origin)Agonist activity at 5-HT1B receptor (unknown origin)
ChEMBL 586 3 2 9 4.5 O=C1CCc2cc3cc(c2N1Cc1ccccc1)OC/C=C/CO[C@H]1C[C@@H](CO)N(C1)c1cc(n2ncc(Cl)c2n1)N3 10.1021/acs.jmedchem.7b00359
11539632 77336 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
CHEMBL194837 77336 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibitory concentration against 5-hydroxytryptamine 1B receptorInhibitory concentration against 5-hydroxytryptamine 1B receptor
ChEMBL 447 8 1 5 4.8 Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12 10.1021/jm050103y
1043 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
3251 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1982133 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None 4 29 Rat 9.7 pIC50 = 9.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
9952249 59446 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 388 6 1 7 2.3 c1cnc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
CHEMBL159396 59446 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 388 6 1 7 2.3 c1cnc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
9846928 46453 15 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 457 6 3 5 4.0 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=N)N)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL147503 46453 15 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 457 6 3 5 4.0 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=N)N)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
2543 10479 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
5358 10479 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
54 10479 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
CHEMBL128 10479 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
DB00669 10479 68 None -3 32 Human 9.3 pIC50 = 9.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm000956k
11333554 103436 22 None - 1 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26379 103436 22 None - 1 Rat 9.1 pIC50 = 9.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 223 1 2 2 2.4 N#Cc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
10531 8202 21 None -5 24 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -5 24 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -5 24 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -5 24 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -5 24 Rat 9.1 pIC50 = 9.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
10323598 45673 21 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL146735 45673 21 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
15646678 103434 27 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 214 1 3 2 2.3 Oc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26378 103434 27 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 214 1 3 2 2.3 Oc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
9881526 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
CHEMBL296161 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
9881526 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
CHEMBL296161 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
10718709 46058 19 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 458 6 2 5 3.8 COc1ccc(NC(=O)c2ccc(-c3ccc(C(N)=O)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL147071 46058 19 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 458 6 2 5 3.8 COc1ccc(NC(=O)c2ccc(-c3ccc(C(N)=O)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
9881526 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9704558
CHEMBL296161 108025 1 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 255 4 1 4 1.9 CN(C)CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9704558
107780 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
14 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
CHEMBL15928 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm9811054
107780 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
14 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
CHEMBL15928 8625 54 None -4 18 Rat 8.8 pIC50 = 8.8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
11344959 104068 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 216 1 2 1 2.7 Fc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL26906 104068 38 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 216 1 2 1 2.7 Fc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
2543 10479 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
5358 10479 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
54 10479 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
CHEMBL128 10479 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
DB00669 10479 68 None -3 32 Human 8.0 pIC50 = 8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9910021
1588 9105 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None -58 44 Rat 8.0 pIC50 = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10552663 127917 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127917 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 50815 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 50815 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 46762 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.3 OC[C@@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL147853 46762 0 None - 0 Human 7.0 pIC50 = 7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.3 OC[C@@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10076176 113212 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 113212 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 113212 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 48750 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 48750 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 175086 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 175086 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 16994 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 16994 0 None - 0 Human 7.0 pIC50 = 7 Binding
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 209506 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 209506 0 None - 0 Rat 6.0 pIC50 = 6 Binding
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 129758 0 None - 5 Human 6.0 pIC50 = 6 Binding
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 129758 0 None - 5 Human 6.0 pIC50 = 6 Binding
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 10425 50 None -43651 58 Rat 6.0 pIC50 = 6 Binding
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 10425 50 None -43651 58 Rat 6.0 pIC50 = 6 Binding
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 10425 50 None -43651 58 Rat 6.0 pIC50 = 6 Binding
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 10425 50 None -43651 58 Rat 6.0 pIC50 = 6 Binding
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 10425 50 None -43651 58 Rat 6.0 pIC50 = 6 Binding
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 20503 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 20503 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 20503 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 106245 0 None - 1 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 106245 0 None - 1 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 106245 0 None - 1 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 204254 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 204254 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 204254 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Binding affinity for 5-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 209790 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 209790 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 209818 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 209818 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 210149 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 210149 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 104165 0 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 104165 0 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 104165 0 None - 1 Rat 5.0 pIC50 = 5 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
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 16938 7 None - 1 Rat 5.0 pIC50 = 5 Binding
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 108648 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 108648 0 None - 0 Rat 5.0 pIC50 = 5 Binding
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 74727 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 74727 0 None - 0 Human 5.0 pIC50 = 5 Binding
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 106524 0 None - 1 Rat 4.0 pIC50 = 4 Binding
Binding affinity for 5-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 106524 0 None - 1 Rat 4.0 pIC50 = 4 Binding
Binding affinity for 5-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 63331 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 471 8 1 6 3.1 CN(C)C(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL164035 63331 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 471 8 1 6 3.1 CN(C)C(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
9863146 201771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 201771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 201771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 201771 1 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 210211 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 210211 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 7516 40 None -48 35 Rat 7.0 pIC50 = 7.0 Binding
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 7516 40 None -48 35 Rat 7.0 pIC50 = 7.0 Binding
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 7516 40 None -48 35 Rat 7.0 pIC50 = 7.0 Binding
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 7516 40 None -48 35 Rat 7.0 pIC50 = 7.0 Binding
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 7516 40 None -48 35 Rat 7.0 pIC50 = 7.0 Binding
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 119867 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 119867 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
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 210115 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 210115 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
5358 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
54 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
CHEMBL128 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
DB00669 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980569z
10621021 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL65367 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 400 7 1 5 3.5 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
2543 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
5358 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
54 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
CHEMBL128 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
DB00669 10479 68 None -3 32 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805687
10789334 172120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 8 1 5 3.7 CC(=O)N(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL423599 172120 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 442 8 1 5 3.7 CC(=O)N(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10621021 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 210163 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
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 10479 68 None -17 32 Rat 7.0 pIC50 = 7.0 Binding
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 10479 68 None -17 32 Rat 7.0 pIC50 = 7.0 Binding
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 10479 68 None -17 32 Rat 7.0 pIC50 = 7.0 Binding
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 10479 68 None -17 32 Rat 7.0 pIC50 = 7.0 Binding
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 10479 68 None -17 32 Rat 7.0 pIC50 = 7.0 Binding
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 18179 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL118012 18179 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10787241 61366 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)ccn1 10.1021/jm9805687
CHEMBL161066 61366 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)ccn1 10.1021/jm9805687
10788620 46821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46821 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 8334 25 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 8334 25 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 8334 25 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 132167 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 132167 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
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 171706 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 171706 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 85147 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 85147 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 121985 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 121985 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 96045 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96045 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 210245 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 210245 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
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 105090 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 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 105090 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 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 18179 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
CHEMBL118012 18179 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 444 9 3 6 3.5 OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
5 6927 72 None -11 53 Human 7.9 pIC50 = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pIC50 = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pIC50 = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pIC50 = 7.9 Binding
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 96476 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 96476 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 126682 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 390 8 2 6 3.0 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)co1 10.1021/jm9805687
CHEMBL349185 126682 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 390 8 2 6 3.0 c1cc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)co1 10.1021/jm9805687
10838684 125918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 487 10 3 7 3.6 NC(=O)OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL342805 125918 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 487 10 3 7 3.6 NC(=O)OC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10814424 105780 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 475 6 2 4 4.8 COc1ccc(NC(=O)N2CCC(CCc3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL280000 105780 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 475 6 2 4 4.8 COc1ccc(NC(=O)N2CCC(CCc3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10574762 16915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL115750 16915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10597901 17425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 17425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 16915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 16915 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 126166 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 126166 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 169239 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 169239 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 209818 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 209818 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 96052 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96052 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 17425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704558
CHEMBL117046 17425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 414 8 2 5 3.9 c1ccc(CNC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9704558
10740531 126644 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 9 2 5 3.4 c1ccc(CCNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL348815 126644 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 9 2 5 3.4 c1ccc(CCNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
2477 7532 59 None -16 29 Rat 4.9 pIC50 = 4.9 Binding
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 7532 59 None -16 29 Rat 4.9 pIC50 = 4.9 Binding
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 7532 59 None -16 29 Rat 4.9 pIC50 = 4.9 Binding
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 7532 59 None -16 29 Rat 4.9 pIC50 = 4.9 Binding
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 7532 59 None -16 29 Rat 4.9 pIC50 = 4.9 Binding
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 201488 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 201488 0 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 7590 103 None -100 22 Rat 5.9 pIC50 = 5.9 Binding
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 7590 103 None -100 22 Rat 5.9 pIC50 = 5.9 Binding
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 7590 103 None -100 22 Rat 5.9 pIC50 = 5.9 Binding
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 7590 103 None -100 22 Rat 5.9 pIC50 = 5.9 Binding
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 7590 103 None -100 22 Rat 5.9 pIC50 = 5.9 Binding
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 62789 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 386 6 1 5 3.5 c1ccc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL162463 62789 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 386 6 1 5 3.5 c1ccc(N2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
44214559 63272 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163462 63272 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10573843 126925 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 4.1 CC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL351346 126925 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 4.1 CC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10504600 46722 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46722 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 86305 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 86305 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 108804 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 108804 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 108804 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 108804 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 126515 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 425 7 1 6 3.4 N#Cc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL347665 126515 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 425 7 1 6 3.4 N#Cc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
9911120 16395 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 16395 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 125539 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 125539 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 209887 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 209887 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 201516 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 201516 1 None - 0 Rat 4.9 pIC50 = 4.9 Binding
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 126746 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 126746 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 105685 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 10 3 5 4.3 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
CHEMBL279320 105685 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 497 10 3 5 4.3 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
10612178 126643 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 126643 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 56995 42 None -38 11 Rat 4.9 pIC50 = 4.9 Binding
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 56995 42 None -38 11 Rat 4.9 pIC50 = 4.9 Binding
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 56995 42 None -38 11 Rat 4.9 pIC50 = 4.9 Binding
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 10625 55 None -6 43 Rat 5.9 pIC50 = 5.9 Binding
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 10625 55 None -6 43 Rat 5.9 pIC50 = 5.9 Binding
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 10625 55 None -6 43 Rat 5.9 pIC50 = 5.9 Binding
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 10625 55 None -6 43 Rat 5.9 pIC50 = 5.9 Binding
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 10625 55 None -6 43 Rat 5.9 pIC50 = 5.9 Binding
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 7293 81 None -35 42 Rat 5.9 pIC50 = 5.9 Binding
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 7293 81 None -35 42 Rat 5.9 pIC50 = 5.9 Binding
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 7293 81 None -35 42 Rat 5.9 pIC50 = 5.9 Binding
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 7293 81 None -35 42 Rat 5.9 pIC50 = 5.9 Binding
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 7293 81 None -35 42 Rat 5.9 pIC50 = 5.9 Binding
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 168346 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 168346 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
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 126036 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 126036 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 209778 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 209778 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 7957 18 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
132552 7957 18 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
CHEMBL159332 7957 18 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 321 5 2 3 1.9 CNS(=O)(=O)Cc1ccc2c(c1)c(c[nH]2)C[C@H]1CCCN1C 10.1021/jm000956k
10718714 44916 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.3 OC[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146131 44916 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.3 OC[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
73351905 96477 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 96477 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
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 45665 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45665 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45859 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47311 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47311 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 109494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 109494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 172061 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 172061 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 109494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 109494 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 54514 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 54514 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
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 110239 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 110239 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 170056 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 170056 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 169226 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 169226 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 109494 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
CHEMBL304857 109494 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 428 8 1 5 4.3 CN(Cc1ccccc1)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
10614907 104961 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 310 5 2 5 1.6 c1cc2[nH]cc(CCCN3CCNCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL274001 104961 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 310 5 2 5 1.6 c1cc2[nH]cc(CCCN3CCNCC3)c2cc1-n1cnnc1 10.1021/jm980569z
9930155 170811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL420874 170811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
9930155 170811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420874 170811 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
11792032 209600 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 209600 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
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 120105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL331612 120105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
150 9287 21 None -6 16 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9287 21 None -6 16 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9287 21 None -6 16 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9287 21 None -6 16 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9287 21 None -6 16 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 107835 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 107835 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 120105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL331612 120105 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 309 5 1 4 3.2 c1cc2[nH]cc(CCCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10597902 59774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 1 5 3.9 CN(Cc1ccccc1)C[C@@H]1CCCN1CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
CHEMBL159683 59774 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 1 5 3.9 CN(Cc1ccccc1)C[C@@H]1CCCN1CCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm9805687
9844873 107835 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 107835 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 7970 19 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
124007 7970 19 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL304008 7970 19 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 215 1 3 2 1.2 O=c1ccc2c([nH]1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
10766319 45532 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.9 OCCC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146628 45532 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 3 6 3.9 OCCC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
16 9033 8 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 9033 8 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 9033 8 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 7689 31 None - 7 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
2689 7689 31 None - 7 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
CHEMBL27403 7689 31 None - 7 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10.1021/jm00170a007
10753377 201502 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 201502 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 61881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 61881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 16627 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 16627 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
5358 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
54 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
CHEMBL128 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
DB00669 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9704558
2543 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
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 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
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 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
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 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
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 10479 68 None -3 32 Human 7.8 pIC50 = 7.8 Binding
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 210460 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 210460 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
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 6927 72 None -11 53 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
5202 6927 72 None -11 53 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
CHEMBL39 6927 72 None -11 53 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
DB08839 6927 72 None -11 53 Human 7.8 pIC50 = 7.8 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm701575k
15951194 78413 12 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 78413 12 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 44917 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 444 9 3 6 3.5 OC[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL146132 44917 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 444 9 3 6 3.5 OC[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10695596 109570 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 109570 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 85147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 85147 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 126697 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 457 9 3 6 3.4 CC(=O)Nc1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL349390 126697 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 457 9 3 6 3.4 CC(=O)Nc1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10502763 126920 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 430 9 3 6 2.9 OC[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL351303 126920 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 430 9 3 6 2.9 OC[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10645471 17814 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL117633 17814 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 8 1 5 3.5 c1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10516184 21301 4 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 21301 4 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 126652 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 9 2 6 3.3 CNCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL348962 126652 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 9 2 6 3.3 CNCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10551207 45372 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 442 9 2 5 4.4 C[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146502 45372 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 442 9 2 5 4.4 C[C@H](Cc1ccccc1)NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
10696275 44783 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44783 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 17814 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 17814 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 121129 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 121129 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 86302 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 86302 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
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 9292 24 None -251 67 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9292 24 None -251 67 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9292 24 None -251 67 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9292 24 None -251 67 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9292 24 None -251 67 Rat 6.8 pIC50 = 6.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 10479 68 None -17 32 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358 10479 68 None -17 32 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
54 10479 68 None -17 32 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL128 10479 68 None -17 32 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB00669 10479 68 None -17 32 Rat 7.8 pIC50 = 7.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
10620429 63038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 1 6 3.1 c1coc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL162805 63038 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 1 6 3.1 c1coc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10644750 63286 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
CHEMBL163573 63286 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)nc1 10.1021/jm980569z
10574671 127003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 430 7 1 5 3.8 S=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
CHEMBL352159 127003 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 430 7 1 5 3.8 S=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
10719938 44734 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44734 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 85146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 285 3 3 3 2.0 N[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2110299 85146 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 285 3 3 3 2.0 N[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10809876 109430 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 109430 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 8334 25 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 8334 25 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 8334 25 None - 0 Rat 6.8 pIC50 = 6.8 Binding
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 174937 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 174937 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
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 173824 3 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 173824 3 None - 2 Rat 6.7 pIC50 = 6.7 Binding
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 9033 8 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
9847194 9033 8 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
CHEMBL313714 9033 8 None - 1 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 462 9 3 6 3.6 OC[C@@H](c1ccc(cc1)F)NC1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm9704558
2351 10059 64 None -10 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -10 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -10 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -10 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -10 21 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
10717512 209847 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 209847 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 17062 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 17062 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 9274 52 None -40 43 Rat 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9274 52 None -40 43 Rat 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9274 52 None -40 43 Rat 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9274 52 None -40 43 Rat 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 9274 52 None -40 43 Rat 7.7 pIC50 = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 107806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 107806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 107806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 107806 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 209719 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 209719 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 108511 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 108511 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 8443 50 None -144 65 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -144 65 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -144 65 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -144 65 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -144 65 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
44305547 210109 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 210109 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 108425 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
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 108425 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor was measured using [3H]5-HT as radioligand
ChEMBL 343 3 0 5 3.3 C=CCN1CCN(c2nc3ccc4ncccc4c3n3cccc23)CC1 10.1021/jm960501o
124 9755 47 None -2 32 Rat 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
2032 9755 47 None -2 32 Rat 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
4636 9755 47 None -2 32 Rat 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
CHEMBL762 9755 47 None -2 32 Rat 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
DB00935 9755 47 None -2 32 Rat 8.7 pIC50 = 8.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C nan
130 10273 47 None -8 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
3378093 10273 47 None -8 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
CHEMBL281350 10273 47 None -8 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm990397l
108029 10187 57 None -3 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
23 10187 57 None -3 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
CHEMBL18785 10187 57 None -3 13 Rat 8.7 pIC50 = 8.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00170a007
10838923 59409 0 None - 3 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 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 59409 0 None - 3 Rat 8.7 pIC50 = 8.7 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 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 61493 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 457 8 2 6 3.5 CC(=O)Nc1cccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL161176 61493 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 457 8 2 6 3.5 CC(=O)Nc1cccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10787240 126584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 4.0 c1ccc(COC[C@@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
CHEMBL348304 126584 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 4.0 c1ccc(COC[C@@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
1042 8362 23 None -5 17 Rat 8.6 pIC50 = 8.6 Binding
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 8362 23 None -5 17 Rat 8.6 pIC50 = 8.6 Binding
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 8362 23 None -5 17 Rat 8.6 pIC50 = 8.6 Binding
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 8362 23 None -5 17 Rat 8.6 pIC50 = 8.6 Binding
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 8362 23 None -5 17 Rat 8.6 pIC50 = 8.6 Binding
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 74573 17 None -1 15 Rat 8.5 pIC50 = 8.5 Binding
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 74573 17 None -1 15 Rat 8.5 pIC50 = 8.5 Binding
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 208877 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 208877 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
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 61919 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 418 7 1 5 3.6 Fc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL161723 61919 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 418 7 1 5 3.6 Fc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10572483 126665 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 390 8 2 6 3.0 c1coc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
CHEMBL349041 126665 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 390 8 2 6 3.0 c1coc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
10522029 209928 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 209928 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 210104 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 210104 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 172040 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](O)c1ccccc1 10.1021/jm9910021
CHEMBL423022 172040 1 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](O)c1ccccc1 10.1021/jm9910021
73347306 96469 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 96469 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 47037 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47037 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 105859 0 None - 1 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for 5-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 105859 0 None - 1 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for 5-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 105859 0 None - 1 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 18025 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 18025 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 18025 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 19140 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 19140 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 19140 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 105323 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 105323 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 105323 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 4.7 pIC50 = 4.7 Binding
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 106335 8 None - 1 Rat 4.7 pIC50 = 4.7 Binding
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 96047 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96047 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96051 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96051 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 108442 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 108442 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
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 213701 96 None -41 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL1559 213701 96 None -41 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
CHEMBL91 213701 96 None -41 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
10621020 117162 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL324287 117162 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10805623 106028 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 320 1 1 4 2.9 FC(F)(F)c1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm00170a007
CHEMBL28178 106028 0 None - 1 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 320 1 1 4 2.9 FC(F)(F)c1ccc2c(c1)nc(N1CCNCC1)c1cccn12 10.1021/jm00170a007
10575878 42302 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](O)c1ccccc1 10.1021/jm9910021
CHEMBL143890 42302 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.9 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](O)c1ccccc1 10.1021/jm9910021
10766318 44547 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 2 6 4.1 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL145815 44547 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 10 2 6 4.1 COC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10551857 172151 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
CHEMBL423749 172151 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@@H](CO)c1ccccc1 10.1021/jm9910021
10621020 117162 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
CHEMBL324287 117162 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 7 1 5 3.5 CN(Cc1ccccc1)[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
10766235 85635 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 85635 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 210442 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 210442 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 7745 93 None -691 90 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
38 7745 93 None -691 90 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
722 7745 93 None -691 90 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
CHEMBL42 7745 93 None -691 90 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
DB00363 7745 93 None -691 90 Rat 5.7 pIC50 = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
146420029 191541 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 191541 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 171699 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1cncc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL422366 171699 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1cncc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10503687 209856 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 209856 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
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 86303 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 86303 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 86424 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 86424 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 213801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 213801 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
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 90314 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 90314 1 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 212292 76 None -44 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL1201049 212292 76 None -44 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
CHEMBL808 212292 76 None -44 34 Rat 4.7 pIC50 = 4.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 nan
11744707 171688 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 171688 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
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 59737 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 508 7 3 5 4.1 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15965 59737 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 508 7 3 5 4.1 COc1ccc(NC(=O)NCCN2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
44267181 16383 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
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 16383 0 None - 0 Human 4.6 pIC50 = 4.6 Binding
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 105379 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 462 2 2 3 5.1 CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12 10.1021/jm9811054
CHEMBL276928 105379 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 462 2 2 3 5.1 CN1CCC2(CC1)COc1ccc(NC(=O)N3CCC(c4c[nH]c5ccc(F)cc45)CC3)cc12 10.1021/jm9811054
11795333 63045 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm980569z
CHEMBL162858 63045 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 401 7 1 6 2.9 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)ccn1 10.1021/jm980569z
10813272 45093 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 446 8 2 5 4.6 CC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
CHEMBL146285 45093 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 446 8 2 5 4.6 CC(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccc(F)cc1 10.1021/jm9910021
3191 109635 97 None -17 25 Rat 5.6 pIC50 = 5.6 Binding
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 109635 97 None -17 25 Rat 5.6 pIC50 = 5.6 Binding
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 109635 97 None -17 25 Rat 5.6 pIC50 = 5.6 Binding
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 118174 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 118174 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 105725 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 451 4 2 4 4.1 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)C2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL279646 105725 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 451 4 2 4 4.1 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)C2)cc1N1CCN(C)CC1 10.1021/jm9811054
10622257 108909 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 108909 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 207724 22 None -22 20 Rat 7.6 pIC50 = 7.6 Binding
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 207724 22 None -22 20 Rat 7.6 pIC50 = 7.6 Binding
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 207724 22 None -22 20 Rat 7.6 pIC50 = 7.6 Binding
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 46566 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46566 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127849 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127849 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 111092 0 None -32359 7 Rat 5.6 pIC50 = 5.6 Binding
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 111092 0 None -32359 7 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
19978038 201798 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 201798 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 127828 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127828 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 107643 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 107643 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 7745 93 None -691 90 Rat 5.6 pIC50 = 5.6 Binding
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 7745 93 None -691 90 Rat 5.6 pIC50 = 5.6 Binding
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 7745 93 None -691 90 Rat 5.6 pIC50 = 5.6 Binding
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 7745 93 None -691 90 Rat 5.6 pIC50 = 5.6 Binding
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 7745 93 None -691 90 Rat 5.6 pIC50 = 5.6 Binding
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 20873 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 20873 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 209513 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 209513 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 20873 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL119785 20873 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 471 9 2 6 3.5 CC(=O)Nc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
11796081 61511 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 9 2 5 3.5 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(Cn5cncn5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL161192 61511 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 9 2 5 3.5 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(Cn5cncn5)cc34)C2)cc1 10.1021/jm9805687
10691928 46698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46698 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 125544 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 125544 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 7532 59 None -16 29 Rat 4.6 pIC50 = 4.6 Binding
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 7532 59 None -16 29 Rat 4.6 pIC50 = 4.6 Binding
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 7532 59 None -16 29 Rat 4.6 pIC50 = 4.6 Binding
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 7532 59 None -16 29 Rat 4.6 pIC50 = 4.6 Binding
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 7532 59 None -16 29 Rat 4.6 pIC50 = 4.6 Binding
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 8844 57 None -1778 18 Rat 4.6 pIC50 = 4.6 Binding
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 8844 57 None -1778 18 Rat 4.6 pIC50 = 4.6 Binding
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 8844 57 None -1778 18 Rat 4.6 pIC50 = 4.6 Binding
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 126804 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 126804 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 200207 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 200207 0 None - 0 Rat 4.6 pIC50 = 4.6 Binding
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 9947 58 None -39 31 Rat 5.6 pIC50 = 5.6 Binding
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 9947 58 None -39 31 Rat 5.6 pIC50 = 5.6 Binding
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 9947 58 None -39 31 Rat 5.6 pIC50 = 5.6 Binding
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 9947 58 None -39 31 Rat 5.6 pIC50 = 5.6 Binding
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 9947 58 None -39 31 Rat 5.6 pIC50 = 5.6 Binding
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 174396 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 472 4 2 5 4.2 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C#N)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL430122 174396 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 472 4 2 5 4.2 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(C#N)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10781299 18448 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 18448 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 18448 7 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 122076 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 122076 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
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 16236 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 16236 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 16974 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 16974 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 10479 68 None -3 32 Human 7.6 pIC50 = 7.6 Binding
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 10479 68 None -3 32 Human 7.6 pIC50 = 7.6 Binding
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 10479 68 None -3 32 Human 7.6 pIC50 = 7.6 Binding
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 10479 68 None -3 32 Human 7.6 pIC50 = 7.6 Binding
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 10479 68 None -3 32 Human 7.6 pIC50 = 7.6 Binding
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 63343 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 1 6 3.1 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm980569z
CHEMBL164111 63343 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 1 6 3.1 c1cc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)co1 10.1021/jm980569z
10765655 121223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 121223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 10563 80 None 1 27 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
4296 10563 80 None 1 27 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
CHEMBL274866 10563 80 None 1 27 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00170a007
10526642 176052 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 430 9 3 6 2.9 OC[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL441296 176052 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 430 9 3 6 2.9 OC[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10838030 30279 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 30279 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
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 11551 101 None -51 34 Rat 4.6 pIC50 = 4.6 Binding
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 11551 101 None -51 34 Rat 4.6 pIC50 = 4.6 Binding
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 175238 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL435060 175238 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10805740 96049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96049 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 8083 62 None -501 50 Rat 5.6 pIC50 = 5.6 Binding
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 8083 62 None -501 50 Rat 5.6 pIC50 = 5.6 Binding
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 8083 62 None -501 50 Rat 5.6 pIC50 = 5.6 Binding
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 8083 62 None -501 50 Rat 5.6 pIC50 = 5.6 Binding
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 8083 62 None -501 50 Rat 5.6 pIC50 = 5.6 Binding
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 121223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
CHEMBL333341 121223 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 442 9 1 5 4.5 CN(Cc1ccccc1)CC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9704558
10468938 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL116092 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10468938 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL116092 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
10468938 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 17016 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42305 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 210500 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 210500 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 210041 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 210041 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
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 170811 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420874 170811 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 387 7 1 5 3.6 c1ccc(CO[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
10836850 47051 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47051 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 210159 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 210159 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
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 63052 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 3.0 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
CHEMBL162899 63052 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 3.0 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1Cc1ccccc1 10.1021/jm980569z
11798502 63267 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 468 7 1 5 4.5 FC(F)(F)c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL163376 63267 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 468 7 1 5 4.5 FC(F)(F)c1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
73351903 96470 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 96470 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 6927 72 None -11 53 Human 7.5 pIC50 = 7.5 Binding
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 6927 72 None -11 53 Human 7.5 pIC50 = 7.5 Binding
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 6927 72 None -11 53 Human 7.5 pIC50 = 7.5 Binding
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 6927 72 None -11 53 Human 7.5 pIC50 = 7.5 Binding
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 132165 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 132165 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 215378 21 None - 1 Rat 5.5 pIC50 = 5.5 Binding
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 210225 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 210225 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
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 105253 64 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 276 1 2 1 3.3 Brc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL27592 105253 64 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 276 1 2 1 3.3 Brc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
10573904 128086 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 128086 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 106223 7 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL282994 106223 7 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 232 1 2 1 3.2 Clc1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
53263 106271 17 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 243 2 2 3 2.5 O=[N+]([O-])c1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
CHEMBL283257 106271 17 None - 1 Rat 8.5 pIC50 = 8.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HTInhibitory activity against 5-hydroxytryptamine 1B receptor of rat cortex using [3H]5-HT
ChEMBL 243 2 2 3 2.5 O=[N+]([O-])c1ccc2[nH]cc(C3=CCNCC3)c2c1 10.1021/jm00170a007
2761023 105542 71 None - 3 Rat 8.4 pIC50 = 8.4 Binding
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 105542 71 None - 3 Rat 8.4 pIC50 = 8.4 Binding
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 105542 71 None - 3 Rat 8.4 pIC50 = 8.4 Binding
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 118094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 118094 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 120170 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 120170 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 36389 24 None -26 17 Rat 7.5 pIC50 = 7.5 Binding
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 36389 24 None -26 17 Rat 7.5 pIC50 = 7.5 Binding
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 17016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL116092 17016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 281 4 1 4 2.4 c1cc2[nH]cc(CCN3CCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
10468938 17016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 17016 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 107698 21 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 107698 21 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 206933 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 206933 1 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 209507 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 209507 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 59225 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 505 5 3 4 4.7 CN1CCC2(CC1)COc1ccc(NC(=O)NCCN3CCC(c4c[nH]c5cc(F)ccc45)CC3)cc12 10.1021/jm9811054
CHEMBL15909 59225 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 505 5 3 4 4.7 CN1CCC2(CC1)COc1ccc(NC(=O)NCCN3CCC(c4c[nH]c5cc(F)ccc45)CC3)cc12 10.1021/jm9811054
44364110 42309 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42309 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 86423 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 86423 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 207920 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 207920 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 105763 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 105763 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 105763 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 172196 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 172196 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 172196 0 None - 1 Rat 5.5 pIC50 = 5.5 Binding
Binding affinity for 5-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 109530 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 109530 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 18017 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 18017 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 18818 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 18818 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 18818 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 103915 0 None - 1 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 103915 0 None - 1 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 103915 0 None - 1 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 105478 0 None - 1 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 105478 0 None - 1 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 200103 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 200103 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Binding affinity for 5-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 74574 19 None -43 18 Rat 5.5 pIC50 = 5.5 Binding
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 74574 19 None -43 18 Rat 5.5 pIC50 = 5.5 Binding
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 169151 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 169151 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 117282 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL324931 117282 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 310 4 1 5 1.5 CN1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
11796807 172322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL424154 172322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1)c1ccccc1 10.1021/jm9805687
9949172 17645 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL117249 17645 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 324 5 1 5 1.9 CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
11794853 209854 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 209854 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 208143 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 208143 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
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 132164 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 132164 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 117282 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 117282 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 209888 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 209888 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 77061 2 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 77061 2 None - 0 Rat 6.5 pIC50 = 6.5 Binding
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 16395 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 16395 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 59536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 59536 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 17967 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 17967 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 108493 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 108493 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 9641 38 None -18 30 Rat 5.5 pIC50 = 5.5 Binding
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 9641 38 None -18 30 Rat 5.5 pIC50 = 5.5 Binding
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 9641 38 None -18 30 Rat 5.5 pIC50 = 5.5 Binding
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 9641 38 None -18 30 Rat 5.5 pIC50 = 5.5 Binding
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 9641 38 None -18 30 Rat 5.5 pIC50 = 5.5 Binding
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 16363 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 16363 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
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 17809 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL117579 17809 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
18691566 96046 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 4 3 3 2.3 CN[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
CHEMBL2368256 96046 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 299 4 3 3 2.3 CN[C@H]1C[C@H](c2c[nH]c3ccc(CC4COC(=O)N4)cc32)C1 10.1021/jm000956k
10571716 47268 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47268 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 104887 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 104887 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 104887 4 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 62591 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 350 8 2 5 2.4 C=CCNC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL162296 62591 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 350 8 2 5 2.4 C=CCNC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10501944 17809 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
CHEMBL117579 17809 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 414 8 1 5 3.7 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9704558
10693206 61936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 9 1 5 4.2 c1ccc(COC[C@@H]2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL161735 61936 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 415 9 1 5 4.2 c1ccc(COC[C@@H]2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
109 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 7689 31 None - 7 Rat 6.5 pIC50 = 6.5 Binding
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 210167 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 210167 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
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 45067 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45067 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 16871 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 16871 1 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 25322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 25322 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
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 201496 63 None -2 3 Rat 4.5 pIC50 = 4.5 Binding
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 201496 63 None -2 3 Rat 4.5 pIC50 = 4.5 Binding
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 201496 63 None -2 3 Rat 4.5 pIC50 = 4.5 Binding
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 120266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
CHEMBL331970 120266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 428 8 2 5 4.5 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9704558
10502988 44786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44786 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 120266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 120266 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44938 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 485 9 3 6 4.5 CC(=O)Nc1ccc([C@@H](C)NC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
CHEMBL146150 44938 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 485 9 3 6 4.5 CC(=O)Nc1ccc([C@@H](C)NC2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm9910021
44296810 168773 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 168773 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
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 105185 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
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 105185 0 None - 0 Human 4.5 pIC50 = 4.5 Binding
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 17238 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 17238 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
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 7736 33 None -138 21 Rat 6.5 pIC50 = 6.5 Binding
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 7736 33 None -138 21 Rat 6.5 pIC50 = 6.5 Binding
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 7736 33 None -138 21 Rat 6.5 pIC50 = 6.5 Binding
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 7736 33 None -138 21 Rat 6.5 pIC50 = 6.5 Binding
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 7736 33 None -138 21 Rat 6.5 pIC50 = 6.5 Binding
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 63687 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 2 6 2.2 c1c[nH]c(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)n1 10.1021/jm980569z
CHEMBL164413 63687 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 390 7 2 6 2.2 c1c[nH]c(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)n1 10.1021/jm980569z
10644514 107834 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 107834 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 109394 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 109394 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 170879 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm980569z
CHEMBL420965 170879 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm980569z
376254 125282 2 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 125282 2 None - 1 Rat 6.4 pIC50 = 6.4 Binding
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 7189 56 None -389 40 Rat 5.4 pIC50 = 5.4 Binding
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 7189 56 None -389 40 Rat 5.4 pIC50 = 5.4 Binding
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 7189 56 None -389 40 Rat 5.4 pIC50 = 5.4 Binding
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 7189 56 None -389 40 Rat 5.4 pIC50 = 5.4 Binding
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 7189 56 None -389 40 Rat 5.4 pIC50 = 5.4 Binding
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 109490 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 109490 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 10036 95 None -2 23 Rat 6.4 pIC50 = 6.4 Binding
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 10036 95 None -2 23 Rat 6.4 pIC50 = 6.4 Binding
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 10036 95 None -2 23 Rat 6.4 pIC50 = 6.4 Binding
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 16395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 16395 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 33188 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 33188 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 6975 55 None -7413 44 Rat 5.4 pIC50 = 5.4 Binding
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 6975 55 None -7413 44 Rat 5.4 pIC50 = 5.4 Binding
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 6975 55 None -7413 44 Rat 5.4 pIC50 = 5.4 Binding
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 6975 55 None -7413 44 Rat 5.4 pIC50 = 5.4 Binding
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 96050 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96050 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 16395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 16395 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 201694 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 201694 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 59614 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 59614 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 63335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.1 CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL164046 63335 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 8 2 5 4.1 CC(C)(NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10764284 62208 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 3.0 O=C1CN(Cc2ccccc2)CCN1CCCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
CHEMBL161969 62208 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 414 7 1 5 3.0 O=C1CN(Cc2ccccc2)CCN1CCCc1c[nH]c2ccc(-n3cnnc3)cc12 10.1021/jm980569z
13673326 23186 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 23186 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 61346 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 267 4 1 4 2.0 c1cc2[nH]cc(CCN3CCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL161045 61346 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 267 4 1 4 2.0 c1cc2[nH]cc(CCN3CCC3)c2cc1-n1cnnc1 10.1021/jm9805687
5 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 126503 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 126503 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 210097 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 210097 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 106266 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for 5-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 106266 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for 5-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 106266 0 None - 1 Rat 6.4 pIC50 = 6.4 Binding
Binding affinity for 5-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 46889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46889 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 106202 0 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Binding affinity for 5-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 106202 0 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Binding affinity for 5-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 106202 0 None - 1 Rat 4.4 pIC50 = 4.4 Binding
Binding affinity for 5-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 7706 68 None -147 72 Rat 5.4 pIC50 = 5.4 Binding
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 7706 68 None -147 72 Rat 5.4 pIC50 = 5.4 Binding
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 7706 68 None -147 72 Rat 5.4 pIC50 = 5.4 Binding
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 7706 68 None -147 72 Rat 5.4 pIC50 = 5.4 Binding
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 7706 68 None -147 72 Rat 5.4 pIC50 = 5.4 Binding
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 209722 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 209722 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 10107 82 None -1 5 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
5078 10107 82 None -1 5 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
51 10107 82 None -1 5 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
CHEMBL905 10107 82 None -1 5 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
DB00953 10107 82 None -1 5 Human 7.4 pIC50 = 7.4 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10.1021/jm9704558
10693140 59853 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL159759 59853 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 4.0 C[C@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
11795644 47207 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 47207 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46743 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46743 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 195952 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 195952 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 195952 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 195952 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
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 42429 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42429 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 7541 6 None -16 6 Rat 6.4 pIC50 = 6.4 Binding
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 7541 6 None -16 6 Rat 6.4 pIC50 = 6.4 Binding
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 7541 6 None -16 6 Rat 6.4 pIC50 = 6.4 Binding
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 108905 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 108905 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 17645 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 17645 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
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 201724 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 201724 0 None - 0 Rat 4.4 pIC50 = 4.4 Binding
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 58732 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 58732 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 35333 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 35333 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
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 63006 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 8 1 5 4.1 CC(CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm980569z
CHEMBL162722 63006 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 8 1 5 4.1 CC(CN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm980569z
10719203 45153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45153 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 63129 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 496 9 1 8 3.9 Cc1noc(-c2ccc(CCN3CCN(CCCc4c[nH]c5ccc(-n6cnnc6)cc45)CC3)cc2)n1 10.1021/jm980569z
CHEMBL163114 63129 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 496 9 1 8 3.9 Cc1noc(-c2ccc(CCN3CCN(CCCc4c[nH]c5ccc(-n6cnnc6)cc45)CC3)cc2)n1 10.1021/jm980569z
10788207 207546 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 207546 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 44915 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44915 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 50801 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 423 6 4 5 3.0 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(O)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15139 50801 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 423 6 4 5 3.0 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(O)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
10645615 107778 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 107778 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 117675 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 117675 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL420965 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
10811007 59919 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL159819 59919 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10386282 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL420965 170879 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10503731 17061 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 17061 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 214620 103 None -3 16 Rat 5.3 pIC50 = 5.3 Binding
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 214620 103 None -3 16 Rat 5.3 pIC50 = 5.3 Binding
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 126762 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)nc1 10.1021/jm9805687
CHEMBL349893 126762 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1ccc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)nc1 10.1021/jm9805687
10527882 42367 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42367 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 105227 39 None -162 7 Rat 6.3 pIC50 = 6.3 Binding
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 105227 39 None -162 7 Rat 6.3 pIC50 = 6.3 Binding
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 195002 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 195002 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 59551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 59551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 59551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
CHEMBL159483 59551 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 432 9 3 4 3.5 O=C1N[C@@H](Cc2ccc3[nH]cc(CCN4CC[C@@H](CNCc5ccccc5)C4)c3c2)CO1 10.1021/jm9805687
11797644 60197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 60197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 107661 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 107661 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 132166 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 132166 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
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 6927 72 None -11 53 Human 8.3 pIC50 = 8.3 Binding
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 6927 72 None -11 53 Human 8.3 pIC50 = 8.3 Binding
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 6927 72 None -11 53 Human 8.3 pIC50 = 8.3 Binding
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 6927 72 None -11 53 Human 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 6927 72 None -13 53 Rat 8.3 pIC50 = 8.3 Binding
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 210215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 210215 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
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 60197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 60197 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 59919 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL159819 59919 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 400 8 2 5 3.4 c1ccc(CNC[C@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
9824884 58633 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 447 4 2 4 4.3 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15855 58633 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 447 4 2 4 4.3 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10412190 59692 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cccc(F)c34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15961 59692 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cccc(F)c34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
49836496 25327 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 25327 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
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 16938 7 None - 1 Rat 5.3 pIC50 = 5.3 Binding
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 10764 94 None - 3 Rat 5.3 pIC50 = 5.3 Binding
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 10764 94 None - 3 Rat 5.3 pIC50 = 5.3 Binding
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 10764 94 None - 3 Rat 5.3 pIC50 = 5.3 Binding
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 10764 94 None - 3 Rat 5.3 pIC50 = 5.3 Binding
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 10764 94 None - 3 Rat 5.3 pIC50 = 5.3 Binding
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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
Binding affinity for 5-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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
Binding affinity for 5-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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
Binding affinity for 5-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 169278 0 None - 1 Rat 4.3 pIC50 = 4.3 Binding
Binding affinity for 5-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 169278 0 None - 1 Rat 4.3 pIC50 = 4.3 Binding
Binding affinity for 5-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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
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 8844 57 None -1778 18 Rat 4.3 pIC50 = 4.3 Binding
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 22035 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 22035 2 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 16938 7 None - 1 Human 5.3 pIC50 = 5.3 Binding
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 16938 7 None - 1 Human 5.3 pIC50 = 5.3 Binding
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 16938 7 None - 1 Human 5.3 pIC50 = 5.3 Binding
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 10563 80 None 1 27 Rat 7.3 pIC50 = 7.3 Binding
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 10563 80 None 1 27 Rat 7.3 pIC50 = 7.3 Binding
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 10563 80 None 1 27 Rat 7.3 pIC50 = 7.3 Binding
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 106335 8 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity for 5-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 106335 8 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity for 5-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 171674 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 338 6 1 5 2.3 CN1CCN(CCCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL422191 171674 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 338 6 1 5 2.3 CN1CCN(CCCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10527884 35147 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 35147 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 107446 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 107446 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 41964 0 None -4 4 Human 6.3 pIC50 = 6.3 Binding
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 41964 0 None -4 4 Human 6.3 pIC50 = 6.3 Binding
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 109089 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 109089 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 16373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 16373 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
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 63272 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163462 63272 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 443 8 2 6 2.5 NC(=O)C(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
145 6928 49 None -8 30 Human 6.3 pIC50 = 6.3 Binding
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 6928 49 None -8 30 Human 6.3 pIC50 = 6.3 Binding
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 6928 49 None -8 30 Human 6.3 pIC50 = 6.3 Binding
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 6928 49 None -8 30 Human 6.3 pIC50 = 6.3 Binding
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 105290 4 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 105290 4 None - 0 Rat 5.3 pIC50 = 5.3 Binding
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 63141 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 457 8 2 6 3.5 CC(=O)Nc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL163127 63141 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 457 8 2 6 3.5 CC(=O)Nc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
18366015 85147 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 85147 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 200215 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 200215 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 58056 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 437 3 2 4 3.7 COc1ccc(NC(=O)N2CCc3[nH]c4ccc(F)cc4c3C2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15808 58056 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 437 3 2 4 3.7 COc1ccc(NC(=O)N2CCc3[nH]c4ccc(F)cc4c3C2)cc1N1CCN(C)CC1 10.1021/jm9811054
44344504 119609 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
CHEMBL330803 119609 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9704558
44341657 119834 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 119834 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 96473 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 96473 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 119609 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
CHEMBL330803 119609 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 295 4 1 4 2.8 c1cc2[nH]cc(CCN3CCCCC3)c2cc1-n1cnnc1 10.1021/jm9805687
10834908 59439 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 4.0 c1ccc(COC[C@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
CHEMBL159381 59439 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 4.0 c1ccc(COC[C@H]2CCCN2CCc2c[nH]c3ccc(-n4cnnc4)cc23)cc1 10.1021/jm9805687
11796808 59827 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 1 5 3.8 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
CHEMBL159733 59827 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 1 5 3.8 CN(Cc1ccccc1)C[C@@H]1CCN(CCc2c[nH]c3ccc(Cn4cncn4)cc23)C1 10.1021/jm9805687
10590206 209582 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 209582 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 45222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45222 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 30955 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 30955 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 210546 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 210546 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 201133 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 201133 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 61885 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 434 7 1 5 4.2 Clc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL161696 61885 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 434 7 1 5 4.2 Clc1ccc(CN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10836301 59738 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 1 5 4.1 CN(Cc1ccccc1)C[C@@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL159650 59738 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 428 9 1 5 4.1 CN(Cc1ccccc1)C[C@@H]1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
108029 10187 57 None -3 13 Rat 8.2 pIC50 = 8.2 Binding
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 10187 57 None -3 13 Rat 8.2 pIC50 = 8.2 Binding
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 10187 57 None -3 13 Rat 8.2 pIC50 = 8.2 Binding
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 10924 89 None -8 7 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
60 10924 89 None -8 7 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
60857 10924 89 None -8 7 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
CHEMBL1185 10924 89 None -8 7 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
DB00315 10924 89 None -8 7 Human 8.2 pIC50 = 8.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1021/jm000956k
10528410 46156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46156 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 128796 17 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 128796 17 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 6927 72 None -11 53 Human 8.2 pIC50 = 8.2 Binding
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 6927 72 None -11 53 Human 8.2 pIC50 = 8.2 Binding
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 6927 72 None -11 53 Human 8.2 pIC50 = 8.2 Binding
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 6927 72 None -11 53 Human 8.2 pIC50 = 8.2 Binding
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 42377 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42377 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 51226 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 533 7 1 8 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
CHEMBL151894 51226 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 533 7 1 8 4.6 COc1ccc(NS(=O)(=O)c2ccc(-c3ccc(-c4nnc(C)o4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm990397l
10645076 207089 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 207089 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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 16938 7 None - 1 Rat 5.2 pIC50 = 5.2 Binding
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 103835 0 None - 1 Rat 4.2 pIC50 = 4.2 Binding
Binding affinity for 5-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 103835 0 None - 1 Rat 4.2 pIC50 = 4.2 Binding
Binding affinity for 5-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 103835 0 None - 1 Rat 4.2 pIC50 = 4.2 Binding
Binding affinity for 5-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 16844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 16844 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 107552 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 107552 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 118443 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 118443 4 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 61993 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 61993 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 61993 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
CHEMBL161780 61993 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 440 10 3 4 2.9 CNS(=O)(=O)Cc1ccc2[nH]cc(CCN3CC[C@@H](CNCc4ccccc4)C3)c2c1 10.1021/jm9805687
10525100 126299 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1cncc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
CHEMBL345657 126299 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 2 6 2.8 c1cncc(CNC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)c1 10.1021/jm9805687
10341917 174828 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 174828 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
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 60489 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 425 6 3 4 3.4 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL16035 60489 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 425 6 3 4 3.4 COc1ccc(NC(=O)NCCc2c[nH]c3ccc(F)cc23)cc1N1CCN(C)CC1 10.1021/jm9811054
10592083 42375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42375 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 22219 15 None -1 4 Rat 6.2 pIC50 = 6.2 Binding
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 22219 15 None -1 4 Rat 6.2 pIC50 = 6.2 Binding
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 96048 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96048 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 210073 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 210073 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 105820 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 454 7 2 4 4.7 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
CHEMBL280314 105820 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 454 7 2 4 4.7 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1OCCN(C)C 10.1021/jm9811054
10833258 103193 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 103193 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
197 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
3822 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
88 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
CHEMBL51 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
DB12465 8962 96 None -2511 51 Human 5.2 pIC50 = 5.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm9704558
10839082 46487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46487 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 126043 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 126043 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 42394 0 None -6 4 Human 6.2 pIC50 = 6.2 Binding
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 42394 0 None -6 4 Human 6.2 pIC50 = 6.2 Binding
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 16395 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 16395 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 107689 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 107689 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
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 86301 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 86301 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 126789 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 126789 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 35128 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 35128 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 16653 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 16653 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
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 201525 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 201525 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 171729 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 171729 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 63054 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 311 5 1 5 2.0 c1cc2[nH]cc(CCCN3CCOCC3)c2cc1-n1cnnc1 10.1021/jm980569z
CHEMBL162930 63054 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 311 5 1 5 2.0 c1cc2[nH]cc(CCCN3CCOCC3)c2cc1-n1cnnc1 10.1021/jm980569z
10717072 170022 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 170022 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
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 176457 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 176457 15 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 21313 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 21313 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
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 51019 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 51019 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assayInhibition affinity against 5-HT-1B receptor in rat frontal cortex using radio binding assay
ChEMBL 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 18814 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 18814 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 18814 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Binding affinity for 5-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 9688 112 None -162 65 Rat 6.2 pIC50 = 6.2 Binding
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 9688 112 None -162 65 Rat 6.2 pIC50 = 6.2 Binding
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 9688 112 None -162 65 Rat 6.2 pIC50 = 6.2 Binding
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 9688 112 None -162 65 Rat 6.2 pIC50 = 6.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 107515 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 107515 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 10036 95 None -2 23 Rat 5.2 pIC50 = 5.2 Binding
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 209870 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 209870 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 108366 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 108366 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
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 16863 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 16863 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
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 125713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](CO)c1ccccc1 10.1021/jm9910021
CHEMBL342330 125713 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 2 6 3.8 CN(C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)[C@H](CO)c1ccccc1 10.1021/jm9910021
114 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
6426760 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
CHEMBL292779 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 10.1021/jm980569z
114 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 109222 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 109222 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 61708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 4.0 C[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
CHEMBL161410 61708 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 414 8 2 5 4.0 C[C@@H](NC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1)c1ccccc1 10.1021/jm9805687
10741826 45973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45973 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 209863 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 209863 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
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 169821 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 169821 0 None - 0 Human 5.1 pIC50 = 5.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 96468 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 96468 1 None - 0 Rat 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 9034 14 None - 1 Human 7.1 pIC50 = 7.1 Binding
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 44755 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44755 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 58406 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 522 8 2 5 4.2 COc1ccc(NC(=O)N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL15837 58406 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 522 8 2 5 4.2 COc1ccc(NC(=O)N2CCN(CCCCc3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10645335 195492 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 195492 0 None - 0 Rat 4.1 pIC50 = 4.1 Binding
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 47022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 521 11 3 7 3.0 CS(=O)(=O)NC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148071 47022 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 521 11 3 7 3.0 CS(=O)(=O)NC[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10836290 62211 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 8 1 5 3.1 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1CCc1ccccc1 10.1021/jm980569z
CHEMBL161970 62211 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 8 1 5 3.1 O=C1CN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CCN1CCc1ccccc1 10.1021/jm980569z
11795525 127894 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 127894 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46916 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46916 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 22045 3 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 22045 3 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 210163 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 210163 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
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 7146 27 None -5 21 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 7146 27 None -5 21 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 7146 27 None -5 21 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 7146 27 None -5 21 Rat 8.1 pIC50 = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 45156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45156 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 46863 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 105631 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL278917 105631 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4cc(F)ccc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
9804849 74230 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 74230 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 45229 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 390 7 1 5 3.1 CC#CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
CHEMBL146396 45229 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 390 7 1 5 3.1 CC#CCN(C)C1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm9910021
14450364 62777 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 62777 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 117253 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 117253 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 20729 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
CHEMBL119668 20729 1 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 450 8 1 5 3.8 Fc1ccc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1F 10.1021/jm980569z
9881324 35145 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 35145 3 None - 0 Human 6.1 pIC50 = 6.1 Binding
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 126846 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 126846 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 16588 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 16588 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 47073 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 471 9 3 6 3.8 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
CHEMBL148110 47073 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 471 9 3 6 3.8 C[C@@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)C(=O)Nc1ccccc1 10.1021/jm9910021
10412189 84028 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
CHEMBL2079627 84028 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.Binding affinity towards 5-hydroxytryptamine 1B receptor in rat frontal cortex using [125I]iodocyanopindolol as radio-ligand.
ChEMBL 465 4 2 4 4.5 COc1ccc(NC(=O)N2CCC(c3c[nH]c4ccc(F)cc34)CC2)cc1N1CCN(C)CC1 10.1021/jm9811054
10670211 126998 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 9 1 5 3.9 c1ccc(CCCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
CHEMBL352123 126998 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 428 9 1 5 3.9 c1ccc(CCCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)cc1 10.1021/jm980569z
10739818 117920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL326371 117920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10719245 44582 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 44582 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 7186 66 None -10 31 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2157 7186 66 None -10 31 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2566 7186 66 None -10 31 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
CHEMBL633 7186 66 None -10 31 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
DB01118 7186 66 None -10 31 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
2105 9828 37 None -6 32 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
47811 9828 37 None -6 32 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
48 9828 37 None -6 32 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
CHEMBL531 9828 37 None -6 32 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
DB01186 9828 37 None -6 32 Rat 7.1 pIC50 = 7.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
10500370 59564 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 386 7 2 5 3.7 c1ccc(NC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
CHEMBL159493 59564 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 386 7 2 5 3.7 c1ccc(NC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9805687
10670879 126646 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 126646 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 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 117920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
CHEMBL326371 117920 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
ChEMBL 401 8 1 5 3.8 c1ccc(COC[C@@H]2CCN(CCc3c[nH]c4ccc(-n5cnnc5)cc34)C2)cc1 10.1021/jm9704558
44341609 16667 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 16667 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
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 125975 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 125975 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 175113 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 175113 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 54879 25 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 54879 25 None - 0 Rat 6.1 pIC50 = 6.1 Binding
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 27105 57 None -19 17 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
CHEMBL1306 27105 57 None -19 17 Rat 4.1 pIC50 = 4.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10720175 45344 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 45344 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 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 63269 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 430 8 2 6 3.0 OCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL163386 63269 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 430 8 2 6 3.0 OCC(c1ccccc1)N1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
10588665 96044 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 278 3 2 2 4.2 N[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL2368254 96044 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 278 3 2 2 4.2 N[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
9981024 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 102872 0 None - 1 Rat 5.1 pIC50 = 5.1 Binding
Binding affinity for 5-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 210206 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 210206 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 126922 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 415 8 1 6 2.9 c1cncc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
CHEMBL351311 126922 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 415 8 1 6 2.9 c1cncc(CCN2CCN(CCCc3c[nH]c4ccc(-n5cnnc5)cc34)CC2)c1 10.1021/jm980569z
10519108 59718 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 311 5 2 5 1.6 OC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL159627 59718 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 311 5 2 5 1.6 OC[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10780344 126714 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 297 4 2 5 1.4 O[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
CHEMBL349528 126714 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cellsDisplacement of [3H]5-HT binding from the cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
ChEMBL 297 4 2 5 1.4 O[C@@H]1CCN(CCc2c[nH]c3ccc(-n4cnnc4)cc23)C1 10.1021/jm9805687
10526737 109519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 109519 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
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 47042 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 428 8 2 5 4.5 C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148087 47042 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 428 8 2 5 4.5 C[C@H](NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
10456869 16764 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 16764 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 96043 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 306 4 1 2 4.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
CHEMBL2368253 96043 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 306 4 1 2 4.8 CN(C)[C@H]1C[C@H](c2c[nH]c3ccc(Oc4ccccc4)cc32)C1 10.1021/jm000956k
18691565 96047 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 96047 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptorBinding affinity in CHO-K1 cells transfected with human recombinant 5-hydroxytryptamine 1B receptor
ChEMBL 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 195673 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 195673 0 None - 0 Rat 4.0 pIC50 = 4.0 Binding
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 47167 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.6 CC(CO)(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
CHEMBL148194 47167 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.Binding affinity at cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells by [3H]5-HT displacement.
ChEMBL 458 9 3 6 3.6 CC(CO)(NC1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1)c1ccccc1 10.1021/jm9910021
9802530 42160 1 None -2 4 Human 7.0 pIC50 = 7.0 Binding
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 42160 1 None -2 4 Human 7.0 pIC50 = 7.0 Binding
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 16994 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
CHEMBL116031 16994 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.Displacement of [3H]5-HT binding from cloned human 5-hydroxytryptamine 1B receptor stably expressed in CHO cells.
ChEMBL 432 8 1 5 3.7 Fc1ccccc1CCN1CCN(CCCc2c[nH]c3ccc(-n4cnnc4)cc23)CC1 10.1021/jm980569z
6426761 20729 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 20729 1 None - 0 Human 7.0 pIC50 = 7.0 Binding
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 199804 2 None - 1 Guinea pig 9.4 pKd = 9.4 Binding
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 199804 2 None - 1 Guinea pig 9.4 pKd = 9.4 Binding
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 199804 2 None - 1 Guinea pig 9.4 pKd = 9.4 Binding
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 10924 89 None -8 7 Human 8.8 pKd = 8.8 Binding
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 10924 89 None -8 7 Human 8.8 pKd = 8.8 Binding
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 10924 89 None -8 7 Human 8.8 pKd = 8.8 Binding
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 10924 89 None -8 7 Human 8.8 pKd = 8.8 Binding
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 10924 89 None -8 7 Human 8.8 pKd = 8.8 Binding
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 199804 2 None - 1 Guinea pig 11.0 pKi = 11 Binding
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 199804 2 None - 1 Guinea pig 11.0 pKi = 11 Binding
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 199804 2 None - 1 Guinea pig 11.0 pKi = 11 Binding
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 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
149 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
3251 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
8223 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1982133 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL442 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00696 8363 14 None 4 29 Rat 10.0 pKi = 10.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
11797998 42466 0 None 1 3 Human 10.0 pKi = 10 Binding
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 42466 0 None 1 3 Human 10.0 pKi = 10 Binding
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 143980 0 None 14 2 Human 10.0 pKi = 10 Binding
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 143980 0 None 14 2 Human 10.0 pKi = 10 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 8625 54 None 1 18 Human 9.9 pKi = 9.9 Binding
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 123876 0 None 5 3 Human 9.9 pKi = 9.9 Binding
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 123876 0 None 5 3 Human 9.9 pKi = 9.9 Binding
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 100544 0 None 1 3 Human 9.7 pKi = 9.7 Binding
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 100544 0 None 1 3 Human 9.7 pKi = 9.7 Binding
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 193747 0 None -23 7 Human 9.7 pKi = 9.7 Binding
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 193747 0 None -23 7 Human 9.7 pKi = 9.7 Binding
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 126099 37 None 6 3 Human 9.7 pKi = 9.7 Binding
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 126099 37 None 6 3 Human 9.7 pKi = 9.7 Binding
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 85553 0 None 2 3 Human 9.7 pKi = 9.7 Binding
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 85553 0 None 2 3 Human 9.7 pKi = 9.7 Binding
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 79302 0 None 1 3 Human 9.6 pKi = 9.6 Binding
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 79302 0 None 1 3 Human 9.6 pKi = 9.6 Binding
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 132462 0 None - 1 Chinese hamster 9.6 pKi = 9.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132462 0 None - 1 Chinese hamster 9.6 pKi = 9.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 9755 47 None 1 32 Human 9.5 pKi = 9.5 Binding
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 9755 47 None 1 32 Human 9.5 pKi = 9.5 Binding
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 9755 47 None 1 32 Human 9.5 pKi = 9.5 Binding
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 9755 47 None 1 32 Human 9.5 pKi = 9.5 Binding
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 9755 47 None 1 32 Human 9.5 pKi = 9.5 Binding
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 124922 0 None 2 3 Human 9.5 pKi = 9.5 Binding
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 124922 0 None 2 3 Human 9.5 pKi = 9.5 Binding
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 10164 80 None 1 6 Human 9.5 pKi = 9.5 Binding
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 10164 80 None 1 6 Human 9.5 pKi = 9.5 Binding
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 10164 80 None 1 6 Human 9.5 pKi = 9.5 Binding
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 191075 0 None 1 3 Human 9.5 pKi = 9.5 Binding
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 191075 0 None 1 3 Human 9.5 pKi = 9.5 Binding
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 140311 0 None 1 3 Human 9.5 pKi = 9.5 Binding
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 140311 0 None 1 3 Human 9.5 pKi = 9.5 Binding
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 85551 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 85551 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 8202 21 None -5 24 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
121 8202 21 None -5 24 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
888 8202 21 None -5 24 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
CHEMBL1732 8202 21 None -5 24 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
DB00320 8202 21 None -5 24 Rat 9.4 pKi = 9.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O nan
9977716 176909 0 None -1 3 Human 9.4 pKi = 9.4 Binding
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 176909 0 None -1 3 Human 9.4 pKi = 9.4 Binding
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 194664 0 None -1 3 Human 9.4 pKi = 9.4 Binding
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 194664 0 None -1 3 Human 9.4 pKi = 9.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.084
45104767 208389 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 208389 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 208389 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 208389 0 None - 1 Human 9.4 pKi = 9.4 Binding
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 26242 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 26242 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 85552 0 None 2 3 Human 9.4 pKi = 9.4 Binding
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 85552 0 None 2 3 Human 9.4 pKi = 9.4 Binding
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 123614 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 123614 0 None 1 3 Human 9.4 pKi = 9.4 Binding
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 132986 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132986 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 18871 0 None 52 3 Human 9.3 pKi = 9.3 Binding
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 18871 0 None 52 3 Human 9.3 pKi = 9.3 Binding
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 18871 0 None 52 3 Human 9.3 pKi = 9.3 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 463 4 1 5 3.7 COc1ccc(NC(=O)N2CCN(c3cccc4c3CCCC4)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
24881204 195201 0 None 3 2 Human 9.3 pKi = 9.3 Binding
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 195201 0 None 3 2 Human 9.3 pKi = 9.3 Binding
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 106108 0 None 10 3 Human 9.3 pKi = 9.3 Binding
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 106108 0 None 10 3 Human 9.3 pKi = 9.3 Binding
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 63160 0 None -1 9 Human 9.3 pKi = 9.3 Binding
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 63160 0 None -1 9 Human 9.3 pKi = 9.3 Binding
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 63232 0 None -1 9 Human 9.3 pKi = 9.3 Binding
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 63232 0 None -1 9 Human 9.3 pKi = 9.3 Binding
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 193747 0 None -23 7 Human 9.3 pKi = 9.3 Binding
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 193747 0 None -23 7 Human 9.3 pKi = 9.3 Binding
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 194866 0 None -2 3 Human 9.3 pKi = 9.3 Binding
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 194866 0 None -2 3 Human 9.3 pKi = 9.3 Binding
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 199378 0 None -3 3 Human 9.3 pKi = 9.3 Binding
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 199378 0 None -3 3 Human 9.3 pKi = 9.3 Binding
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 199761 0 None -5 3 Human 9.3 pKi = 9.3 Binding
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 199761 0 None -5 3 Human 9.3 pKi = 9.3 Binding
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 193747 0 None -23 7 Human 9.3 pKi = 9.3 Binding
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 193747 0 None -23 7 Human 9.3 pKi = 9.3 Binding
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 77261 0 None 1 3 Human 9.3 pKi = 9.3 Binding
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 77261 0 None 1 3 Human 9.3 pKi = 9.3 Binding
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 132457 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132457 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132478 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132478 0 None - 1 Chinese hamster 9.3 pKi = 9.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 195071 0 None 3 2 Human 9.2 pKi = 9.2 Binding
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 195071 0 None 3 2 Human 9.2 pKi = 9.2 Binding
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 78589 0 None 25 2 Human 9.2 pKi = 9.2 Binding
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 78589 0 None 25 2 Human 9.2 pKi = 9.2 Binding
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 191103 0 None -5 3 Human 9.2 pKi = 9.2 Binding
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 191103 0 None -5 3 Human 9.2 pKi = 9.2 Binding
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 193577 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 193577 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 193916 0 None -3 3 Human 9.2 pKi = 9.2 Binding
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 193916 0 None -3 3 Human 9.2 pKi = 9.2 Binding
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 79264 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 79264 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 59089 0 None 1 3 Human 9.2 pKi = 9.2 Binding
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 59089 0 None 1 3 Human 9.2 pKi = 9.2 Binding
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 59089 0 None 1 3 Human 9.2 pKi = 9.2 Binding
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 59089 0 None 1 3 Human 9.2 pKi = 9.2 Binding
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 106216 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 106216 0 None -1 3 Human 9.2 pKi = 9.2 Binding
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 132472 0 None - 1 Chinese hamster 9.2 pKi = 9.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132472 0 None - 1 Chinese hamster 9.2 pKi = 9.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 112289 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 112289 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 112289 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 112289 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 176911 0 None 1 2 Human 9.1 pKi = 9.1 Binding
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 176911 0 None 1 2 Human 9.1 pKi = 9.1 Binding
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 180010 0 None 1 2 Human 9.1 pKi = 9.1 Binding
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 180010 0 None 1 2 Human 9.1 pKi = 9.1 Binding
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 23416 8 None -16 6 Human 9.1 pKi = 9.1 Binding
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 23416 8 None -16 6 Human 9.1 pKi = 9.1 Binding
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 98729 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 98729 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 63163 0 None -6 9 Human 9.1 pKi = 9.1 Binding
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 63163 0 None -6 9 Human 9.1 pKi = 9.1 Binding
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 193611 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 193611 0 None -1 3 Human 9.1 pKi = 9.1 Binding
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 193725 0 None -3 3 Human 9.1 pKi = 9.1 Binding
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 193725 0 None -3 3 Human 9.1 pKi = 9.1 Binding
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 199939 0 None 31 3 Human 9.1 pKi = 9.1 Binding
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 199939 0 None 31 3 Human 9.1 pKi = 9.1 Binding
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 140222 1 None 5 3 Human 9.1 pKi = 9.1 Binding
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 140222 1 None 5 3 Human 9.1 pKi = 9.1 Binding
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 21197 0 None 1 3 Human 9.1 pKi = 9.1 Binding
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 21197 0 None 1 3 Human 9.1 pKi = 9.1 Binding
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 21197 0 None 1 3 Human 9.1 pKi = 9.1 Binding
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 195086 0 None 13 2 Human 9.1 pKi = 9.1 Binding
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 195086 0 None 13 2 Human 9.1 pKi = 9.1 Binding
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 132466 0 None - 1 Chinese hamster 9.1 pKi = 9.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132466 0 None - 1 Chinese hamster 9.1 pKi = 9.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132464 0 None - 1 Chinese hamster 9.1 pKi = 9.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132464 0 None - 1 Chinese hamster 9.1 pKi = 9.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 91827 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 91827 0 None - 1 Human 9.1 pKi = 9.1 Binding
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 9755 47 None -2 32 Rat 9.0 pKi = 9.0 Binding
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 9755 47 None -2 32 Rat 9.0 pKi = 9.0 Binding
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 9755 47 None -2 32 Rat 9.0 pKi = 9.0 Binding
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 9755 47 None -2 32 Rat 9.0 pKi = 9.0 Binding
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 9755 47 None -2 32 Rat 9.0 pKi = 9.0 Binding
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 207614 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 207614 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 207614 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 207614 0 None - 1 Human 9.0 pKi = 9.0 Binding
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 8625 54 None 1 18 Human 9.0 pKi = 9 Binding
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 8625 54 None 1 18 Human 9.0 pKi = 9 Binding
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 8625 54 None 1 18 Human 9.0 pKi = 9 Binding
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 10269 46 None 13 10 Human 9.0 pKi = 9 Binding
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 10269 46 None 13 10 Human 9.0 pKi = 9 Binding
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 10269 46 None 13 10 Human 9.0 pKi = 9 Binding
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 115313 1 None 4 3 Human 9.0 pKi = 9 Binding
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 115313 1 None 4 3 Human 9.0 pKi = 9 Binding
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 118082 1 None -1 3 Human 9.0 pKi = 9 Binding
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 118082 1 None -1 3 Human 9.0 pKi = 9 Binding
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 63161 0 None -5 3 Human 9.0 pKi = 9 Binding
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 63161 0 None -5 3 Human 9.0 pKi = 9 Binding
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 193612 0 None -5 3 Human 9.0 pKi = 9 Binding
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 193612 0 None -5 3 Human 9.0 pKi = 9 Binding
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 132482 0 None - 1 Chinese hamster 9.0 pKi = 9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132482 0 None - 1 Chinese hamster 9.0 pKi = 9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 78928 0 None 1 3 Human 9.0 pKi = 9 Binding
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 78928 0 None 1 3 Human 9.0 pKi = 9 Binding
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 142079 0 None -1 3 Human 9.0 pKi = 9 Binding
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 142079 0 None -1 3 Human 9.0 pKi = 9 Binding
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 147139 0 None -3 3 Human 9.0 pKi = 9 Binding
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 147139 0 None -3 3 Human 9.0 pKi = 9 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 6927 72 None -13 53 Rat 9.0 pKi = 9.0 Binding
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 115756 0 None 8 2 Human 9.0 pKi = 9.0 Binding
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 115756 0 None 8 2 Human 9.0 pKi = 9.0 Binding
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 6927 72 None -11 53 Human 9.0 pKi = 9.0 Binding
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 6927 72 None -11 53 Human 9.0 pKi = 9.0 Binding
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 6927 72 None -11 53 Human 9.0 pKi = 9.0 Binding
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 6927 72 None -11 53 Human 9.0 pKi = 9.0 Binding
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 132456 0 None - 1 Chinese hamster 9.0 pKi = 9.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132456 0 None - 1 Chinese hamster 9.0 pKi = 9.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 511 7 1 7 4.3 O=C(Nc1ccc(N2CCOCC2)cc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
106 6936 26 None 4 6 Human 8.9 pKi = 8.9 Binding
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 6936 26 None 4 6 Human 8.9 pKi = 8.9 Binding
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 6936 26 None 4 6 Human 8.9 pKi = 8.9 Binding
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 6922 32 None -15 37 Human 8.9 pKi = 8.9 Binding
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 6922 32 None -15 37 Human 8.9 pKi = 8.9 Binding
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 6922 32 None -15 37 Human 8.9 pKi = 8.9 Binding
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 63166 0 None -10 3 Human 8.9 pKi = 8.9 Binding
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 63166 0 None -10 3 Human 8.9 pKi = 8.9 Binding
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 63233 0 None -6 3 Human 8.9 pKi = 8.9 Binding
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 63233 0 None -6 3 Human 8.9 pKi = 8.9 Binding
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 63243 0 None -6 9 Human 8.9 pKi = 8.9 Binding
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 63243 0 None -6 9 Human 8.9 pKi = 8.9 Binding
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 63246 0 None -7 9 Human 8.9 pKi = 8.9 Binding
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 63246 0 None -7 9 Human 8.9 pKi = 8.9 Binding
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 194541 0 None 1 3 Human 8.9 pKi = 8.9 Binding
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 194541 0 None 1 3 Human 8.9 pKi = 8.9 Binding
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 194472 0 None -3 3 Human 8.9 pKi = 8.9 Binding
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 194472 0 None -3 3 Human 8.9 pKi = 8.9 Binding
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 77331 0 None 1 3 Human 8.9 pKi = 8.9 Binding
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 77331 0 None 1 3 Human 8.9 pKi = 8.9 Binding
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 8362 23 None -5 17 Rat 8.9 pKi = 8.9 Binding
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 8362 23 None -5 17 Rat 8.9 pKi = 8.9 Binding
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 8362 23 None -5 17 Rat 8.9 pKi = 8.9 Binding
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 8362 23 None -5 17 Rat 8.9 pKi = 8.9 Binding
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 8362 23 None -5 17 Rat 8.9 pKi = 8.9 Binding
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 18158 0 None 28 3 Human 8.9 pKi = 8.9 Binding
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 18158 0 None 28 3 Human 8.9 pKi = 8.9 Binding
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 18158 0 None 28 3 Human 8.9 pKi = 8.9 Binding
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 178538 0 None -1 2 Human 8.9 pKi = 8.9 Binding
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 178538 0 None -1 2 Human 8.9 pKi = 8.9 Binding
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 179365 0 None -1 2 Human 8.9 pKi = 8.9 Binding
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 179365 0 None -1 2 Human 8.9 pKi = 8.9 Binding
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 132990 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132990 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 74573 17 None -1 15 Rat 8.9 pKi = 8.9 Binding
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 74573 17 None -1 15 Rat 8.9 pKi = 8.9 Binding
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 132477 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132477 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132996 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132996 0 None - 1 Chinese hamster 8.9 pKi = 8.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 25733 0 None 1 3 Human 8.9 pKi = 8.9 Binding
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 25733 0 None 1 3 Human 8.9 pKi = 8.9 Binding
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 486 5 0 5 4.2 Cc1cc(C)c(N2CCN(C(=O)COc3ccc4cccc(N5CCN(C)CC5)c4c3)CC2)c(C)c1 10.1021/jm9703552
44342784 16599 0 None -3 2 Human 8.8 pKi = 8.8 Binding
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 16599 0 None -3 2 Human 8.8 pKi = 8.8 Binding
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 16897 0 None -2 2 Human 8.8 pKi = 8.8 Binding
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 16897 0 None -2 2 Human 8.8 pKi = 8.8 Binding
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 78509 0 None 79 2 Human 8.8 pKi = 8.8 Binding
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 78509 0 None 79 2 Human 8.8 pKi = 8.8 Binding
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 89164 0 None 15 3 Human 8.8 pKi = 8.8 Binding
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 89164 0 None 15 3 Human 8.8 pKi = 8.8 Binding
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 63173 0 None -10 9 Human 8.8 pKi = 8.8 Binding
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 63173 0 None -10 9 Human 8.8 pKi = 8.8 Binding
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 63234 0 None -10 3 Human 8.8 pKi = 8.8 Binding
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 63234 0 None -10 3 Human 8.8 pKi = 8.8 Binding
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 63241 0 None -10 3 Human 8.8 pKi = 8.8 Binding
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 63241 0 None -10 3 Human 8.8 pKi = 8.8 Binding
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 100585 0 None -3 3 Human 8.8 pKi = 8.8 Binding
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 100585 0 None -3 3 Human 8.8 pKi = 8.8 Binding
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 176263 0 None -1 3 Human 8.8 pKi = 8.8 Binding
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 176263 0 None -1 3 Human 8.8 pKi = 8.8 Binding
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 194633 0 None -6 3 Human 8.8 pKi = 8.8 Binding
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 194633 0 None -6 3 Human 8.8 pKi = 8.8 Binding
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 172938 0 None 1 3 Human 8.8 pKi = 8.8 Binding
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 172938 0 None 1 3 Human 8.8 pKi = 8.8 Binding
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 16146 1 None -1 3 Human 8.8 pKi = 8.8 Binding
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 16146 1 None -1 3 Human 8.8 pKi = 8.8 Binding
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 132988 0 None - 1 Chinese hamster 8.8 pKi = 8.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132988 0 None - 1 Chinese hamster 8.8 pKi = 8.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 207839 1 None - 1 Human 8.8 pKi = 8.8 Binding
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 207839 1 None - 1 Human 8.8 pKi = 8.8 Binding
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 207839 1 None - 1 Human 8.8 pKi = 8.8 Binding
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 207839 1 None - 1 Human 8.8 pKi = 8.8 Binding
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 18861 0 None 47 3 Human 8.7 pKi = 8.7 Binding
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 18861 0 None 47 3 Human 8.7 pKi = 8.7 Binding
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 18861 0 None 47 3 Human 8.7 pKi = 8.7 Binding
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 132458 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132458 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132463 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132463 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 142012 0 None 3 6 Human 8.7 pKi = 8.7 Binding
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 142012 0 None 3 6 Human 8.7 pKi = 8.7 Binding
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 127857 3 None -4 3 Human 8.7 pKi = 8.7 Binding
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 127857 3 None -4 3 Human 8.7 pKi = 8.7 Binding
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 77663 0 None 6 3 Human 8.7 pKi = 8.7 Binding
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 77663 0 None 6 3 Human 8.7 pKi = 8.7 Binding
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 78183 0 None 50 2 Human 8.7 pKi = 8.7 Binding
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 78183 0 None 50 2 Human 8.7 pKi = 8.7 Binding
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 63170 0 None -12 9 Human 8.7 pKi = 8.7 Binding
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 63170 0 None -12 9 Human 8.7 pKi = 8.7 Binding
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 63174 0 None -3 3 Human 8.7 pKi = 8.7 Binding
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 63174 0 None -3 3 Human 8.7 pKi = 8.7 Binding
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 63235 0 None -6 3 Human 8.7 pKi = 8.7 Binding
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 63235 0 None -6 3 Human 8.7 pKi = 8.7 Binding
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 63245 0 None -7 3 Human 8.7 pKi = 8.7 Binding
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 63245 0 None -7 3 Human 8.7 pKi = 8.7 Binding
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 63247 0 None -12 3 Human 8.7 pKi = 8.7 Binding
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 63247 0 None -12 3 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 182834 0 None -1 3 Human 8.7 pKi = 8.7 Binding
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 182834 0 None -1 3 Human 8.7 pKi = 8.7 Binding
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 194542 0 None -6 3 Human 8.7 pKi = 8.7 Binding
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 194542 0 None -6 3 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 196807 0 None -3 3 Human 8.7 pKi = 8.7 Binding
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 196807 0 None -3 3 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 194863 0 None -3 12 Human 8.7 pKi = 8.7 Binding
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 79326 0 None 2 3 Human 8.7 pKi = 8.7 Binding
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 79326 0 None 2 3 Human 8.7 pKi = 8.7 Binding
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 147669 0 None -1 3 Human 8.7 pKi = 8.7 Binding
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 147669 0 None -1 3 Human 8.7 pKi = 8.7 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 10104 118 None -93 66 Human 8.0 pKi = 8 Binding
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 10104 118 None -93 66 Human 8.0 pKi = 8 Binding
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 10104 118 None -93 66 Human 8.0 pKi = 8 Binding
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 10104 118 None -93 66 Human 8.0 pKi = 8 Binding
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 10104 118 None -93 66 Human 8.0 pKi = 8 Binding
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 10479 68 None -3 32 Human 8.0 pKi = 8 Binding
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 10479 68 None -3 32 Human 8.0 pKi = 8 Binding
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 10479 68 None -3 32 Human 8.0 pKi = 8 Binding
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 10479 68 None -3 32 Human 8.0 pKi = 8 Binding
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 10479 68 None -3 32 Human 8.0 pKi = 8 Binding
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 16132 12 None - 1 Human 8.0 pKi = 8 Binding
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 16132 12 None - 1 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10304 15 None -7 9 Human 8.0 pKi = 8 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 10273 47 None -1 13 Human 8.0 pKi = 8 Binding
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 132473 0 None - 1 Chinese hamster 8.0 pKi = 8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132473 0 None - 1 Chinese hamster 8.0 pKi = 8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 10107 82 None -1 5 Human 8.0 pKi = 8 Binding
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 10107 82 None -1 5 Human 8.0 pKi = 8 Binding
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 10107 82 None -1 5 Human 8.0 pKi = 8 Binding
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 10107 82 None -1 5 Human 8.0 pKi = 8 Binding
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 10107 82 None -1 5 Human 8.0 pKi = 8 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8 Binding
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 10.1021/jm9703552
1251 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
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 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
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 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
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 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
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 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
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 175953 0 None -36 2 Human 8.0 pKi = 8.0 Binding
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 175953 0 None -36 2 Human 8.0 pKi = 8.0 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8.0 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8.0 Binding
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 6824 49 None -4 19 Human 8.0 pKi = 8.0 Binding
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 214787 0 None -45 8 Human 7.0 pKi = 7 Binding
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 214787 0 None -45 8 Human 7.0 pKi = 7 Binding
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 108757 0 None -25 4 Human 7.0 pKi = 7 Binding
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 108757 0 None -25 4 Human 7.0 pKi = 7 Binding
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 108757 0 None -25 4 Human 7.0 pKi = 7 Binding
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 75460 0 None -10 3 Human 7.0 pKi = 7 Binding
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 75460 0 None -10 3 Human 7.0 pKi = 7 Binding
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 100745 0 None -10 3 Human 7.0 pKi = 7 Binding
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 100745 0 None -10 3 Human 7.0 pKi = 7 Binding
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 195105 0 None -165 2 Human 7.0 pKi = 7 Binding
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 195105 0 None -165 2 Human 7.0 pKi = 7 Binding
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 191102 0 None 1 3 Human 7.0 pKi = 7 Binding
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 191102 0 None 1 3 Human 7.0 pKi = 7 Binding
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 194743 0 None -63 3 Human 7.0 pKi = 7 Binding
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 194743 0 None -63 3 Human 7.0 pKi = 7 Binding
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 185351 5 None -50 22 Human 7.0 pKi = 7 Binding
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 185351 5 None -50 22 Human 7.0 pKi = 7 Binding
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 185351 5 None -50 22 Human 7.0 pKi = 7 Binding
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 185351 5 None -50 22 Human 7.0 pKi = 7 Binding
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 126475 0 None -14 3 Rat 7.0 pKi = 7 Binding
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 126475 0 None -14 3 Rat 7.0 pKi = 7 Binding
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 109259 0 None -316 4 Human 6.0 pKi = 6 Binding
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 109259 0 None -316 4 Human 6.0 pKi = 6 Binding
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 109259 0 None -316 4 Human 6.0 pKi = 6 Binding
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 7152 29 None -57 19 Rat 6.0 pKi = 6 Binding
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 7152 29 None -57 19 Rat 6.0 pKi = 6 Binding
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 7152 29 None -57 19 Rat 6.0 pKi = 6 Binding
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 73987 25 None -1023 14 Rat 6.0 pKi = 6 Binding
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 73987 25 None -1023 14 Rat 6.0 pKi = 6 Binding
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 211140 0 None -25 7 Human 6.0 pKi = 6 Binding
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 211140 0 None -25 7 Human 6.0 pKi = 6 Binding
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 7258 124 None -380 51 Human 6.0 pKi = 6 Binding
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 7258 124 None -380 51 Human 6.0 pKi = 6 Binding
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 7258 124 None -380 51 Human 6.0 pKi = 6 Binding
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 7258 124 None -380 51 Human 6.0 pKi = 6 Binding
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 7258 124 None -380 51 Human 6.0 pKi = 6 Binding
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 7745 93 None -151 90 Human 6.0 pKi = 6 Binding
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 7745 93 None -151 90 Human 6.0 pKi = 6 Binding
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 7745 93 None -151 90 Human 6.0 pKi = 6 Binding
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 7745 93 None -151 90 Human 6.0 pKi = 6 Binding
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 7745 93 None -151 90 Human 6.0 pKi = 6 Binding
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 9688 112 None -199 65 Human 6.0 pKi = 6 Binding
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 9688 112 None -199 65 Human 6.0 pKi = 6 Binding
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 9688 112 None -199 65 Human 6.0 pKi = 6 Binding
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 9688 112 None -199 65 Human 6.0 pKi = 6 Binding
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 10285 44 None -741 12 Human 6.0 pKi = 6 Binding
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 10285 44 None -741 12 Human 6.0 pKi = 6 Binding
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 10285 44 None -741 12 Human 6.0 pKi = 6 Binding
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 10285 44 None -741 12 Human 6.0 pKi = 6 Binding
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 10285 44 None -741 12 Human 6.0 pKi = 6 Binding
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 17234 0 None -501 7 Human 6.0 pKi = 6 Binding
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 17234 0 None -501 7 Human 6.0 pKi = 6 Binding
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 97071 0 None -2511 10 Human 6.0 pKi = 6 Binding
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 97071 0 None -2511 10 Human 6.0 pKi = 6 Binding
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 97546 0 None -50 3 Human 6.0 pKi = 6 Binding
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 97546 0 None -50 3 Human 6.0 pKi = 6 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 456 6 1 6 4.1 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cc(C#N)cc2n1 10.1016/j.bmcl.2006.11.031
11046087 11719 0 None -134 4 Human 6.0 pKi = 6 Binding
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 11719 0 None -134 4 Human 6.0 pKi = 6 Binding
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 11902 0 None -158 4 Human 6.0 pKi = 6 Binding
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 11902 0 None -158 4 Human 6.0 pKi = 6 Binding
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 33777 1 None -2 3 Rat 6.0 pKi = 6 Binding
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 33777 1 None -2 3 Rat 6.0 pKi = 6 Binding
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 35894 1 None -3 3 Rat 6.0 pKi = 6 Binding
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 35894 1 None -3 3 Rat 6.0 pKi = 6 Binding
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 212292 76 None -44 34 Rat 5.0 pKi = 5 Binding
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 212292 76 None -44 34 Rat 5.0 pKi = 5 Binding
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 212292 76 None -44 34 Rat 5.0 pKi = 5 Binding
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 193264 1 None -20 5 Human 6.0 pKi = 6.0 Binding
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 193264 1 None -20 5 Human 6.0 pKi = 6.0 Binding
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 10650 121 None -204 25 Rat 5.0 pKi = 5.0 Binding
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 10650 121 None -204 25 Rat 5.0 pKi = 5.0 Binding
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 10650 121 None -204 25 Rat 5.0 pKi = 5.0 Binding
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 10650 121 None -204 25 Rat 5.0 pKi = 5.0 Binding
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 72837 0 None -30 2 Human 5.0 pKi = 5.0 Binding
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 72837 0 None -30 2 Human 5.0 pKi = 5.0 Binding
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 179525 0 None -4 2 Human 7.0 pKi = 7.0 Binding
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 179525 0 None -4 2 Human 7.0 pKi = 7.0 Binding
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 152015 0 None -14 4 Human 7.0 pKi = 7.0 Binding
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 152015 0 None -14 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
11297 74119 18 None -26 6 Rat 6.0 pKi = 6.0 Binding
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 74119 18 None -26 6 Rat 6.0 pKi = 6.0 Binding
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 124265 0 None -131 12 Human 6.0 pKi = 6.0 Binding
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 124265 0 None -131 12 Human 6.0 pKi = 6.0 Binding
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 66701 0 None -23 2 Human 7.0 pKi = 7.0 Binding
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 66701 0 None -23 2 Human 7.0 pKi = 7.0 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 294 4 1 2 4.3 C1=CCN(CCc2c[nH]c3ccc(-c4cccs4)cc23)C1 10.1016/s0960-894x(00)00133-5
4431 9506 25 None -3090 12 Rat 6.0 pKi = 6.0 Binding
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 9506 25 None -3090 12 Rat 6.0 pKi = 6.0 Binding
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 9506 25 None -3090 12 Rat 6.0 pKi = 6.0 Binding
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 9292 24 None -251 67 Rat 7.0 pKi = 7.0 Binding
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 9292 24 None -251 67 Rat 7.0 pKi = 7.0 Binding
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 9292 24 None -251 67 Rat 7.0 pKi = 7.0 Binding
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 9292 24 None -251 67 Rat 7.0 pKi = 7.0 Binding
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 9292 24 None -251 67 Rat 7.0 pKi = 7.0 Binding
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 211096 0 None -154 4 Human 7.0 pKi = 7.0 Binding
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 211096 0 None -154 4 Human 7.0 pKi = 7.0 Binding
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 109867 0 None -22 3 Human 6.0 pKi = 6.0 Binding
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 109867 0 None -22 3 Human 6.0 pKi = 6.0 Binding
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 29379 0 None -295 2 Rat 6.0 pKi = 6.0 Binding
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 29379 0 None -295 2 Rat 6.0 pKi = 6.0 Binding
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 114307 0 None -3 4 Human 8.0 pKi = 8.0 Binding
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 114307 0 None -3 4 Human 8.0 pKi = 8.0 Binding
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 18151 0 None 21 2 Human 8.0 pKi = 8.0 Binding
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 18151 0 None 21 2 Human 8.0 pKi = 8.0 Binding
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 18151 0 None 21 2 Human 8.0 pKi = 8.0 Binding
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 213899 0 None -7 9 Human 8.0 pKi = 8.0 Binding
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 213899 0 None -7 9 Human 8.0 pKi = 8.0 Binding
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 120586 0 None -2 2 Human 8.0 pKi = 8.0 Binding
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 120586 0 None -2 2 Human 8.0 pKi = 8.0 Binding
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 9274 52 None -40 43 Rat 8.0 pKi = 8.0 Binding
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 9274 52 None -40 43 Rat 8.0 pKi = 8.0 Binding
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 9274 52 None -40 43 Rat 8.0 pKi = 8.0 Binding
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 9274 52 None -40 43 Rat 8.0 pKi = 8.0 Binding
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 9274 52 None -40 43 Rat 8.0 pKi = 8.0 Binding
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 207724 22 None -22 20 Rat 8.0 pKi = 8.0 Binding
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 207724 22 None -22 20 Rat 8.0 pKi = 8.0 Binding
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 207724 22 None -22 20 Rat 8.0 pKi = 8.0 Binding
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 109655 0 None -9 4 Human 8.0 pKi = 8.0 Binding
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 109655 0 None -9 4 Human 8.0 pKi = 8.0 Binding
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 210947 0 None -18 4 Human 8.0 pKi = 8.0 Binding
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 210947 0 None -18 4 Human 8.0 pKi = 8.0 Binding
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 133004 0 None - 1 Chinese hamster 8.0 pKi = 8.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 133004 0 None - 1 Chinese hamster 8.0 pKi = 8.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 5 0 5 3.7 CN(C)C(=O)c1cc2c(Br)ccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44404394 139593 0 None 3 7 Human 8.0 pKi = 8.0 Binding
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 139593 0 None 3 7 Human 8.0 pKi = 8.0 Binding
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 214971 95 None 2 5 Rat 7.9 pKi = 7.9 Binding
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 214971 95 None 2 5 Rat 7.9 pKi = 7.9 Binding
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 214184 0 None -223 9 Human 7.0 pKi = 7.0 Binding
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 214184 0 None -223 9 Human 7.0 pKi = 7.0 Binding
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 126764 0 None -11 2 Human 7.0 pKi = 7.0 Binding
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 126764 0 None -11 2 Human 7.0 pKi = 7.0 Binding
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 11642 1 None -4 3 Human 7.0 pKi = 7.0 Binding
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 11642 1 None -4 3 Human 7.0 pKi = 7.0 Binding
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 11788 0 None -85 4 Human 6.0 pKi = 6.0 Binding
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 11788 0 None -85 4 Human 6.0 pKi = 6.0 Binding
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 36809 5 None -28 4 Rat 6.0 pKi = 6.0 Binding
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 36809 5 None -28 4 Rat 6.0 pKi = 6.0 Binding
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 67040 0 None -13 2 Human 7.0 pKi = 7.0 Binding
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 67040 0 None -13 2 Human 7.0 pKi = 7.0 Binding
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 140252 0 None -8 4 Human 6.9 pKi = 6.9 Binding
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 140252 0 None -8 4 Human 6.9 pKi = 6.9 Binding
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 172053 0 None -40 4 Human 6.9 pKi = 6.9 Binding
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 172053 0 None -40 4 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 451 9 1 4 4.5 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
115 10563 80 None 1 27 Rat 6.9 pKi = 6.9 Binding
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 10563 80 None 1 27 Rat 6.9 pKi = 6.9 Binding
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 10563 80 None 1 27 Rat 6.9 pKi = 6.9 Binding
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 79119 0 None -97 9 Rat 6.9 pKi = 6.9 Binding
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 79119 0 None -97 9 Rat 6.9 pKi = 6.9 Binding
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 108646 0 None -33 2 Human 6.9 pKi = 6.9 Binding
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 108646 0 None -33 2 Human 6.9 pKi = 6.9 Binding
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 69807 0 None -199 4 Human 6.9 pKi = 6.9 Binding
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 69807 0 None -199 4 Human 6.9 pKi = 6.9 Binding
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 221652 0 None 1 9 Human 7.9 pKi = 7.9 Binding
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 207871 4 None - 1 Human 7.9 pKi = 7.9 Binding
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 207871 4 None - 1 Human 7.9 pKi = 7.9 Binding
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 134332 0 None -39 2 Human 7.9 pKi = 7.9 Binding
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 134332 0 None -39 2 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 207871 4 None - 1 Human 7.9 pKi = 7.9 Binding
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 207871 4 None - 1 Human 7.9 pKi = 7.9 Binding
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 78445 0 None 19 7 Human 7.9 pKi = 7.9 Binding
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 78445 0 None 19 7 Human 7.9 pKi = 7.9 Binding
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 78445 0 None 19 7 Human 7.9 pKi = 7.9 Binding
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 140324 0 None 19 2 Human 7.9 pKi = 7.9 Binding
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 140324 0 None 19 2 Human 7.9 pKi = 7.9 Binding
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 101177 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 101177 0 None - 1 Human 7.9 pKi = 7.9 Binding
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 10289 4 None -3 13 Human 7.9 pKi = 7.9 Binding
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 10289 4 None -3 13 Human 7.9 pKi = 7.9 Binding
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 10289 4 None -3 13 Human 7.9 pKi = 7.9 Binding
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 83906 0 None 3 3 Human 7.9 pKi = 7.9 Binding
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 83906 0 None 3 3 Human 7.9 pKi = 7.9 Binding
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 63167 0 None -39 3 Human 7.9 pKi = 7.9 Binding
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 63167 0 None -39 3 Human 7.9 pKi = 7.9 Binding
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 196704 0 None -6 3 Human 7.9 pKi = 7.9 Binding
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 196704 0 None -6 3 Human 7.9 pKi = 7.9 Binding
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 194435 0 None -7 3 Human 7.9 pKi = 7.9 Binding
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 194435 0 None -7 3 Human 7.9 pKi = 7.9 Binding
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 199892 0 None -7 11 Human 7.9 pKi = 7.9 Binding
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 199892 0 None -7 11 Human 7.9 pKi = 7.9 Binding
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 74692 0 None -2 2 Human 6.9 pKi = 6.9 Binding
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 74692 0 None -2 2 Human 6.9 pKi = 6.9 Binding
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 69825 7 None - 1 Rat 6.9 pKi = 6.9 Binding
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 69825 7 None - 1 Rat 6.9 pKi = 6.9 Binding
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 158115 0 None -229 10 Human 5.9 pKi = 5.9 Binding
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 158115 0 None -229 10 Human 5.9 pKi = 5.9 Binding
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 11477 0 None -158 8 Human 5.9 pKi = 5.9 Binding
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 11477 0 None -158 8 Human 5.9 pKi = 5.9 Binding
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 179410 0 None -208 4 Human 5.9 pKi = 5.9 Binding
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 179410 0 None -208 4 Human 5.9 pKi = 5.9 Binding
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 9947 58 None -39 31 Rat 5.9 pKi = 5.9 Binding
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 9947 58 None -39 31 Rat 5.9 pKi = 5.9 Binding
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 9947 58 None -39 31 Rat 5.9 pKi = 5.9 Binding
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 9947 58 None -39 31 Rat 5.9 pKi = 5.9 Binding
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 9947 58 None -39 31 Rat 5.9 pKi = 5.9 Binding
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 173622 0 None -93 11 Human 5.9 pKi = 5.9 Binding
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 173622 0 None -93 11 Human 5.9 pKi = 5.9 Binding
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 211099 0 None -52 4 Human 6.9 pKi = 6.9 Binding
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 211099 0 None -52 4 Human 6.9 pKi = 6.9 Binding
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 68856 0 None -77 7 Human 6.9 pKi = 6.9 Binding
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 68856 0 None -77 7 Human 6.9 pKi = 6.9 Binding
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 111237 4 None -11 13 Human 5.9 pKi = 5.9 Binding
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 111237 4 None -11 13 Human 5.9 pKi = 5.9 Binding
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 111237 4 None -11 13 Human 5.9 pKi = 5.9 Binding
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 111237 4 None -11 13 Human 5.9 pKi = 5.9 Binding
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 11551 101 None -51 34 Rat 4.9 pKi = 4.9 Binding
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 11551 101 None -51 34 Rat 4.9 pKi = 4.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 nan
62597539 112989 2 None -1 2 Human 5.9 pKi = 5.9 Binding
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 112989 2 None -1 2 Human 5.9 pKi = 5.9 Binding
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 112989 2 None -1 2 Human 5.9 pKi = 5.9 Binding
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 86987 1 None 1 3 Human 6.9 pKi = 6.9 Binding
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 86987 1 None 1 3 Human 6.9 pKi = 6.9 Binding
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 182275 0 None -50 3 Human 6.9 pKi = 6.9 Binding
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 182275 0 None -50 3 Human 6.9 pKi = 6.9 Binding
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 182473 0 None -15 3 Human 6.9 pKi = 6.9 Binding
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 182473 0 None -15 3 Human 6.9 pKi = 6.9 Binding
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 194865 0 None -501 3 Human 6.9 pKi = 6.9 Binding
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 194865 0 None -501 3 Human 6.9 pKi = 6.9 Binding
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 214761 0 None -1000 5 Human 5.9 pKi = 5.9 Binding
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 214761 0 None -1000 5 Human 5.9 pKi = 5.9 Binding
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 168620 0 None -3981 11 Human 5.9 pKi = 5.9 Binding
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 168620 0 None -3981 11 Human 5.9 pKi = 5.9 Binding
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 97545 0 None -794 3 Human 5.9 pKi = 5.9 Binding
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 97545 0 None -794 3 Human 5.9 pKi = 5.9 Binding
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 194455 0 None -7 3 Human 5.9 pKi = 5.9 Binding
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 194455 0 None -7 3 Human 5.9 pKi = 5.9 Binding
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 195566 0 None -125 2 Human 6.9 pKi = 6.9 Binding
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 195566 0 None -125 2 Human 6.9 pKi = 6.9 Binding
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 195817 0 None -9 2 Human 6.9 pKi = 6.9 Binding
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 195817 0 None -9 2 Human 6.9 pKi = 6.9 Binding
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 8083 62 None -501 50 Rat 5.9 pKi = 5.9 Binding
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 8083 62 None -501 50 Rat 5.9 pKi = 5.9 Binding
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 8083 62 None -501 50 Rat 5.9 pKi = 5.9 Binding
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 8083 62 None -501 50 Rat 5.9 pKi = 5.9 Binding
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 8083 62 None -501 50 Rat 5.9 pKi = 5.9 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 nan
50878551 97520 61 None -7 18 Human 6.9 pKi = 6.9 Binding
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 97520 61 None -7 18 Human 6.9 pKi = 6.9 Binding
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 97520 61 None -7 18 Human 6.9 pKi = 6.9 Binding
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 97520 61 None -7 18 Human 6.9 pKi = 6.9 Binding
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 16591 0 None -6 2 Human 7.9 pKi = 7.9 Binding
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 16591 0 None -6 2 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 6936 26 None -4 6 Rat 7.9 pKi = 7.9 Binding
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 6936 26 None -4 6 Rat 7.9 pKi = 7.9 Binding
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 6936 26 None -4 6 Rat 7.9 pKi = 7.9 Binding
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 24693 0 None -24 6 Human 7.9 pKi = 7.9 Binding
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 24693 0 None -24 6 Human 7.9 pKi = 7.9 Binding
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 20883 0 None 35 2 Human 7.9 pKi = 7.9 Binding
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 20883 0 None 35 2 Human 7.9 pKi = 7.9 Binding
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 78772 0 None -2 6 Human 7.9 pKi = 7.9 Binding
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 78772 0 None -2 6 Human 7.9 pKi = 7.9 Binding
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 104948 69 None -1 3 Rat 7.9 pKi = 7.9 Binding
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 104948 69 None -1 3 Rat 7.9 pKi = 7.9 Binding
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 63036 0 None -4 2 Human 6.9 pKi = 6.9 Binding
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 63036 0 None -4 2 Human 6.9 pKi = 6.9 Binding
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 91957 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 91957 0 None - 1 Human 5.9 pKi = 5.9 Binding
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 109251 0 None - 1 Rat 5.9 pKi = 5.9 Binding
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 109251 0 None - 1 Rat 5.9 pKi = 5.9 Binding
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 9271 16 None -7585 25 Rat 4.9 pKi = 4.9 Binding
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 9271 16 None -7585 25 Rat 4.9 pKi = 4.9 Binding
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 9271 16 None -7585 25 Rat 4.9 pKi = 4.9 Binding
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 120855 0 None -15 8 Human 6.9 pKi = 6.9 Binding
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 120855 0 None -15 8 Human 6.9 pKi = 6.9 Binding
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 212130 0 None -15 3 Human 6.9 pKi = 6.9 Binding
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 212130 0 None -15 3 Human 6.9 pKi = 6.9 Binding
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 40518 0 None -363 2 Rat 5.9 pKi = 5.9 Binding
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 40518 0 None -363 2 Rat 5.9 pKi = 5.9 Binding
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 40518 0 None -363 2 Rat 5.9 pKi = 5.9 Binding
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 67072 0 None -40 2 Human 6.9 pKi = 6.9 Binding
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 67072 0 None -40 2 Human 6.9 pKi = 6.9 Binding
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 144192 0 None -42 19 Human 5.9 pKi = 5.9 Binding
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 144192 0 None -42 19 Human 5.9 pKi = 5.9 Binding
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 111235 0 None -131 24 Human 5.9 pKi = 5.9 Binding
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 111235 0 None -131 24 Human 5.9 pKi = 5.9 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.7 CN1CCc2c(c3cccc4c3n2-c2ccccc2CC4)C1 10.1016/j.bmcl.2013.12.024
10498633 170082 0 None 1 3 Human 6.9 pKi = 6.9 Binding
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 170082 0 None 1 3 Human 6.9 pKi = 6.9 Binding
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 215378 21 None - 1 Rat 5.9 pKi = 5.9 Binding
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 126938 8 None -1 2 Rat 6.9 pKi = 6.9 Binding
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 126938 8 None -1 2 Rat 6.9 pKi = 6.9 Binding
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 84009 0 None -245 2 Rat 4.9 pKi = 4.9 Binding
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 84009 0 None -245 2 Rat 4.9 pKi = 4.9 Binding
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 111235 0 None -131 24 Human 5.9 pKi = 5.9 Binding
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 111235 0 None -131 24 Human 5.9 pKi = 5.9 Binding
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 74574 19 None -43 18 Rat 5.9 pKi = 5.9 Binding
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 74574 19 None -43 18 Rat 5.9 pKi = 5.9 Binding
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 191648 1 None -52 7 Human 5.9 pKi = 5.9 Binding
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 191648 1 None -52 7 Human 5.9 pKi = 5.9 Binding
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 69842 35 None - 1 Rat 5.9 pKi = 5.9 Binding
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 69842 35 None - 1 Rat 5.9 pKi = 5.9 Binding
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 108864 1 None -22 4 Human 6.9 pKi = 6.9 Binding
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 108864 1 None -22 4 Human 6.9 pKi = 6.9 Binding
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 108864 1 None -22 4 Human 6.9 pKi = 6.9 Binding
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 108864 1 None -22 4 Human 6.9 pKi = 6.9 Binding
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 214307 1 None -1 4 Human 7.9 pKi = 7.9 Binding
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 214307 1 None -1 4 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 8633 14 None 39 3 Human 7.9 pKi = 7.9 Binding
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 16943 0 None -18 2 Human 7.9 pKi = 7.9 Binding
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 16943 0 None -18 2 Human 7.9 pKi = 7.9 Binding
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 116891 0 None -4 2 Human 7.9 pKi = 7.9 Binding
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 116891 0 None -4 2 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 10879 53 None -4 8 Human 7.9 pKi = 7.9 Binding
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 41967 0 None -2 4 Human 7.9 pKi = 7.9 Binding
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 41967 0 None -2 4 Human 7.9 pKi = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pKi = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pKi = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pKi = 7.9 Binding
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 6927 72 None -11 53 Human 7.9 pKi = 7.9 Binding
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 16126 2 None 2 3 Human 7.9 pKi = 7.9 Binding
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 16126 2 None 2 3 Human 7.9 pKi = 7.9 Binding
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 69806 0 None -15 3 Human 7.9 pKi = 7.9 Binding
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 69806 0 None -15 3 Human 7.9 pKi = 7.9 Binding
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 116564 0 None -5 3 Human 7.9 pKi = 7.9 Binding
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 116564 0 None -5 3 Human 7.9 pKi = 7.9 Binding
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 133000 0 None - 1 Chinese hamster 7.9 pKi = 7.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 133000 0 None - 1 Chinese hamster 7.9 pKi = 7.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 108627 20 None -35 2 Human 7.9 pKi = 7.9 Binding
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 108627 20 None -35 2 Human 7.9 pKi = 7.9 Binding
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 126681 0 None -11 2 Human 6.9 pKi = 6.9 Binding
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 126681 0 None -11 2 Human 6.9 pKi = 6.9 Binding
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 126730 0 None -12 2 Human 6.9 pKi = 6.9 Binding
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 126730 0 None -12 2 Human 6.9 pKi = 6.9 Binding
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 133003 0 None - 1 Chinese hamster 6.9 pKi = 6.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 133003 0 None - 1 Chinese hamster 6.9 pKi = 6.9 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 206166 0 None - 1 Rat 5.9 pKi = 5.9 Binding
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 206166 0 None - 1 Rat 5.9 pKi = 5.9 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 2.4 N#CC1=Cc2cccc(OCC3CCCNC3)c2OC1 10.1021/jm970806i
10066481 25248 0 None -371 3 Rat 5.9 pKi = 5.9 Binding
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 25248 0 None -371 3 Rat 5.9 pKi = 5.9 Binding
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 122918 0 None -501 2 Rat 5.9 pKi = 5.9 Binding
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 122918 0 None -501 2 Rat 5.9 pKi = 5.9 Binding
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 109635 97 None -17 25 Rat 5.9 pKi = 5.9 Binding
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 109635 97 None -17 25 Rat 5.9 pKi = 5.9 Binding
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 109635 97 None -17 25 Rat 5.9 pKi = 5.9 Binding
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 210953 1 None -93 4 Human 6.9 pKi = 6.9 Binding
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 210953 1 None -93 4 Human 6.9 pKi = 6.9 Binding
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 72046 2 None -26 2 Human 5.8 pKi = 5.8 Binding
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 72046 2 None -26 2 Human 5.8 pKi = 5.8 Binding
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 169015 0 None -5 13 Human 5.8 pKi = 5.8 Binding
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 169015 0 None -5 13 Human 5.8 pKi = 5.8 Binding
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 9641 38 None -18 30 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
2404 9641 38 None -18 30 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
4543 9641 38 None -18 30 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
CHEMBL445 9641 38 None -18 30 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
DB00540 9641 38 None -18 30 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 nan
76326512 113027 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 113027 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 113027 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 153918 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 153918 0 None - 1 Human 5.8 pKi = 5.8 Binding
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 152019 0 None -15 4 Human 7.8 pKi = 7.8 Binding
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 152019 0 None -15 4 Human 7.8 pKi = 7.8 Binding
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 208509 0 None -15 8 Human 7.8 pKi = 7.8 Binding
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 208509 0 None -15 8 Human 7.8 pKi = 7.8 Binding
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 110578 0 None -3 4 Human 7.8 pKi = 7.8 Binding
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 110578 0 None -3 4 Human 7.8 pKi = 7.8 Binding
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 194889 0 None -61 2 Human 7.8 pKi = 7.8 Binding
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 194889 0 None -61 2 Human 7.8 pKi = 7.8 Binding
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 85793 0 None 15 3 Human 7.8 pKi = 7.8 Binding
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 85793 0 None 15 3 Human 7.8 pKi = 7.8 Binding
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 197705 0 None -15 3 Human 7.8 pKi = 7.8 Binding
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 197705 0 None -15 3 Human 7.8 pKi = 7.8 Binding
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 194905 0 None -25 3 Human 7.8 pKi = 7.8 Binding
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 194905 0 None -25 3 Human 7.8 pKi = 7.8 Binding
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 77294 0 None -1 3 Human 7.8 pKi = 7.8 Binding
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 77294 0 None -1 3 Human 7.8 pKi = 7.8 Binding
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 78683 0 None -6 3 Human 7.8 pKi = 7.8 Binding
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 78683 0 None -6 3 Human 7.8 pKi = 7.8 Binding
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 215022 7 None 1 3 Rat 7.8 pKi = 7.8 Binding
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 215022 7 None 1 3 Rat 7.8 pKi = 7.8 Binding
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 18152 0 None -41 2 Human 6.8 pKi = 6.8 Binding
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 18152 0 None -41 2 Human 6.8 pKi = 6.8 Binding
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 18152 0 None -41 2 Human 6.8 pKi = 6.8 Binding
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 11776 0 None -12 4 Human 6.8 pKi = 6.8 Binding
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 11776 0 None -12 4 Human 6.8 pKi = 6.8 Binding
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 106952 0 None 7 2 Rat 5.8 pKi = 5.8 Binding
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 106952 0 None 7 2 Rat 5.8 pKi = 5.8 Binding
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 37037 5 None -19 3 Rat 5.8 pKi = 5.8 Binding
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 37037 5 None -19 3 Rat 5.8 pKi = 5.8 Binding
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 108898 0 None -11 4 Human 5.8 pKi = 5.8 Binding
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 108898 0 None -11 4 Human 5.8 pKi = 5.8 Binding
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 29651 0 None -1071 2 Rat 5.8 pKi = 5.8 Binding
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 29651 0 None -1071 2 Rat 5.8 pKi = 5.8 Binding
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 84639 15 None - 1 Rat 5.8 pKi = 5.8 Binding
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 84639 15 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 174 2 2 1 2.1 C[C@H](N)Cc1c[nH]c2ccccc12 10.1021/jm00402a026
10070281 212340 0 None -28 3 Human 6.8 pKi = 6.8 Binding
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 212340 0 None -28 3 Human 6.8 pKi = 6.8 Binding
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 205516 8 None -74 9 Human 5.8 pKi = 5.8 Binding
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 205516 8 None -74 9 Human 5.8 pKi = 5.8 Binding
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 69841 2 None - 1 Rat 5.8 pKi = 5.8 Binding
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 69841 2 None - 1 Rat 5.8 pKi = 5.8 Binding
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 212148 0 None -4 3 Human 6.8 pKi = 6.8 Binding
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 212148 0 None -4 3 Human 6.8 pKi = 6.8 Binding
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 212494 0 None -7 3 Human 6.8 pKi = 6.8 Binding
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 212494 0 None -7 3 Human 6.8 pKi = 6.8 Binding
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 201496 63 None -2 3 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 201496 63 None -2 3 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 201496 63 None -2 3 Rat 4.8 pKi = 4.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 109852 0 None -21 2 Human 5.8 pKi = 5.8 Binding
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 109852 0 None -21 2 Human 5.8 pKi = 5.8 Binding
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 109852 0 None -21 2 Human 5.8 pKi = 5.8 Binding
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 109852 0 None -21 2 Human 5.8 pKi = 5.8 Binding
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 24534 0 None 5 2 Human 5.8 pKi = 5.8 Binding
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 24534 0 None 5 2 Human 5.8 pKi = 5.8 Binding
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 20480 0 None -12 4 Human 6.8 pKi = 6.8 Binding
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 20480 0 None -12 4 Human 6.8 pKi = 6.8 Binding
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 20480 0 None -12 4 Human 6.8 pKi = 6.8 Binding
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 91164 0 None -125 4 Human 6.8 pKi = 6.8 Binding
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 91164 0 None -125 4 Human 6.8 pKi = 6.8 Binding
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 91164 0 None -125 4 Human 6.8 pKi = 6.8 Binding
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 85764 0 None -50 3 Human 6.8 pKi = 6.8 Binding
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 85764 0 None -50 3 Human 6.8 pKi = 6.8 Binding
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 98755 0 None -3 3 Human 6.8 pKi = 6.8 Binding
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 98755 0 None -3 3 Human 6.8 pKi = 6.8 Binding
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 182838 0 None -39 3 Human 6.8 pKi = 6.8 Binding
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 182838 0 None -39 3 Human 6.8 pKi = 6.8 Binding
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 196277 0 None -100 3 Human 6.8 pKi = 6.8 Binding
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 196277 0 None -100 3 Human 6.8 pKi = 6.8 Binding
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 194425 0 None -63 3 Human 6.8 pKi = 6.8 Binding
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 194425 0 None -63 3 Human 6.8 pKi = 6.8 Binding
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 103181 0 None -2511 4 Human 5.8 pKi = 5.8 Binding
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 103181 0 None -2511 4 Human 5.8 pKi = 5.8 Binding
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 24767 6 None -512 7 Human 5.8 pKi = 5.8 Binding
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 24767 6 None -512 7 Human 5.8 pKi = 5.8 Binding
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 121366 0 None -398 8 Human 5.8 pKi = 5.8 Binding
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 121366 0 None -398 8 Human 5.8 pKi = 5.8 Binding
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 97070 0 None -630 10 Human 5.8 pKi = 5.8 Binding
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 97070 0 None -630 10 Human 5.8 pKi = 5.8 Binding
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 194456 0 None -316 3 Human 5.8 pKi = 5.8 Binding
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 194456 0 None -316 3 Human 5.8 pKi = 5.8 Binding
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 33360 0 None -3 3 Rat 5.8 pKi = 5.8 Binding
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 33360 0 None -3 3 Rat 5.8 pKi = 5.8 Binding
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 193628 0 None -4 2 Human 7.8 pKi = 7.8 Binding
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 193628 0 None -4 2 Human 7.8 pKi = 7.8 Binding
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 132469 0 None - 1 Chinese hamster 7.8 pKi = 7.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132469 0 None - 1 Chinese hamster 7.8 pKi = 7.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 18832 0 None 63 2 Human 7.8 pKi = 7.8 Binding
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 18832 0 None 63 2 Human 7.8 pKi = 7.8 Binding
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 78883 0 None 19 5 Human 7.8 pKi = 7.8 Binding
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 78883 0 None 19 5 Human 7.8 pKi = 7.8 Binding
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 221684 0 None -19 8 Human 6.8 pKi = 6.8 Binding
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 222278 0 None -7 7 Human 6.8 pKi = 6.8 Binding
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 11490 0 None -144 4 Human 5.8 pKi = 5.8 Binding
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 11490 0 None -144 4 Human 5.8 pKi = 5.8 Binding
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 129801 0 None -5 2 Human 5.8 pKi = 5.8 Binding
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 129801 0 None -5 2 Human 5.8 pKi = 5.8 Binding
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 84596 0 None -1071 4 Human 5.8 pKi = 5.8 Binding
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 84596 0 None -1071 4 Human 5.8 pKi = 5.8 Binding
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 84596 0 None -1071 4 Human 5.8 pKi = 5.8 Binding
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 193752 0 None -36 2 Human 5.8 pKi = 5.8 Binding
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 193752 0 None -36 2 Human 5.8 pKi = 5.8 Binding
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 210977 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 210977 4 None - 1 Human 5.8 pKi = 5.8 Binding
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 196749 0 None -35 12 Human 6.8 pKi = 6.8 Binding
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 196749 0 None -35 12 Human 6.8 pKi = 6.8 Binding
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 210991 0 None -19 4 Human 5.8 pKi = 5.8 Binding
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 210991 0 None -19 4 Human 5.8 pKi = 5.8 Binding
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 66861 0 None -1659 7 Human 5.8 pKi = 5.8 Binding
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 66861 0 None -1659 7 Human 5.8 pKi = 5.8 Binding
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 66861 0 None -1659 7 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 390 4 3 5 3.2 O=S(=O)(c1cccc(Cl)c1)c1n[nH]c2ccc(NC3CCNCC3)cc12 10.1016/j.bmc.2010.10.033
14547415 107447 1 None -10 4 Human 5.8 pKi = 5.8 Binding
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 107447 1 None -10 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
180 7189 56 None -389 40 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
200 7189 56 None -389 40 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
2160 7189 56 None -389 40 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
CHEMBL629 7189 56 None -389 40 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
DB00321 7189 56 None -389 40 Rat 5.8 pKi = 5.8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C nan
44214329 66213 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 66213 0 None -33 2 Human 7.8 pKi = 7.8 Binding
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 17300 0 None -21 2 Human 7.8 pKi = 7.8 Binding
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 17300 0 None -21 2 Human 7.8 pKi = 7.8 Binding
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 132484 0 None - 1 Chinese hamster 7.8 pKi = 7.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 132484 0 None - 1 Chinese hamster 7.8 pKi = 7.8 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA 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 7532 59 None -16 29 Rat 7.8 pKi = 7.8 Binding
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 7532 59 None -16 29 Rat 7.8 pKi = 7.8 Binding
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 7532 59 None -16 29 Rat 7.8 pKi = 7.8 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
CHEMBL49 7532 59 None -16 29 Rat 7.8 pKi = 7.8 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
DB00490 7532 59 None -16 29 Rat 7.8 pKi = 7.8 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 10.1021/jm00027a013
2303 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
4946 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
564 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
63 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
91536 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL27 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL452861 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
DB00571 9961 68 None -57 26 Rat 7.8 pKi = 7.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
1346 6871 117 None -40 9 Rat 7.8 pKi = 7.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
280 6871 117 None -40 9 Rat 7.8 pKi = 7.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
9899402 6871 117 None -40 9 Rat 7.8 pKi = 7.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9666 6871 117 None -40 9 Rat 7.8 pKi = 7.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 10.1021/jm00125a020
44376283 63282 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
CHEMBL163516 63282 0 None -5 2 Human 6.8 pKi = 6.8 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
11465618 109175 23 None -630 19 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL3039528 109175 23 None -630 19 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
CHEMBL5191141 109175 23 None -630 19 Rat 6.8 pKi = 6.8 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 354 2 0 2 4.9 CN1CCN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CC1(C)C 10.1016/j.bmcl.2022.128879
22184640 91952 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 519 8 2 7 3.5 CCN1CCC(N(CC)c2cc(OC)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)C1 10.1016/j.bmc.2006.10.037
CHEMBL225310 91952 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 519 8 2 7 3.5 CCN1CCC(N(CC)c2cc(OC)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)C1 10.1016/j.bmc.2006.10.037
11011968 11713 0 None -173 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 2 3 2.7 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CC4)nc23)CC1 10.1021/jm030020m
CHEMBL104720 11713 0 None -173 4 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 298 3 2 3 2.7 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CC4)nc23)CC1 10.1021/jm030020m
10618751 41964 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143510 41964 0 None -4 4 Human 6.8 pKi = 6.8 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor alpha expressed in CHO-K1 cells.
ChEMBL 364 7 1 4 3.3 CCN(CC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
10496545 16099 0 None 13 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 328 9 2 2 5.1 CCCCCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL111107 16099 0 None 13 2 Human 6.8 pKi = 6.8 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 328 9 2 2 5.1 CCCCCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL4520788 220754 10 None -83 25 Human 5.8 pKi = 5.8 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR1BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000743a HTR1B
ChEMBL None None None CNCc1ccccc1-c1csc([C@H](C)Nc2nc(C)nc3cc(OC)c(OC)cc23)c1 10.6019/CHEMBL5212743
10088038 211135 0 None -30 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 7 1 1 5.2 CCCc1c[nH]c2c(F)cc3c(c12)CC(N(CCC)CCC)CC3 10.1021/jm00012a021
CHEMBL71663 211135 0 None -30 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 7 1 1 5.2 CCCc1c[nH]c2c(F)cc3c(c12)CC(N(CCC)CCC)CC3 10.1021/jm00012a021
132787 10203 45 None -1000 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
26 10203 45 None -1000 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
32 10203 45 None -1000 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
CHEMBL49247 10203 45 None -1000 6 Rat 5.8 pKi = 5.8 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 10.1021/jm00020a020
127026052 144331 0 None -107 19 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754496 144331 0 None -107 19 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 258 7 1 1 3.5 C=CCN(CC=C)CCc1c[nH]c2ccc(F)cc12 10.1016/j.bmcl.2015.12.053
107992 9331 49 None -12 10 Rat 6.8 pKi = 6.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
165 9331 49 None -12 10 Rat 6.8 pKi = 6.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
CHEMBL269521 9331 49 None -12 10 Rat 6.8 pKi = 6.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
DB12111 9331 49 None -12 10 Rat 6.8 pKi = 6.8 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00125a020
10064361 210943 0 None -223 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL70652 210943 0 None -223 4 Human 6.8 pKi = 6.8 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
19066188 18870 0 None 19 3 Human 7.8 pKi = 7.8 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1183944 18870 0 None 19 3 Human 7.8 pKi = 7.8 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL325131 18870 0 None 19 3 Human 7.8 pKi = 7.8 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 409 4 1 5 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
24882268 179336 0 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL448555 179336 0 None -11 2 Human 7.8 pKi = 7.8 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
5 6927 72 None -11 53 Human 7.8 pKi = 7.8 Binding
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 6927 72 None -11 53 Human 7.8 pKi = 7.8 Binding
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 6927 72 None -11 53 Human 7.8 pKi = 7.8 Binding
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 6927 72 None -11 53 Human 7.8 pKi = 7.8 Binding
Displacement of radiolabeled serotonin from human 5HT1B receptorDisplacement of radiolabeled serotonin from human 5HT1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm8007618
44404396 78232 0 None 5 5 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196169 78232 0 None 5 5 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccccc3F)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10643939 20883 0 None 35 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
CHEMBL119800 20883 0 None 35 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C/CN(C)C 10.1021/jm9702948
25263302 198763 0 None -1380 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT1b receptorBinding affinity to 5HT1b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
CHEMBL520129 198763 0 None -1380 5 Human 5.8 pKi = 5.8 Binding
Binding affinity to 5HT1b receptorBinding affinity to 5HT1b receptor
ChEMBL 434 4 2 6 3.4 O=C(Nc1ccc2cnn(S(=O)(=O)c3cccc4ccccc34)c2c1)C1CCCNC1 10.1016/j.bmcl.2009.03.071
14011047 65803 22 None -446 2 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 274 8 1 2 3.8 CCCN(CCC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm00399a031
CHEMBL169328 65803 22 None -446 2 Rat 5.8 pKi = 5.8 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 274 8 1 2 3.8 CCCN(CCC)CCc1c[nH]c2ccc(OC)cc12 10.1021/jm00399a031
14519865 38361 1 None -39 4 Rat 5.8 pKi = 5.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL140417 38361 1 None -39 4 Rat 5.8 pKi = 5.8 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 243 6 0 2 3.6 CCCN(C)CCOc1cccc2ccccc12 10.1021/jm00124a021
117209857 191917 1 None -43 8 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4856702 191917 1 None -43 8 Human 5.7 pKi = 5.7 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 246 2 2 3 1.6 Fc1cccc(-c2n[nH]cc2N2CCNCC2)c1 10.1021/acs.jmedchem.1c01093
2726 7706 68 None -147 72 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
621 7706 68 None -147 72 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
83 7706 68 None -147 72 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
CHEMBL71 7706 68 None -147 72 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
DB00477 7706 68 None -147 72 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C nan
44455426 161928 0 None -26 12 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL402143 161928 0 None -26 12 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
44460810 212402 0 None -48 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 436 5 1 4 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2csc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL81703 212402 0 None -48 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 436 5 1 4 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2csc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
9949568 130208 0 None -61 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 334 4 0 2 5.1 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCN1Cc1ccccc1 10.1016/j.bmcl.2004.06.085
CHEMBL361729 130208 0 None -61 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 334 4 0 2 5.1 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCN1Cc1ccccc1 10.1016/j.bmcl.2004.06.085
10068238 26491 0 None -1479 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 3.8 c1ccc2c(c1)CC(CCCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL130103 26491 0 None -1479 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 3.8 c1ccc2c(c1)CC(CCCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10432512 109166 0 None -234 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 424 9 1 3 5.7 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL303921 109166 0 None -234 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 424 9 1 3 5.7 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10517352 14400 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 286 6 2 2 3.9 CCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL108818 14400 0 None 5 2 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 286 6 2 2 3.9 CCCCCCOc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
10500422 85250 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
CHEMBL2111779 85250 0 None 15 3 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
73453 36389 24 None -26 17 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 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 36389 24 None -26 17 Rat 7.7 pKi = 7.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 561 4 3 6 2.0 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 nan
59636772 132454 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1ccccn1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647259 132454 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1ccccn1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
59636774 132483 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 7 3.3 Cc1ccnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)n1 nan
CHEMBL3647287 132483 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 7 3.3 Cc1ccnc(CCNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)n1 nan
59636731 132998 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccc(F)cn4)CC3)c2o1 nan
CHEMBL3650040 132998 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccc(F)cn4)CC3)c2o1 nan
2543 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
5358 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
54 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
CHEMBL128 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
DB00669 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(98)00090-0
44402875 77229 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 413 3 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL194610 77229 0 None 12 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 413 3 0 4 4.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1cccc(Cl)c1)CC2 10.1016/j.bmcl.2005.07.085
10161028 97547 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL239168 97547 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
10237964 194393 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL494806 194393 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 418 7 1 5 3.7 CC(=O)Nc1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
10216873 194579 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 443 7 0 4 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5=O)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL495895 194579 0 None -9 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 443 7 0 4 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5=O)c4)CC3)cccc2n1 10.1021/jm8001444
10173263 200178 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 417 7 1 4 4.8 CC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL525712 200178 0 None -39 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 417 7 1 4 4.8 CC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
9867475 24785 0 None -63 9 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL126340 24785 0 None -63 9 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 432 7 0 5 4.2 CN(C)CCc1cccc2c1cc(C(=O)c1ccccc1)n2S(=O)(=O)c1ccccc1 10.1021/jm010943m
1524 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
197 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
3822 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
88 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
CHEMBL51 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
DB12465 8962 96 None -512 51 Rat 5.7 pKi = 5.7 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1021/jm00384a001
10016864 211027 0 None -17 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 286 5 1 2 3.2 CCCN(CCC)C1CCc2ccc3c(c2C1)CC(=O)N3 10.1021/jm00012a021
CHEMBL71091 211027 0 None -17 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 286 5 1 2 3.2 CCCN(CCC)C1CCc2ccc3c(c2C1)CC(=O)N3 10.1021/jm00012a021
10267412 211131 0 None -323 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 310 6 1 2 4.0 CCCN(CC1CC1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL71640 211131 0 None -323 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 310 6 1 2 4.0 CCCN(CC1CC1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
4656 129738 7 None -39 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 355 1 2 1 2.8 Clc1cc(I)cc(Cl)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL360803 129738 7 None -39 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 355 1 2 1 2.8 Clc1cc(I)cc(Cl)c1N=C1NCCN1 10.1016/j.bmcl.2004.06.085
46905266 16946 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL1159649 16946 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
10427962 27600 0 None -114 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.3 c1ccc2c(c1)CCC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131011 27600 0 None -114 3 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.3 c1ccc2c(c1)CCC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
10287730 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
77 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
CHEMBL425190 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm049039v
11259254 131947 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 440 7 0 6 4.3 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL364495 131947 0 None -39 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 440 7 0 6 4.3 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
44588720 191124 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OC(C)CN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484386 191124 0 None -2 3 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OC(C)CN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10287730 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
77 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
CHEMBL425190 10309 40 None -251 12 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 10.1021/jm8001444
173 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
5011 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
CHEMBL18772 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm990151g
10655811 211217 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(CC2=NCCN2)c(C)c1O 10.1021/jm970513p
CHEMBL72167 211217 0 None -1 2 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(CC2=NCCN2)c(C)c1O 10.1021/jm970513p
44444557 161465 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
CHEMBL399704 161465 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity at 5HT1B receptorBinding affinity at 5HT1B receptor
ChEMBL 493 4 0 5 3.7 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(S(=O)(=O)c1cccc(Br)c1)CC2 10.1016/j.bmcl.2007.09.067
6918603 214750 1 None -999 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL97158 214750 1 None -999 4 Human 5.7 pKi = 5.7 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10127209 75433 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191980 75433 0 None 1 2 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(Cl)c(Cl)c4)CC3)cccc2n1 10.1021/jm049039v
44439165 152531 0 None -794 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391661 152531 0 None -794 8 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc5c(cc4F)OCC(=O)N5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL4576555 220796 5 None -2 19 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
10478367 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL196370 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL430500 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
10478367 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196370 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL430500 78445 0 None 19 7 Human 8.7 pKi = 8.7 Binding
Affinity towards 5-hydroxytryptamine 1B receptorAffinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 439 5 1 6 2.8 COc1ccc(NC(=O)N2CCN(c3ccccc3OC)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10664203 12255 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 10 2 2 5.4 CC(C)(C)CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL107617 12255 0 None 31 2 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 10 2 2 5.4 CC(C)(C)CCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636753 132993 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.1 CC(=O)c1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
CHEMBL3650036 132993 0 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.1 CC(=O)c1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
44351692 26228 6 None -2 3 Human 8.7 pKi = 8.7 Binding
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 242 2 1 3 2.3 COc1ccc2ccc(N3CCNCC3)cc2c1 10.1021/jm9703552
CHEMBL129661 26228 6 None -2 3 Human 8.7 pKi = 8.7 Binding
Receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cellsReceptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor in Cos-7 cells
ChEMBL 242 2 1 3 2.3 COc1ccc2ccc(N3CCNCC3)cc2c1 10.1021/jm9703552
44279889 109971 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 510 7 0 6 5.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5cccc(N6CCN(C)CC6)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL30831 109971 0 None -1 3 Human 8.7 pKi = 8.7 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 510 7 0 6 5.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5cccc(N6CCN(C)CC6)c5c4)cc23)CC1 10.1016/s0960-894x(98)00222-4
1043 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
149 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
3251 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
8223 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
CHEMBL1982133 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
CHEMBL442 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
DB00696 8363 14 None -29 29 Human 8.7 pKi = 8.7 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2011.09.046
49848635 132465 3 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 378 5 0 5 2.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647269 132465 3 None - 1 Chinese hamster 8.7 pKi = 8.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 378 5 0 5 2.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
115 10563 80 None 1 27 Rat 8.7 pKi = 8.7 Binding
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
4296 10563 80 None 1 27 Rat 8.7 pKi = 8.7 Binding
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
CHEMBL274866 10563 80 None 1 27 Rat 8.7 pKi = 8.7 Binding
Binding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00125a020
10251722 18149 0 None 20 3 Human 8.6 pKi = 8.6 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL105970 18149 0 None 20 3 Human 8.6 pKi = 8.6 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1179958 18149 0 None 20 3 Human 8.6 pKi = 8.6 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 423 4 1 5 3.1 COc1ccc(NC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
9928474 16105 0 None 6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 9 2 2 5.0 CC(C)(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111150 16105 0 None 6 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 9 2 2 5.0 CC(C)(C)CCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636733 132480 0 None - 1 Chinese hamster 8.6 pKi = 8.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647284 132480 0 None - 1 Chinese hamster 8.6 pKi = 8.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 470 8 1 6 4.1 COc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
44342785 16607 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 5 2 3 5.3 COc1ccc(NC(=S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL113994 16607 0 None -5 2 Human 8.6 pKi = 8.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 5 2 3 5.3 COc1ccc(NC(=S)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
59636730 132995 0 None - 1 Chinese hamster 8.6 pKi = 8.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.0 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N5CCC5)oc34)CC2)n1 nan
CHEMBL3650038 132995 0 None - 1 Chinese hamster 8.6 pKi = 8.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 420 6 0 6 3.0 COc1cccc(CCN2CCN(c3cccc4cc(C(=O)N5CCC5)oc34)CC2)n1 nan
5 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
5202 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
CHEMBL39 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
DB08839 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00014a021
44402883 78792 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 481 3 0 5 4.9 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL197505 78792 0 None 12 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 481 3 0 5 4.9 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402882 139787 0 None 19 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 496 3 1 4 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL370214 139787 0 None 19 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 496 3 1 4 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
44402884 142070 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 0 5 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL372731 142070 0 None 10 2 Human 8.6 pKi = 8.6 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 0 5 5.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Oc1cccc(C(F)(F)F)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
10791443 83969 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 7 1 7 5.0 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)N(CCN(C)C)CCO5)cc3)c(C)c2)no1 10.1021/jm970457s
CHEMBL20791 83969 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 497 7 1 7 5.0 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)N(CCN(C)C)CCO5)cc3)c(C)c2)no1 10.1021/jm970457s
10624768 106174 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 485 9 2 7 5.3 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1NCCN(C)C 10.1021/jm970457s
CHEMBL282693 106174 0 None 1 3 Human 8.6 pKi = 8.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 485 9 2 7 5.3 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1NCCN(C)C 10.1021/jm970457s
11328382 98758 0 None -3 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241503 98758 0 None -3 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2006.11.031
49850874 63236 0 None -7 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632210 63236 0 None -7 9 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 450 6 1 4 5.2 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
10477223 191796 0 None -12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL485491 191796 0 None -12 3 Human 8.6 pKi = 8.6 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 420 4 1 5 3.4 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2008.08.084
44404253 142057 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 477 4 1 7 3.5 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCNCC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL372651 142057 0 None -1 3 Human 8.6 pKi = 8.6 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 477 4 1 7 3.5 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCNCC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
5 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
5202 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
CHEMBL39 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
DB08839 6927 72 None -13 53 Rat 8.6 pKi = 8.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm990151g
44279550 106581 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 650 8 0 8 3.6 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(C(=O)COc5ccc6cccc(N7CCN(C)CC7)c6c5)CC4)cc23)CC1 10.1016/s0960-894x(98)00222-4
CHEMBL285402 106581 0 None -2 3 Human 8.6 pKi = 8.6 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 650 8 0 8 3.6 CN1CCN(c2cccc3ccc(OCC(=O)N4CCN(C(=O)COc5ccc6cccc(N7CCN(C)CC7)c6c5)CC4)cc23)CC1 10.1016/s0960-894x(98)00222-4
11827039 214755 1 None 6 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1nncc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL97184 214755 1 None 6 4 Human 8.6 pKi = 8.6 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1nncc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
11038248 118252 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL327662 118252 0 None 1 4 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
11038263 119571 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL330603 119571 0 None -1 4 Human 7.7 pKi = 7.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
10060289 67089 1 None -13 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 242 2 1 2 2.4 CN(C)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL1744040 67089 1 None -13 4 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 242 2 1 2 2.4 CN(C)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
59636773 132994 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 435 6 1 6 2.9 CC(=O)Nc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
CHEMBL3650037 132994 0 None - 1 Chinese hamster 7.7 pKi = 7.7 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 435 6 1 6 2.9 CC(=O)Nc1ccc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)nc1 nan
10310103 114089 0 None -51 9 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL317333 114089 0 None -51 9 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 425 5 0 5 5.3 N#CCCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
44460826 177207 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 439 5 1 5 4.4 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2nsc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL444843 177207 0 None -5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 439 5 1 5 4.4 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2nsc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44310169 211136 0 None -23 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 264 5 1 2 3.4 CCCN(CCC)C1CCc2c(ccc(F)c2N)C1 10.1021/jm00012a021
CHEMBL71676 211136 0 None -23 4 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 264 5 1 2 3.4 CCCN(CCC)C1CCc2c(ccc(F)c2N)C1 10.1021/jm00012a021
9802187 212627 0 None -51 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2007.03.101
CHEMBL83617 212627 0 None -51 4 Human 6.7 pKi = 6.7 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2007.03.101
137646281 164585 0 None -4677 17 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
CHEMBL4083252 164585 0 None -4677 17 Human 5.7 pKi = 5.7 Binding
Displacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from recombinant human 5HT1B receptor stably expressed in HEK cell membranes measured after 90 mins by microbeta scintillation counting method
ChEMBL 423 8 0 7 3.8 COc1ccccc1N1CCN(CCCSc2nnc(-c3ccccc3)n2C)CC1 10.1021/acs.jmedchem.9b00412
10385009 27268 0 None -331 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CCC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130734 27268 0 None -331 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CCC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
164 8242 19 None -89 10 Rat 5.7 pKi = 5.7 Binding
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
85875 8242 19 None -89 10 Rat 5.7 pKi = 5.7 Binding
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
CHEMBL8600 8242 19 None -89 10 Rat 5.7 pKi = 5.7 Binding
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
DB01528 8242 19 None -89 10 Rat 5.7 pKi = 5.7 Binding
Binding affinity against 5-HT1B serotonin receptor in rat striatumBinding affinity against 5-HT1B serotonin receptor in rat striatum
ChEMBL 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC 10.1021/jm00399a031
9827354 119367 0 None -5 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL330171 119367 0 None -5 4 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
173 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
5011 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
CHEMBL18772 10036 95 None -2 23 Rat 6.7 pKi = 6.7 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00014a021
10640199 15767 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 13 2 2 5.6 CCCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL109839 15767 0 None 3 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 13 2 2 5.6 CCCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44431536 94096 0 None -23 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 454 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL233210 94096 0 None -23 4 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 454 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
2735875 105259 92 None 1 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 187 1 1 3 1.0 N#Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL275943 105259 92 None 1 2 Rat 7.7 pKi = 7.7 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 187 1 1 3 1.0 N#Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
10870264 211127 1 None -389 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL71625 211127 1 None -389 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL5074880 221118 0 None -21 9 Human 6.7 pKi = 6.7 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
44461297 176045 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 2 4 3.6 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2[nH]nc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL441259 176045 0 None -8 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 420 5 2 4 3.6 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2[nH]nc3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44461425 212638 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 430 5 1 3 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccc(F)cc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL83732 212638 0 None -7 3 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 430 5 1 3 4.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2cccc3ccc(F)cc23)CC1 10.1016/j.bmcl.2004.03.003
9997154 27835 0 None -120 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 3 0 4 2.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131198 27835 0 None -120 2 Rat 6.7 pKi = 6.7 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 336 3 0 4 2.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
899057 67097 7 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@@H](C)N)c[nH]c2c1 10.1021/jm00402a026
CHEMBL1744073 67097 7 None - 1 Rat 5.7 pKi = 5.7 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@@H](C)N)c[nH]c2c1 10.1021/jm00402a026
3117 214620 103 None -3 16 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
CHEMBL964 214620 103 None -3 16 Rat 5.7 pKi = 5.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC nan
10424220 109643 0 None -151 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)C1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL305743 109643 0 None -151 4 Human 6.7 pKi = 6.7 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)C1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL4576555 220796 5 None -2 19 Human 5.7 pKi = 5.7 Binding
GPCRScan assay: inhibition of 5-HT1BGPCRScan assay: inhibition of 5-HT1B
ChEMBL None None None CN1CCN(C(=O)C(C)(C)c2ccc(C(=O)Nc3cn4cc(-c5cc(C(C)(C)C)cc(C(C)(C)C)c5)ccc4n3)cc2)CC1 10.6019/CHEMBL4507307
44582676 196558 0 None -16 17 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL516088 196558 0 None -16 17 Human 5.7 pKi = 5.7 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 403 9 0 4 4.3 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
11778645 67090 0 None -60 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 284 5 1 1 4.4 CCCN(CC(C)C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL1744041 67090 0 None -60 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 284 5 1 1 4.4 CCCN(CC(C)C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
2543 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
5358 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
54 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
CHEMBL128 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
DB00669 10479 68 None -3 32 Human 7.7 pKi = 7.7 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9604890
10710400 15958 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 314 8 2 2 4.8 NCCc1c[nH]c2ccc(OCCCCC3CCCCC3)cc12 10.1021/jm950498t
CHEMBL110318 15958 0 None 2 3 Human 7.7 pKi = 7.7 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 314 8 2 2 4.8 NCCc1c[nH]c2ccc(OCCCCC3CCCCC3)cc12 10.1021/jm950498t
10786335 18832 0 None 63 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
CHEMBL118360 18832 0 None 63 2 Human 7.7 pKi = 7.7 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 385 5 1 4 3.9 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1C#CCN(C)C 10.1021/jm9702948
10917953 214767 0 None -630 10 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL97242 214767 0 None -630 10 Human 6.7 pKi = 6.7 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 489 6 0 8 3.6 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
26987 7736 33 None -138 21 Rat 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
6063 7736 33 None -138 21 Rat 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
671 7736 33 None -138 21 Rat 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
CHEMBL1626 7736 33 None -138 21 Rat 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
DB00283 7736 33 None -138 21 Rat 6.7 pKi = 6.7 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C nan
24841480 190678 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
CHEMBL481153 190678 0 None -1096 20 Human 5.7 pKi = 5.7 Binding
Antagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assayAntagonist activity at serotonin 5HT1B receptor (unknown origin) by PDSP assay
ChEMBL 340 3 0 4 4.5 O=C(OCCN1CCCC1)N1c2ccccc2Sc2ccccc21 10.1016/j.bmcl.2013.04.082
6918542 211703 24 None -2238 10 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL76237 211703 24 None -2238 10 Human 5.7 pKi = 5.7 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
11743042 210829 0 None -117 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 423 8 1 3 4.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL69943 210829 0 None -117 4 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 423 8 1 3 4.7 CCCN(CCCCN1C(=O)CC(C)(C)CC1=O)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10400189 112432 0 None -229 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 256 4 2 2 2.8 CCCNC1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL312525 112432 0 None -229 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 256 4 2 2 2.8 CCCNC1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10468376 108863 1 None -512 4 Human 5.6 pKi = 5.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL302171 108863 1 None -512 4 Human 5.6 pKi = 5.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
10468376 108863 1 None -512 4 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL302171 108863 1 None -512 4 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)[C@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
11948707 172946 0 None -562 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT1B receptor by radioligand binding assayBinding affinity to 5HT1B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
CHEMBL426317 172946 0 None -562 13 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5HT1B receptor by radioligand binding assayBinding affinity to 5HT1B receptor by radioligand binding assay
ChEMBL 373 7 0 8 0.6 COc1cccc(N2CCN(CCCCn3ncc(=O)n(C)c3=O)CC2)c1 10.1016/j.bmcl.2006.01.052
14547414 109061 1 None -15 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL303339 109061 1 None -15 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)[C@@H]1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10245352 211012 0 None -67 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 6 2 1 4.5 c1ccc(CCCNCC2CCc3ccc4[nH]ccc4c3C2)cc1 10.1021/jm00012a022
CHEMBL70980 211012 0 None -67 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 6 2 1 4.5 c1ccc(CCCNCC2CCc3ccc4[nH]ccc4c3C2)cc1 10.1021/jm00012a022
25060119 111092 0 None -32359 7 Rat 5.6 pKi = 5.6 Binding
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 111092 0 None -32359 7 Rat 5.6 pKi = 5.6 Binding
Inhibition of rat 5-HT1B receptorInhibition of rat 5-HT1B receptor
ChEMBL 493 7 1 5 6.1 COc1ccc(CNC(=O)c2cc(-c3cc(Cl)cc(Cl)c3)cnc2-c2cccnc2)cc1OC 10.1016/j.bmcl.2013.10.045
10090960 27840 0 None -114 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 376 4 0 4 4.0 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CC1 10.1021/jm00020a020
CHEMBL131200 27840 0 None -114 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 376 4 0 4 4.0 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CC1 10.1021/jm00020a020
10775682 209971 1 None 109 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1c2c(cc3ccccc13)CCC(N)C2 10.1016/S0960-894X(01)81009-X
CHEMBL64303 209971 1 None 109 2 Rat 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1c2c(cc3ccccc13)CCC(N)C2 10.1016/S0960-894X(01)81009-X
11402988 65984 0 None -32 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL170192 65984 0 None -32 2 Human 7.6 pKi = 7.6 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 270 4 1 2 4.0 CN(C)CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
10096890 116933 0 None -26 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 5 1 3 5.4 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(S(=O)(=O)c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL323666 116933 0 None -26 2 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 5 1 3 5.4 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(S(=O)(=O)c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
2543 10479 68 None -17 32 Rat 7.6 pKi = 7.6 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358 10479 68 None -17 32 Rat 7.6 pKi = 7.6 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
54 10479 68 None -17 32 Rat 7.6 pKi = 7.6 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
CHEMBL128 10479 68 None -17 32 Rat 7.6 pKi = 7.6 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
DB00669 10479 68 None -17 32 Rat 7.6 pKi = 7.6 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
2543 10479 68 None -3 32 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
5358 10479 68 None -3 32 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
54 10479 68 None -3 32 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
CHEMBL128 10479 68 None -3 32 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
DB00669 10479 68 None -3 32 Human 7.6 pKi = 7.6 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00018a020
10447948 106947 0 None 1 3 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 307 1 0 3 3.4 CN1CCN(c2nc3ccccc3c3c2CC2CCC3C2)CC1 10.1021/jm970645i
CHEMBL287987 106947 0 None 1 3 Rat 5.6 pKi = 5.6 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 307 1 0 3 3.4 CN1CCN(c2nc3ccccc3c3c2CC2CCC3C2)CC1 10.1021/jm970645i
9927441 214173 0 None -676 9 Human 5.6 pKi = 5.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
CHEMBL93868 214173 0 None -676 9 Human 5.6 pKi = 5.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 328 5 0 4 3.0 CN(C)CCc1cn(S(=O)(=O)c2ccccc2)c2ccccc12 10.1021/jm010943m
9950390 73025 0 None -588 4 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2n[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL184597 73025 0 None -588 4 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2n[nH]c3ccc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1016/j.bmcl.2004.09.079
76319310 113099 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL2260928 113099 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
CHEMBL3139131 113099 0 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1ccc(Br)cc1Br 10.1007/s00044-009-9164-1
3251 10844 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
5684 10844 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
80 10844 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
CHEMBL31354 10844 58 None -79 12 Human 7.6 pKi = 7.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 422 7 0 5 3.8 COc1ccccc1N1CCN(CC1)CCN(C(=O)C1CCCCC1)c1ccccn1 10.1021/jm1009956
11792868 205966 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 360 4 1 6 0.7 O=C(C1=Cc2cccc(OCC3CNCCO3)c2OC1)N1CCOCC1 10.1021/jm970806i
CHEMBL58961 205966 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 360 4 1 6 0.7 O=C(C1=Cc2cccc(OCC3CNCCO3)c2OC1)N1CCOCC1 10.1021/jm970806i
151 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
20 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
5311258 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
CHEMBL101690 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm030020m
151 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
20 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
5311258 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
CHEMBL101690 9194 44 None -89 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1016/j.bmcl.2004.09.079
44395787 133561 7 None -588 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 1 4 3.7 CN1CCC(n2ncc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL365405 133561 7 None -588 3 Human 5.6 pKi = 5.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 1 4 3.7 CN1CCC(n2ncc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
10475893 170710 0 None -20 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 396 8 1 2 5.9 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL420748 170710 0 None -20 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 396 8 1 2 5.9 CCCN(CCCOc1cccc(Cl)c1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
132060770 169418 0 None -39 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
CHEMBL4169689 169418 0 None -39 10 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting methodDisplacement of [3H]-5-CT from human 5-HT1B receptor expressed in stable HEK cells after 90 mins by microbeta scintillation counting method
ChEMBL 451 7 0 6 3.5 CCOC(=O)CCN1CCN(c2ccc3c(c2)CN(C(=O)OCc2ccccc2)CC3)CC1 10.1016/j.ejmech.2018.02.024
10691904 42394 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143967 42394 0 None -6 4 Human 6.6 pKi = 6.6 Binding
Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-HT1D beta receptor expressed in CHO-K1 cells.
ChEMBL 392 9 1 4 4.1 CCCN(CCC)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
122187378 129804 0 None -8 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
CHEMBL3609143 129804 0 None -8 2 Human 5.6 pKi = 5.6 Binding
Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)Displacement of [3H]GR125743 from 5HT1B receptor (unknown origin)
ChEMBL 455 5 0 5 5.6 COc1cc2c3c(c1OCC1CC1)-c1cc4c(cc1CC3N(C)CC2c1ccccc1)OCO4 10.1016/j.bmcl.2015.07.012
76315631 112990 0 None -4 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL2260925 112990 0 None -4 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL3138773 112990 0 None -4 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
10449461 211238 0 None -354 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 332 6 1 1 5.0 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL72285 211238 0 None -354 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 332 6 1 1 5.0 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
5 6927 72 None -13 53 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
5202 6927 72 None -13 53 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
CHEMBL39 6927 72 None -13 53 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
DB08839 6927 72 None -13 53 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00384a001
133 9274 52 None -40 43 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
1723 9274 52 None -40 43 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
28693 9274 52 None -40 43 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
CHEMBL19215 9274 52 None -40 43 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
DB13520 9274 52 None -40 43 Rat 7.6 pKi = 7.6 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1021/jm00384a001
11809037 11865 0 None -5 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 309 3 1 5 1.7 CN1CCC(c2c[nH]c3ccc(OS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
CHEMBL105556 11865 0 None -5 3 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 309 3 1 5 1.7 CN1CCC(c2c[nH]c3ccc(OS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
44443101 100734 0 None -12 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 536 9 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CCc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248407 100734 0 None -12 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 536 9 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CCc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
44443094 100746 0 None -25 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 460 7 0 6 3.5 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL248458 100746 0 None -25 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 460 7 0 6 3.5 CCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44588745 191761 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 417 5 1 5 4.0 Cc1ccc2c(OC3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485427 191761 0 None -3 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 417 5 1 5 4.0 Cc1ccc2c(OC3CCN(CCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10151492 200161 0 None -100 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 446 8 2 4 5.0 CCNC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL525362 200161 0 None -100 3 Human 7.6 pKi = 7.6 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 446 8 2 4 5.0 CCNC(=O)Nc1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
10778246 172219 0 None -1 3 Rat 7.6 pKi = 7.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandThe compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3ncccc3n3cccc23)CC1 10.1021/jm990151g
CHEMBL423899 172219 0 None -1 3 Rat 7.6 pKi = 7.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandThe compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 267 1 0 5 1.6 CN1CCN(c2nc3ncccc3n3cccc23)CC1 10.1021/jm990151g
10802125 204850 1 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 272 3 1 5 1.4 N#CC1=Cc2cccc(OCC3CNCCO3)c2OC1 10.1021/jm970806i
CHEMBL57423 204850 1 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 272 3 1 5 1.4 N#CC1=Cc2cccc(OCC3CNCCO3)c2OC1 10.1021/jm970806i
CHEMBL5093342 222343 0 None -29 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095971 222343 0 None -29 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
152 7152 29 None -33 19 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
2107 7152 29 None -33 19 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
CHEMBL275854 7152 29 None -33 19 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm950498t
10451312 27443 0 None -316 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2C1 10.1021/jm00020a020
CHEMBL130870 27443 0 None -316 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2C1 10.1021/jm00020a020
10150658 75420 1 None -158 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 392 6 2 6 3.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c(N)c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191895 75420 1 None -158 2 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 392 6 2 6 3.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c(N)c4)CC3)cccc2n1 10.1021/jm049039v
10173169 75426 0 None -100 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncccc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191921 75426 0 None -100 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 412 6 0 5 4.3 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncccc45)CC3)cccc2n1 10.1021/jm049039v
11774585 75948 0 None -31 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 424 7 0 6 3.8 Cc1ccc2c(OCCN3CCN(Cc4ccc(F)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL192536 75948 0 None -31 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 424 7 0 6 3.8 Cc1ccc2c(OCCN3CCN(Cc4ccc(F)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
24865538 194358 0 None -251 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 361 6 0 4 3.7 Cc1ccc2c(OCCN3CCN(Cc4ccccc4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL494631 194358 0 None -251 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 361 6 0 4 3.7 Cc1ccc2c(OCCN3CCN(Cc4ccccc4)CC3)cccc2n1 10.1021/jm8001444
10683189 125860 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 266 1 1 4 2.2 Cc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm990151g
CHEMBL342690 125860 0 None 3 2 Rat 6.6 pKi = 6.6 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 266 1 1 4 2.2 Cc1cccc2nc(N3CCNCC3)c3cccn3c12 10.1021/jm990151g
9805456 214525 0 None -1995 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL95823 214525 0 None -1995 4 Human 5.6 pKi = 5.6 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 2 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN[C@@H](C)C4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
1220 6975 55 None -7413 44 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
31 6975 55 None -7413 44 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
7 6975 55 None -7413 44 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
CHEMBL56 6975 55 None -7413 44 Rat 5.6 pKi = 5.6 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00027a013
10402263 109976 1 None -18 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL308347 109976 1 None -18 4 Human 7.6 pKi = 7.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
44395832 129972 5 None -120 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 1 3 4.3 CN1CCC(n2ccc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL361303 129972 5 None -120 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 351 3 1 3 4.3 CN1CCC(n2ccc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
10692095 211171 0 None -120 4 Western lowland gorilla 4.6 pKi = 4.6 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71907 211171 0 None -120 4 Western lowland gorilla 4.6 pKi = 4.6 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
10326069 46070 1 None -147 9 Human 5.6 pKi = 5.6 Binding
Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
CHEMBL147077 46070 1 None -147 9 Human 5.6 pKi = 5.6 Binding
Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.Binding affinity for recombinant human 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 589 10 3 8 3.3 CNC(=O)C1=C(C)NC(C)=C(C(=O)NCCCN2CCC(C(=O)OC)(c3ccccc3)CC2)C1c1ccc([N+](=O)[O-])cc1 10.1021/jm980506g
14083209 69838 2 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@H](C)N)c12 10.1021/jm00402a026
CHEMBL1788280 69838 2 None - 1 Rat 5.6 pKi = 5.6 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@H](C)N)c12 10.1021/jm00402a026
129503 168447 10 None -22 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL413105 168447 10 None -22 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 214 1 1 1 2.6 CN(C)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10872581 11701 0 None -34 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc([N+](=O)[O-])cc4)nc23)CC1 10.1021/jm030020m
CHEMBL104692 11701 0 None -34 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc([N+](=O)[O-])cc4)nc23)CC1 10.1021/jm030020m
10445946 174642 4 None -53 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 272 2 2 3 2.3 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL431041 174642 4 None -53 4 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 272 2 2 3 2.3 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
53248365 68860 0 None -281 7 Human 6.6 pKi = 6.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
CHEMBL1774995 68860 0 None -281 7 Human 6.6 pKi = 6.6 Binding
Inhibition of 5HT1B receptorInhibition of 5HT1B receptor
ChEMBL 554 6 1 5 2.9 O=C(N(CCN1CCN(c2ccccc2O)CC1)c1ccccn1)C12C3C4C1C1C2C3C41I 10.1021/jm1009956
16117279 66910 0 None -2754 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1642886 66910 0 None -2754 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
CHEMBL1739606 66910 0 None -2754 7 Human 5.6 pKi = 5.6 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 398 5 3 5 3.7 CC(C)c1ccc(S(=O)(=O)c2n[nH]c3ccc(NC4CCNCC4)cc23)cc1 10.1016/j.bmc.2010.10.033
28338386 113002 2 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260921 113002 2 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138811 113002 2 None -2 2 Human 5.6 pKi = 5.6 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
6604864 205597 1 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
CHEMBL1202783 205597 1 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
CHEMBL58353 205597 1 None - 1 Rat 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@@H]1CNCCO1 10.1021/jm970806i
10590370 168597 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 300 11 2 1 5.4 CCCCCCCCCCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL414420 168597 0 None -1 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 300 11 2 1 5.4 CCCCCCCCCCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
9837108 211437 3 None -8 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 3 1 2 2.4 CC(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
CHEMBL73670 211437 3 None -8 2 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 3 1 2 2.4 CC(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
11726413 108883 0 None -14 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 366 6 1 2 4.9 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL302263 108883 0 None -14 4 Human 6.6 pKi = 6.6 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 366 6 1 2 4.9 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(F)(F)F)c3c2C1 10.1021/jm00012a021
9848876 114222 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
CHEMBL318249 114222 0 None 1 4 Human 7.6 pKi = 7.6 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 501 7 1 6 4.3 CCn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
44403102 78507 0 None 12 6 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL196598 78507 0 None 12 6 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 477 4 1 5 3.8 COc1ccc(NC(=O)N2CCN(c3ccc(C(F)(F)F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
70529 214249 110 None 1 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9429 214249 110 None 1 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL5090884 222356 0 None -4 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096072 222356 0 None -4 7 Human 6.6 pKi = 6.6 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
59636748 132982 0 None - 1 Chinese hamster 6.6 pKi = 6.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 7 1 7 3.4 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccnn1C nan
CHEMBL3650025 132982 0 None - 1 Chinese hamster 6.6 pKi = 6.6 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 458 7 1 7 3.4 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccnn1C nan
10063561 174580 1 None - 1 Rat 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 303 1 1 4 3.5 c1ccc2c(c1)nc(N1CCNCC1)c1oc3ccccc3c12 10.1021/jm00014a021
CHEMBL430566 174580 1 None - 1 Rat 6.6 pKi = 6.6 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand.
ChEMBL 303 1 1 4 3.5 c1ccc2c(c1)nc(N1CCNCC1)c1oc3ccccc3c12 10.1021/jm00014a021
9802187 212627 0 None -51 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL83617 212627 0 None -51 4 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
44431531 94800 0 None -60 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CCC1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL234447 94800 0 None -60 3 Human 6.6 pKi = 6.6 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CCC1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
9802187 212627 0 None -51 4 Human 6.6 pKi = 6.6 Binding
Inhibition constant against 5-HT 1B receptorInhibition constant against 5-HT 1B receptor
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm058225d
CHEMBL83617 212627 0 None -51 4 Human 6.6 pKi = 6.6 Binding
Inhibition constant against 5-HT 1B receptorInhibition constant against 5-HT 1B receptor
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CC=C(c2c[nH]c3cc(F)ccc23)CC1 10.1021/jm058225d
10775128 195510 3 None -2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL50492 195510 3 None -2 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1016/s0960-894x(00)00322-x
60820 11080 14 None -144543 12 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT1BBinding affinity to 5HT1B
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
CHEMBL10085 11080 14 None -144543 12 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT1BBinding affinity to 5HT1B
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1016/j.bmc.2008.02.091
60820 11080 14 None -144543 12 Rat 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptorBinding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
CHEMBL10085 11080 14 None -144543 12 Rat 5.5 pKi = 5.5 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptorBinding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 10.1021/jm00034a003
10891048 11583 0 None -13 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 273 2 2 4 1.7 CC(=O)Nc1ncc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL104158 11583 0 None -13 4 Human 5.5 pKi = 5.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 273 2 2 4 1.7 CC(=O)Nc1ncc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
23533329 91888 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 493 9 2 7 3.0 COc1cc(N(C)CCCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL224738 91888 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 493 9 2 7 3.0 COc1cc(N(C)CCCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
115 10563 80 None 1 27 Rat 6.5 pKi = 6.5 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
4296 10563 80 None 1 27 Rat 6.5 pKi = 6.5 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
CHEMBL274866 10563 80 None 1 27 Rat 6.5 pKi = 6.5 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00145a017
10342552 16708 0 None -9 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 4 2 2 5.4 Cc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL114571 16708 0 None -9 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 4 2 2 5.4 Cc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
10613373 118082 1 None -1 3 Human 8.5 pKi = 8.5 Binding
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 118082 1 None -1 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 10 2 2 4.4 CCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
1043 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
3251 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL1982133 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
1043 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
149 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
3251 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
8223 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL1982133 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
CHEMBL442 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
DB00696 8363 14 None -29 29 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1016/j.bmcl.2013.12.024
44402877 77906 0 None 31 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 520 4 0 5 6.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195497 77906 0 None 31 3 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 520 4 0 5 6.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
44402880 78008 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(F)c1C(F)(F)F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195651 78008 0 None 63 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 479 4 0 4 4.5 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Cc1cccc(F)c1C(F)(F)F)CC2 10.1016/j.bmcl.2005.07.085
11591924 78533 3 None 79 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 537 5 1 7 5.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196666 78533 3 None 79 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 537 5 1 7 5.4 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
44402886 78615 0 None 125 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 5 1 5 5.3 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(C(C)=O)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL196951 78615 0 None 125 2 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 5 1 5 5.3 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(C(C)=O)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
11307899 85643 0 None -50 7 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
CHEMBL2112882 85643 0 None -50 7 Human 8.5 pKi = 8.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 597 6 4 6 2.5 CC(C)C[C@H]1C(=O)N[C@@H](Cc2ccccc2)[C@]2(O)O[C@@](C)(NC(=O)[C@@H]3C=C4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)C(=O)N12 10.1021/jm0341204
10370874 89370 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 484 9 1 6 5.8 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1CCCN(C)C 10.1021/jm970457s
CHEMBL21790 89370 0 None 1 3 Human 8.5 pKi = 8.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 484 9 1 6 5.8 COc1ccc(NC(=O)c2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1CCCN(C)C 10.1021/jm970457s
49850671 63165 0 None -6 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631537 63165 0 None -6 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
11292933 63168 45 None -15 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631540 63168 45 None -15 9 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 415 5 1 4 3.4 Cc1ccc2c(N3CCN(CCc4cccc(N5CCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
11419978 63237 0 None -12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632211 63237 0 None -12 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccccc5F)c4)CC3)cccc2n1 10.1021/jm100714c
49850877 63238 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632212 63238 0 None -10 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
49850568 63244 0 None -7 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5csc(C)n5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632218 63244 0 None -7 3 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 471 6 1 6 4.9 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5csc(C)n5)c4)CC3)cccc2n1 10.1021/jm100714c
11397149 63249 0 None -10 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632223 63249 0 None -10 7 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 465 6 2 4 5.6 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5ccccc5)c4)CC3)cccc2n1 10.1021/jm100714c
107780 8625 54 None -4 18 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
14 8625 54 None -4 18 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
CHEMBL15928 8625 54 None -4 18 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm00041a001
44342993 17782 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 4 2 2 6.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL117397 17782 0 None -4 2 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 4 2 2 6.7 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
10970604 11835 0 None 1 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 367 3 3 3 4.2 CN1CCC(c2c[nH]c3ccc(NC(=O)Nc4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL105369 11835 0 None 1 3 Human 8.5 pKi = 8.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 367 3 3 3 4.2 CN1CCC(c2c[nH]c3ccc(NC(=O)Nc4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
11655728 23416 8 None -46 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometryDisplacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometry
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
CHEMBL1241913 23416 8 None -46 6 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometryDisplacement of [3H]-GR125743 from 5HT1B receptor in rat brain cortex after 45 mins by liquid scintillation spectrometry
ChEMBL 468 5 1 7 3.1 Cc1ccc2c(N3CCN(CCc4cccc5c4OCc4c(C(N)=O)ncn4-5)CC3)cccc2n1 10.1021/jm100482n
1884 9512 58 None -3 5 Human 8.5 pKi = 8.5 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
4440 9512 58 None -3 5 Human 8.5 pKi = 8.5 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
45 9512 58 None -3 5 Human 8.5 pKi = 8.5 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
CHEMBL1278 9512 58 None -3 5 Human 8.5 pKi = 8.5 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
DB00952 9512 58 None -3 5 Human 8.5 pKi = 8.5 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10.1021/jm9805945
59636740 132471 0 None - 1 Chinese hamster 8.5 pKi = 8.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 9 1 7 3.7 CS(=O)(=O)Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
CHEMBL3647275 132471 0 None - 1 Chinese hamster 8.5 pKi = 8.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 532 9 1 7 3.7 CS(=O)(=O)Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cc1 nan
5 6927 72 None -13 53 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
5202 6927 72 None -13 53 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
CHEMBL39 6927 72 None -13 53 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
DB08839 6927 72 None -13 53 Rat 8.5 pKi = 8.5 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00402a026
107 6929 121 None -16 31 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
1833 6929 121 None -16 31 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
CHEMBL8165 6929 121 None -16 31 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm950498t
23533322 91845 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 477 5 2 7 2.4 COc1cc(N2CCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL224399 91845 0 None - 1 Human 8.5 pKi = 8.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 477 5 2 7 2.4 COc1cc(N2CCN(C)CC2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
59636761 132987 0 None - 1 Chinese hamster 8.5 pKi = 8.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 2 6 3.8 O=C(NCc1cccc(O)c1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650030 132987 0 None - 1 Chinese hamster 8.5 pKi = 8.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 2 6 3.8 O=C(NCc1cccc(O)c1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44342508 16595 0 None -8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL113893 16595 0 None -8 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 4 2 2 6.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4cccc5ccccc45)CC3)cc12 10.1016/s0960-894x(03)00779-0
44342518 16746 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 4 2 2 5.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL114780 16746 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 4 2 2 5.8 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccc(Cl)cc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
3608822 105286 21 None 3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 2 1 2 2.2 CC(C)c1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL276156 105286 21 None 3 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 204 2 1 2 2.2 CC(C)c1ccccc1N1CCNCC1 10.1021/jm00125a020
75 10287 7 None -3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
9870500 10287 7 None -3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
CHEMBL191971 10287 7 None -3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.07.085
44402870 77890 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 434 3 1 4 4.3 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195432 77890 0 None 3 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 434 3 1 4 4.3 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
44402881 172593 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 3 1 4 5.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL424837 172593 0 None 39 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 3 1 4 5.0 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(C(F)(F)F)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402868 175124 0 None 31 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 534 5 0 5 6.3 CCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
CHEMBL434355 175124 0 None 31 3 Human 8.4 pKi = 8.4 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 534 5 0 5 6.3 CCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
49850670 63164 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631536 63164 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 483 6 2 4 5.7 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)Nc5cccc(F)c5)c4)CC3)cccc2n1 10.1021/jm100714c
49850982 63240 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccccc1C(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
CHEMBL1632214 63240 0 None -6 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccccc1C(=O)Nc1cccc(CCN2CCN(c3cccc4nc(C)ccc34)CC2)c1 10.1021/jm100714c
49850566 63242 0 None -7 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)cc1 10.1021/jm100714c
CHEMBL1632216 63242 0 None -7 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 480 7 1 5 5.2 COc1ccc(C(=O)Nc2cccc(CCN3CCN(c4cccc5nc(C)ccc45)CC3)c2)cc1 10.1021/jm100714c
49850668 63248 0 None -15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 445 5 2 4 4.8 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)NC(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632222 63248 0 None -15 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 445 5 2 4 4.8 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)NC(C)(C)C)c4)CC3)cccc2n1 10.1021/jm100714c
22326688 100372 0 None -4 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 459 7 0 5 4.6 CCN1C(=O)COc2ccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL246598 100372 0 None -4 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 459 7 0 5 4.6 CCN1C(=O)COc2ccc(CC3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
10174078 183673 0 None -5 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)N[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL461670 183673 0 None -5 3 Human 8.4 pKi = 8.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@H](C)N[C@H](C)C5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44404260 79127 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 519 5 0 7 4.6 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C(C)C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL198488 79127 0 None 1 3 Human 8.4 pKi = 8.4 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 519 5 0 7 4.6 CCc1c(C(=O)N2CCc3cc4ccnc(N5CCN(C(C)C)CC5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
115 10563 80 None 1 27 Rat 7.5 pKi = 7.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
4296 10563 80 None 1 27 Rat 7.5 pKi = 7.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
CHEMBL274866 10563 80 None 1 27 Rat 7.5 pKi = 7.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 10.1021/jm00384a001
10299410 91832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 5 1 7 3.2 COc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(F)cc12 10.1016/j.bmc.2006.10.037
CHEMBL224267 91832 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 5 1 7 3.2 COc1cc(C(=O)Nc2ccc(N3CCOCC3)cc2)nc2c(N3CCN(C)CC3)cc(F)cc12 10.1016/j.bmc.2006.10.037
77418 104172 64 None 3 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1cccc(N2CCNCC2)c1 10.1021/jm00125a020
CHEMBL269784 104172 64 None 3 2 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 180 1 1 2 1.2 Fc1cccc(N2CCNCC2)c1 10.1021/jm00125a020
10620719 211129 0 None -794 5 Western lowland gorilla 5.5 pKi = 5.5 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71635 211129 0 None -794 5 Western lowland gorilla 5.5 pKi = 5.5 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CC[C@@H]3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9995233 171890 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 304 4 1 2 4.7 CN(C)CCc1c[nH]c2ccc(-c3ccc(Cl)s3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL422737 171890 0 None -39 2 Human 6.5 pKi = 6.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 304 4 1 2 4.7 CN(C)CCc1c[nH]c2ccc(-c3ccc(Cl)s3)cc12 10.1016/s0960-894x(00)00133-5
10379784 211161 1 None -251 4 Human 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL71804 211161 1 None -251 4 Human 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
11123573 214803 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 473 6 2 5 3.8 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4c[nH]nn4)cc23)CC1 10.1021/jm020938y
CHEMBL97422 214803 0 None 1 4 Human 7.5 pKi = 7.5 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 473 6 2 5 3.8 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4c[nH]nn4)cc23)CC1 10.1021/jm020938y
44438461 97748 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 452 6 0 6 5.0 CC(C)N1CCN(C2CCc3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc32)CC1 10.1016/j.bmcl.2006.12.109
CHEMBL239596 97748 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 452 6 0 6 5.0 CC(C)N1CCN(C2CCc3ccc(OCc4noc(-c5ccc(Cl)cc5)n4)cc32)CC1 10.1016/j.bmcl.2006.12.109
59636742 132479 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1ccccn1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647283 132479 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1ccccn1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
44402869 140921 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 548 6 0 5 6.7 CCCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
CHEMBL371655 140921 0 None 2 3 Human 7.5 pKi = 7.5 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 548 6 0 5 6.7 CCCN1[C@@H](C)CN(c2cc3c(cc2OC)CCN3C(=O)c2ccc(-c3cccc(C)n3)c3ccccc23)C[C@H]1C 10.1016/j.bmcl.2005.07.085
10838923 59409 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm970457s
CHEMBL15933 59409 0 None 31 3 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 494 4 1 6 5.6 Cc1nc(-c2ccc(-c3ccc(C(=O)Nc4ccc5c(c4)C4(CCN(C)CC4)CO5)cc3)c(C)c2)no1 10.1021/jm970457s
22326704 151715 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)c(F)ccc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL391033 151715 0 None -12 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)c(F)ccc2n1 10.1016/j.bmcl.2006.11.031
49850770 63171 0 None -125 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631543 63171 0 None -125 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 430 5 0 5 4.3 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCOC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
44443095 100373 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 474 8 0 6 3.9 CCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL246599 100373 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 474 8 0 6 3.9 CCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44443096 100702 0 None -25 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 9 0 6 4.3 CCCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
CHEMBL248229 100702 0 None -25 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 9 0 6 4.3 CCCCN1C(=O)COc2ccc(CN3CCN(CCOc4cccc5nc(C)ccc45)CC3)cc21 10.1016/j.bmcl.2007.06.078
44443097 100703 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 8 0 6 4.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CC(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248230 100703 0 None -15 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 488 8 0 6 4.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(CC(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
44581260 182371 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@@H](C)NC[C@@H]5C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL457982 182371 0 None -31 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 1 5 5.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5C[C@@H](C)NC[C@@H]5C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10452875 199944 0 None -125 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4cccc5cccnc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
CHEMBL523095 199944 0 None -125 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 388 4 1 5 2.9 O=C1COc2ccc(CCN3CCN(c4cccc5cccnc45)CC3)cc2N1 10.1016/j.bmcl.2008.08.084
173 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
5011 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
CHEMBL18772 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm970645i
173 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
5011 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
CHEMBL18772 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatum.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm981112s
44461247 111533 0 None -43 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 422 5 2 4 3.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CCN(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL310744 111533 0 None -43 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 422 5 2 4 3.2 NC(=O)c1ccc2c(c1)CCOC2CCN1CCN(c2c[nH]c3cc(F)ccc23)CC1 10.1016/j.bmcl.2004.03.003
11824522 11662 0 None -42 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(C#N)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL104484 11662 0 None -42 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccc(C#N)cc4)nc23)CC1 10.1021/jm030020m
6918601 25295 0 None -407 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
CHEMBL127411 25295 0 None -407 4 Human 5.5 pKi = 5.5 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 370 3 1 5 2.7 Cc1ccc(S(=O)(=O)n2cc3c4c(cccc42)[C@H](O)[C@@H](N(C)C)C3)cc1 10.1021/jm010943m
22067856 36313 52 None 1 3 Rat 5.5 pKi = 5.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm00124a021
CHEMBL138509 36313 52 None 1 3 Rat 5.5 pKi = 5.5 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 165 5 1 2 1.7 CNCCCOc1ccccc1 10.1021/jm00124a021
11777940 108208 0 None -123 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 3 1 1 4.1 CC(C)(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL297471 108208 0 None -123 2 Human 6.5 pKi = 6.5 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 270 3 1 1 4.1 CC(C)(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
44461306 212710 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 431 6 2 4 4.1 COc1ccc2[nH]cc(C3=CCN(CCC4OCCc5cc(C(N)=O)ccc54)CC3)c2c1 10.1016/j.bmcl.2004.03.003
CHEMBL84171 212710 0 None -12 3 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 431 6 2 4 4.1 COc1ccc2[nH]cc(C3=CCN(CCC4OCCc5cc(C(N)=O)ccc54)CC3)c2c1 10.1016/j.bmcl.2004.03.003
44364048 45913 0 None -158 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligandBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
CHEMBL146942 45913 0 None -158 6 Human 6.5 pKi = 6.5 Binding
Binding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligandBinding affinity against human 5-hydroxytryptamine 1B receptor cloned receptors in CHO cells using [3H]5-CT as radioligand
ChEMBL 262 6 3 3 2.3 NCCCC1(CCCN)CCc2cccc(O)c2C1 10.1021/jm0341204
10022680 26294 0 None -251 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 380 5 0 5 3.3 COc1ccc2c(c1)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL129947 26294 0 None -251 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 380 5 0 5 3.3 COc1ccc2c(c1)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10066717 27605 0 None -177 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 354 3 0 4 3.1 Fc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131018 27605 0 None -177 2 Rat 6.5 pKi = 6.5 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 354 3 0 4 3.1 Fc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9889681 214842 0 None -630 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
CHEMBL97637 214842 0 None -630 5 Human 6.5 pKi = 6.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 444 5 2 5 4.1 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc(-c2ccccc2)cc1 10.1016/s0960-894x(01)00558-3
75306277 116031 0 None -158 23 Human 6.5 pKi = 6.5 Binding
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
CHEMBL3217984 116031 0 None -158 23 Human 6.5 pKi = 6.5 Binding
Binding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assayBinding affinity to serotonin 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 308 0 0 3 4.2 CN1CCC2C(C1)c1cccc3c1N2c1ccccc1CS3 10.1039/C2MD00311B
11168182 10307 25 None -50 13 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
264 10307 25 None -50 13 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
CHEMBL1181770 10307 25 None -50 13 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 511 14 1 3 6.5 CN(CCN(C(=O)CCC1CCCC1)Cc1ccc(cc1)c1ccc(cc1)CNCCc1ccccc1)C 10.1016/j.bmcl.2005.06.024
11476072 76176 0 None -15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 436 8 0 7 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1[N+](=O)[O-] 10.1021/jm049039v
CHEMBL193268 76176 0 None -15 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 436 8 0 7 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1[N+](=O)[O-] 10.1021/jm049039v
11235335 130803 0 None -125 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 413 6 0 6 3.7 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncncc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL362992 130803 0 None -125 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 413 6 0 6 3.7 Cc1ccc2c(OCCN3CCN(Cc4cccc5ncncc45)CC3)cccc2n1 10.1021/jm049039v
9804612 97310 0 None -79 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238730 97310 0 None -79 5 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
44588722 198020 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 433 8 1 6 3.7 Cc1ccc2c(OCCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL519010 198020 0 None -3 3 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 433 8 1 6 3.7 Cc1ccc2c(OCCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
9870053 215063 0 None -2511 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL98965 215063 0 None -2511 4 Human 5.5 pKi = 5.5 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 5 2 6 4.9 CCc1c(S(=O)(=O)Nc2ccc3nccc(N4CCNCC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
10198700 127574 3 None -18 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 2 2 3.4 NCCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL355517 127574 3 None -18 2 Human 7.5 pKi = 7.5 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 2 2 3.4 NCCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
44376383 62313 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 6 2 3 5.1 Cc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162049 62313 0 None -4 2 Human 7.5 pKi = 7.5 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 6 2 3 5.1 Cc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
9802530 42160 1 None -2 4 Human 7.5 pKi = 7.5 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
CHEMBL143767 42160 1 None -2 4 Human 7.5 pKi = 7.5 Binding
Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.Compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells.
ChEMBL 336 5 1 4 2.5 CN(C)CCc1c[nH]c2ccc(OS(=O)(=O)C(F)(F)F)cc12 10.1021/jm9604890
24881686 195168 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL501645 195168 0 None -8 2 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
11728004 11225 0 None -1 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 356 8 2 3 4.7 CCCCCCCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL101686 11225 0 None -1 3 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 356 8 2 3 4.7 CCCCCCCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
173 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
5011 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
CHEMBL18772 10036 95 None -2 23 Rat 6.5 pKi = 6.5 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 10.1021/jm00384a001
44269070 37996 0 None -162 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 440 6 0 5 3.3 COc1cccc2c1C1CCN(CCCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
CHEMBL14010 37996 0 None -162 2 Rat 6.5 pKi = 6.5 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 440 6 0 5 3.3 COc1cccc2c1C1CCN(CCCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
4806 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
71768094 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
7351 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
9966051 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
CHEMBL2104993 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
DB09068 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
Binding affinity at human 5HT1B receptorBinding affinity at human 5HT1B receptor
ChEMBL 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 10.1021/jm101459g
11568826 139576 0 None -28 8 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
CHEMBL370110 139576 0 None -28 8 Rat 7.5 pKi = 7.5 Binding
Binding affinity for rat 5HT1B receptorBinding affinity for rat 5HT1B receptor
ChEMBL 460 4 0 8 2.8 CN1CCc2c(sc3ncn(CCN4CCN(c5cncc6ccccc56)CC4)c(=O)c23)C1 10.1016/j.bmcl.2005.04.077
2760216 103836 81 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1cccc(N2CCNCC2)c1 10.1021/jm00125a020
CHEMBL267153 103836 81 None - 1 Rat 7.5 pKi = 7.5 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 207 2 1 4 1.0 O=[N+]([O-])c1cccc(N2CCNCC2)c1 10.1021/jm00125a020
11759467 11941 0 None -39 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccncc4)nc23)CC1 10.1021/jm030020m
CHEMBL105958 11941 0 None -39 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 335 3 2 4 3.0 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccncc4)nc23)CC1 10.1021/jm030020m
10331436 7112 10 None -1659 6 Human 5.5 pKi = 5.5 Binding
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
160 7112 10 None -1659 6 Human 5.5 pKi = 5.5 Binding
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
CHEMBL133455 7112 10 None -1659 6 Human 5.5 pKi = 5.5 Binding
Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligandInhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand
ChEMBL 230 2 2 2 2.4 C[C@@H](Cc1c[nH]c2c1c1CCCOc1cc2)N 10.1021/jm030205t
44582705 193775 0 None -21 13 Human 5.5 pKi = 5.5 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL490632 193775 0 None -21 13 Human 5.5 pKi = 5.5 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 399 9 0 4 4.5 COc1c(OCCF)cccc1C(=O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
59636771 132985 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1cccnc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650028 132985 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 441 7 1 6 3.5 O=C(NCc1cccnc1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
9910451 170909 0 None -338 7 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL420997 170909 0 None -338 7 Human 6.5 pKi = 6.5 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 428 5 0 6 4.7 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCC#N)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
145988313 174014 0 None -758 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292326 174014 0 None -758 5 Human 5.5 pKi = 5.5 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 451 6 2 2 5.0 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
9881478 13423 27 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 1 2 2 2.0 COc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
CHEMBL108337 13423 27 None 3 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 1 2 2 2.0 COc1ccc2[nH]c3c(c2c1)CC(N)CC3 10.1021/jm950498t
3016908 211223 24 None -47 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 2 1 2 2.2 Cc1cc(C)c(CC2=NCCN2)c(C)c1 10.1021/jm970513p
CHEMBL72178 211223 24 None -47 2 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 202 2 1 2 2.2 Cc1cc(C)c(CC2=NCCN2)c(C)c1 10.1021/jm970513p
13096730 210145 5 None -54 4 Human 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL65196 210145 5 None -54 4 Human 6.5 pKi = 6.5 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a021
13096730 210145 5 None -54 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL65196 210145 5 None -54 4 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 270 5 1 1 4.1 CCCN(CCC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
10567450 16127 1 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 12 2 2 5.2 CCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL111284 16127 1 None 1 3 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 12 2 2 5.2 CCCCCCCCCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44422352 144927 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 6 2 7 2.8 COc1cc(N2CC[C@@H](N(C)C)C2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL376813 144927 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 491 6 2 7 2.8 COc1cc(N2CC[C@@H](N(C)C)C2)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
59636769 132481 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 467 7 1 6 4.0 O=C(NC1(c2ccccn2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647285 132481 0 None - 1 Chinese hamster 7.5 pKi = 7.5 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 467 7 1 6 4.0 O=C(NC1(c2ccccn2)CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
145 6928 49 None -47 30 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
1832 6928 49 None -47 30 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
CHEMBL7257 6928 49 None -47 30 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
DB14010 6928 49 None -47 30 Rat 6.5 pKi = 6.5 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00399a031
11831220 199337 8 None -8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 10.1021/jm7011722
CHEMBL521235 199337 8 None -8 2 Human 6.5 pKi = 6.5 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 10.1021/jm7011722
142601343 192382 0 None -123 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
CHEMBL4863868 192382 0 None -123 7 Human 5.5 pKi = 5.5 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 256 2 2 3 2.2 Cc1ccc(-c2n[nH]cc2N2CCCNCC2)cc1 10.1021/acs.jmedchem.1c01093
9848303 118357 0 None -12 10 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
CHEMBL328187 118357 0 None -12 10 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)nn1 10.1021/jm020938y
2543 10479 68 None -3 32 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
5358 10479 68 None -3 32 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
54 10479 68 None -3 32 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
CHEMBL128 10479 68 None -3 32 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
DB00669 10479 68 None -3 32 Human 7.4 pKi = 7.4 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00133-5
44376282 126886 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL351036 126886 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
1150 10650 121 None -7 25 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
125 10650 121 None -7 25 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
CHEMBL6640 10650 121 None -7 25 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
DB08653 10650 121 None -7 25 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 10.1021/jm950498t
9859280 113111 1 None 56 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL2260920 113111 1 None 56 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
CHEMBL3139165 113111 1 None 56 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cccc(Cl)c1Cl 10.1007/s00044-009-9164-1
11092112 214407 0 None -645 9 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL95175 214407 0 None -645 9 Human 6.4 pKi = 6.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 0 6 4.9 O=C1OCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10850769 208611 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 286 3 0 5 1.7 CN1CCOC(COc2cccc3c2OCC(C#N)=C3)C1 10.1021/jm970806i
CHEMBL60705 208611 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 286 3 0 5 1.7 CN1CCOC(COc2cccc3c2OCC(C#N)=C3)C1 10.1021/jm970806i
44554395 25495 0 None -2290 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
CHEMBL1277565 25495 0 None -2290 7 Human 5.4 pKi = 5.4 Binding
Displacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cellsDisplacement of [3H]LSD from human cloned 5HT1B receptor expressed in human HeLa cells
ChEMBL 406 3 1 6 3.0 Cn1nc(S(=O)(=O)c2cccc3ccccc23)c2cc(N3CCNCC3)ccc21 10.1021/jm1007825
107992 9331 49 None -12 10 Rat 5.4 pKi = 5.4 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
165 9331 49 None -12 10 Rat 5.4 pKi = 5.4 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
CHEMBL269521 9331 49 None -12 10 Rat 5.4 pKi = 5.4 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
DB12111 9331 49 None -12 10 Rat 5.4 pKi = 5.4 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
178081 109426 8 None -707 5 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL304426 109426 8 None -707 5 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
16614092 113018 5 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260922 113018 5 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138881 113018 5 None 1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 219 4 1 2 2.6 CNCCOc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
9837525 109932 1 None -33 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 3 1 2 3.0 Cc1cc(C(C)C)cc(C)c1CC1=NCCN1 10.1021/jm970513p
CHEMBL308042 109932 1 None -33 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 3 1 2 3.0 Cc1cc(C(C)C)cc(C)c1CC1=NCCN1 10.1021/jm970513p
59636775 132459 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 444 7 1 7 2.9 Cn1cnc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647263 132459 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 444 7 1 7 2.9 Cn1cnc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
4595 183494 106 None -7 14 Rat 5.4 pKi = 5.4 Binding
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
CHEMBL46 183494 106 None -7 14 Rat 5.4 pKi = 5.4 Binding
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
ChEMBL 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O 10.1021/jm00075a026
11725335 109047 0 None -33 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 348 6 1 3 3.6 CCCN(CCC)C1CCc2ccc3[nH]cc(S(C)(=O)=O)c3c2C1 10.1021/jm00012a021
CHEMBL303269 109047 0 None -33 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 348 6 1 3 3.6 CCCN(CCC)C1CCc2ccc3[nH]cc(S(C)(=O)=O)c3c2C1 10.1021/jm00012a021
44311908 179480 3 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 176 2 2 3 0.9 Oc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
CHEMBL450281 179480 3 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 176 2 2 3 0.9 Oc1cccc(CC2=NCCN2)c1 10.1021/jm970513p
122483281 144886 0 None -741 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3763779 144886 0 None -741 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765873 144886 0 None -741 8 Human 5.4 pKi = 5.4 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 441 7 0 5 5.4 COc1ccccc1N1CCN(CCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
9994674 210935 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
CHEMBL70589 210935 0 None -44 4 Human 7.4 pKi = 7.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 295 5 1 2 4.0 CCCN(CCC)C1CCc2ccc3[nH]cc(C#N)c3c2C1 10.1021/jm00012a021
44376723 126636 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 6 2 3 5.3 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
CHEMBL348756 126636 0 None -3 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 436 6 2 3 5.3 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C1CCCCC1 10.1016/j.bmcl.2003.11.023
24882266 195066 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL500230 195066 0 None -2 2 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
59636732 132984 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 1 7 3.2 Cc1ncc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3650027 132984 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 456 7 1 7 3.2 Cc1ncc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
44403098 77047 0 None 4 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccc(F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL194206 77047 0 None 4 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 427 4 1 5 2.9 COc1ccc(NC(=O)N2CCN(c3ccc(F)cc3)CC2)cc1N1CCN(C)CC1 10.1016/j.bmcl.2005.07.024
10946905 170461 0 None -43 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 2 3 3.1 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCC4)nc23)CC1 10.1021/jm030020m
CHEMBL420475 170461 0 None -43 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 312 3 2 3 3.1 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCC4)nc23)CC1 10.1021/jm030020m
10023301 25699 0 None -120 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 390 4 0 4 4.4 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CCC1 10.1021/jm00020a020
CHEMBL128546 25699 0 None -120 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 390 4 0 4 4.4 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)c2ccccc2CCC1 10.1021/jm00020a020
14083212 69839 6 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@@H](C)N)c2c1 10.1021/jm00402a026
CHEMBL1788281 69839 6 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@@H](C)N)c2c1 10.1021/jm00402a026
10445578 126997 1 None 1 3 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 265 1 0 3 2.4 CN1CCN(c2ccc3c(n2)-c2ccccc2C3)CC1 10.1021/jm970645i
CHEMBL352107 126997 1 None 1 3 Rat 5.4 pKi = 5.4 Binding
Ability to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatumAbility to displace [3H]5-HT bound to 5-hydroxytryptamine 1B receptor in rat striatum
ChEMBL 265 1 0 3 2.4 CN1CCN(c2ccc3c(n2)-c2ccccc2C3)CC1 10.1021/jm970645i
10541847 109078 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 294 5 1 3 3.4 Cc1ccc(CC2=NCCN2)c(C)c1OCc1ccccc1 10.1021/jm970513p
CHEMBL303441 109078 0 None -3 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 294 5 1 3 3.4 Cc1ccc(CC2=NCCN2)c(C)c1OCc1ccccc1 10.1021/jm970513p
49799868 17311 0 None -54 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL1169435 17311 0 None -54 3 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 419 5 2 3 4.2 NC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CC=C(c2c[nH]c3c(F)cccc23)CC1 10.1016/j.bmcl.2004.03.003
44342507 116966 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 4 2 2 6.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL323705 116966 0 None -6 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 488 4 2 2 6.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/C45C[C@H]6C[C@@H](C4)C[C@@H](C5)C6)CC3)cc12 10.1016/s0960-894x(03)00779-0
49850769 63169 0 None -125 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 429 5 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631541 63169 0 None -125 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 429 5 1 4 3.8 Cc1ccc2c(N3CCN(CCc4cccc(N5CCCNC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
49850771 63172 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 428 5 0 5 3.6 Cc1ccc2c(N3CCN(CCc4cccc(N5C(=O)CCC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631544 63172 0 None -25 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 428 5 0 5 3.6 Cc1ccc2c(N3CCN(CCc4cccc(N5C(=O)CCC5=O)c4)CC3)cccc2n1 10.1021/jm100714c
10183895 100744 0 None -22 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248456 100744 0 None -22 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 473 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C(C)C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10127149 181693 0 None -6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 426 7 0 4 6.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccoc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456460 181693 0 None -6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 426 7 0 4 6.1 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccoc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10173443 181782 0 None -15 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 429 7 0 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456684 181782 0 None -15 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 429 7 0 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44593711 191102 0 None 1 3 Human 7.4 pKi = 7.4 Binding
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 191102 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 5 4.6 Cc1ccc2c(OCC(C)N3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10128059 194473 0 None -6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 483 9 1 6 4.3 COc1ccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1NS(C)(=O)=O 10.1021/jm8001444
CHEMBL495217 194473 0 None -6 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 483 9 1 6 4.3 COc1ccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1NS(C)(=O)=O 10.1021/jm8001444
24865543 194907 0 None -31 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 7 0 4 4.9 CC(=O)N(C)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL498356 194907 0 None -31 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 431 7 0 4 4.9 CC(=O)N(C)c1cccc(CC2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
22611622 11466 8 None -39 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 271 2 2 2 2.9 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2c1 10.1021/jm030020m
CHEMBL103424 11466 8 None -39 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 271 2 2 2 2.9 CC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2c1 10.1021/jm030020m
11047115 11792 0 None -9 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc([N+](=O)[O-])c4)nc23)CC1 10.1021/jm030020m
CHEMBL105118 11792 0 None -9 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 379 4 2 5 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc([N+](=O)[O-])c4)nc23)CC1 10.1021/jm030020m
11056946 115670 0 None -54 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccs4)nc23)CC1 10.1021/jm030020m
CHEMBL321080 115670 0 None -54 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 340 3 2 4 3.7 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccs4)nc23)CC1 10.1021/jm030020m
142601329 193296 5 None -588 7 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
CHEMBL4877603 193296 5 None -588 7 Human 5.4 pKi = 5.4 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 276 2 2 3 2.5 Clc1cccc(-c2n[nH]cc2N2CCCNCC2)c1 10.1021/acs.jmedchem.1c01093
176 7186 66 None -10 31 Rat 4.4 pKi = 4.4 Binding
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 7186 66 None -10 31 Rat 4.4 pKi = 4.4 Binding
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 7186 66 None -10 31 Rat 4.4 pKi = 4.4 Binding
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 7186 66 None -10 31 Rat 4.4 pKi = 4.4 Binding
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 7186 66 None -10 31 Rat 4.4 pKi = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 nan
23533328 91951 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 8 2 7 2.6 COc1cc(N(C)CCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL225308 91951 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 479 8 2 7 2.6 COc1cc(N(C)CCN(C)C)c2[nH]c(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(=O)c2c1 10.1016/j.bmc.2006.10.037
193381 17812 21 None -1258 4 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2cccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
CHEMBL11760 17812 21 None -1258 4 Rat 5.4 pKi = 5.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 261 6 0 2 3.7 CCCN(CCC)C1CCc2cccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
6918647 107522 2 None -79 14 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL292759 107522 2 None -79 14 Human 6.4 pKi = 6.4 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 439 5 1 5 3.0 COc1ccc(NS(=O)(=O)c2ccc(Br)cc2)cc1N1CCN(C)CC1 10.1021/jm980532e
10216160 74369 0 None -125 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4cccc5cc[nH]c45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL190190 74369 0 None -125 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 400 6 1 4 4.2 Cc1ccc2c(OCCN3CCN(Cc4cccc5cc[nH]c45)CC3)cccc2n1 10.1021/jm049039v
11464355 134011 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 422 7 1 7 3.4 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL365810 134011 0 None -39 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 422 7 1 7 3.4 Cc1ccc2c(OCCN3CCN(Cc4ccc(O)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
11178830 154905 0 None -251 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL393539 154905 0 None -251 9 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 467 6 1 5 4.5 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4F)NC(=O)CO5)CC3)cc(F)cc2n1 10.1016/j.bmcl.2006.11.031
44588742 198028 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.4 Cc1ccc2c(OCCCN3CC(Oc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL519019 198028 0 None -2 3 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.4 Cc1ccc2c(OCCCN3CC(Oc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
10423801 34401 0 None - 1 Rat 6.4 pKi = 6.4 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 280 1 0 4 2.5 Cc1cccc2nc(N3CCN(C)CC3)c3cccn3c12 10.1021/jm990151g
CHEMBL136978 34401 0 None - 1 Rat 6.4 pKi = 6.4 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 280 1 0 4 2.5 Cc1cccc2nc(N3CCN(C)CC3)c3cccn3c12 10.1021/jm990151g
10249573 214372 0 None -398 11 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
CHEMBL94984 214372 0 None -398 11 Human 5.4 pKi = 5.4 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor (human cloned receptor) in CHO cells using [3H]5-HT as radioligand
ChEMBL 386 5 0 3 4.1 CC1CCN(CC[C@H]2CCCN2S(=O)(=O)c2cccc3ccccc23)CC1 10.1021/jm991151j
10689158 123453 0 None - 1 Rat 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 349 3 0 6 3.3 c1csc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c1 10.1021/jm990151g
CHEMBL337101 123453 0 None - 1 Rat 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.The compound was tested for the binding affinity against 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand.
ChEMBL 349 3 0 6 3.3 c1csc(CN2CCN(c3nc4cccnc4n4cccc34)CC2)c1 10.1021/jm990151g
9892409 107727 0 None -794 9 Human 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29410 107727 0 None -794 9 Human 5.4 pKi = 5.4 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 505 5 1 6 5.3 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCCCC2C1 10.1016/s0960-894x(02)00172-5
108029 10187 57 None -3 13 Rat 8.4 pKi = 8.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
23 10187 57 None -3 13 Rat 8.4 pKi = 8.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
CHEMBL18785 10187 57 None -3 13 Rat 8.4 pKi = 8.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 10.1021/jm00384a001
14479837 214290 7 None 2 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 234 5 1 3 2.3 CCCCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9452 214290 7 None 2 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 234 5 1 3 2.3 CCCCOc1ccccc1N1CCNCC1 10.1021/jm00125a020
5 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
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 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
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 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
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 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity to human 5-HT1B receptor by radioligand displacement assayBinding affinity to human 5-HT1B receptor by radioligand displacement assay
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/j.ejmech.2013.01.044
5 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
5202 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
CHEMBL39 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
DB08839 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligandBinding affinity towards cloned human 5-hydroxytryptamine 1D receptor beta was determined using [3H]8-OH-DPAT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm950498t
5 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5202 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
CHEMBL39 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
DB08839 6927 72 None -11 53 Human 8.4 pKi = 8.4 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
107 6929 121 None -30 31 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
1833 6929 121 None -30 31 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
CHEMBL8165 6929 121 None -30 31 Rat 8.4 pKi = 8.4 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00399a031
10972931 214844 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm020938y
CHEMBL97650 214844 0 None 8 4 Human 8.4 pKi = 8.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4cncnc4)cc23)CC1 10.1021/jm020938y
44342830 174760 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 5 2 3 5.1 COc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
CHEMBL431866 174760 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 5 2 3 5.1 COc1ccc(NC(=O)N2CC=C(c3ccc4[nH]cc(C[C@H]5CCCN5C)c4c3)CC2)cc1 10.1016/s0960-894x(03)00779-0
2869 10924 89 None -8 7 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60 10924 89 None -8 7 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
60857 10924 89 None -8 7 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
CHEMBL1185 10924 89 None -8 7 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
DB00315 10924 89 None -8 7 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligandIn vitro binding affinity was determined towards cloned human 5-hydroxytryptamine 1B receptor using [3H]5-CT radioligand
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1016/s0960-894x(98)00090-0
11384146 208512 0 None -10 9 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
CHEMBL606556 208512 0 None -10 9 Human 8.4 pKi = 8.4 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 403 5 2 3 4.3 CN1CCC[C@@H]1Cc1c[nH]c2ccc(NS(=O)(=O)c3cccc(Cl)c3)cc12 10.1021/jm049243i
107780 8625 54 None 1 18 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
14 8625 54 None 1 18 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
CHEMBL15928 8625 54 None 1 18 Human 8.4 pKi = 8.4 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1016/j.bmcl.2005.07.024
1355 8792 88 None -1 16 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
142 8792 88 None -1 16 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
CHEMBL478 8792 88 None -1 16 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
DB12110 8792 88 None -1 16 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00125a020
59636780 132470 0 None - 1 Chinese hamster 8.4 pKi = 8.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 404 5 0 5 3.4 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCCC1 nan
CHEMBL3647274 132470 0 None - 1 Chinese hamster 8.4 pKi = 8.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 404 5 0 5 3.4 O=C(c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)N1CCCC1 nan
1588 9105 27 None -58 44 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
28864 9105 27 None -58 44 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
43 9105 27 None -58 44 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
CHEMBL157138 9105 27 None -58 44 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
DB00589 9105 27 None -58 44 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC nan
10751317 15421 21 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 218 5 2 2 2.5 CCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL109526 15421 21 None 19 2 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 218 5 2 2 2.5 CCCOc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
5 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
5202 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
CHEMBL39 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
DB08839 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm020938y
44342722 117320 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 4 2 2 5.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL325175 117320 0 None -10 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 4 2 2 5.1 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(C(=O)Nc4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
19066235 18157 0 None 75 3 Human 7.4 pKi = 7.4 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL110601 18157 0 None 75 3 Human 7.4 pKi = 7.4 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
CHEMBL1180011 18157 0 None 75 3 Human 7.4 pKi = 7.4 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 437 6 1 6 2.5 COc1ccc(NCC(=O)N2CCN(c3ccccc3C)CC2)cc1N1CCN(C)CC1 10.1016/S0960-894X(97)10164-0
44376516 63158 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 6 2 3 4.2 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
CHEMBL163151 63158 0 None -4 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 414 6 2 3 4.2 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
2105 9828 37 None -6 32 Rat 7.4 pKi = 7.4 Binding
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 9828 37 None -6 32 Rat 7.4 pKi = 7.4 Binding
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 9828 37 None -6 32 Rat 7.4 pKi = 7.4 Binding
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 9828 37 None -6 32 Rat 7.4 pKi = 7.4 Binding
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 9828 37 None -6 32 Rat 7.4 pKi = 7.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 nan
10782681 116244 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 12 1 2 5.4 CCCCCCCCCOc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL322054 116244 0 None 1 3 Human 7.4 pKi = 7.4 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 330 12 1 2 5.4 CCCCCCCCCOc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
11740280 109703 0 None -15 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 376 8 1 2 5.4 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL306197 109703 0 None -15 4 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 376 8 1 2 5.4 CCCN(CCCc1ccccc1OC)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
107 6929 121 None -30 31 Rat 6.4 pKi = 6.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
1833 6929 121 None -30 31 Rat 6.4 pKi = 6.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
CHEMBL8165 6929 121 None -30 31 Rat 6.4 pKi = 6.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00384a001
161 7541 6 None -16 6 Rat 6.4 pKi = 6.4 Binding
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 7541 6 None -16 6 Rat 6.4 pKi = 6.4 Binding
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 7541 6 None -16 6 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 286 5 2 3 3.7 CC(Cc1c[nH]c2c1cc(OCc1cccs1)cc2)N nan
14083214 67098 2 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
CHEMBL1744074 67098 2 None - 1 Rat 5.4 pKi = 5.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2cccc(O)c12 10.1021/jm00402a026
441383 27105 57 None -19 17 Rat 4.4 pKi = 4.4 Binding
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 27105 57 None -19 17 Rat 4.4 pKi = 4.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10247448 211168 0 None -7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 352 6 1 1 5.3 CCCN(CCC)C1CCc2ccc3[nH]cc(CC(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL71899 211168 0 None -7 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 352 6 1 1 5.3 CCCN(CCC)C1CCc2ccc3[nH]cc(CC(F)(F)F)c3c2C1 10.1021/jm00012a021
CHEMBL5077293 221270 0 None -144 9 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(C2CCNC2)ccc1Cl 10.1021/acs.jmedchem.1c00110
44376491 62264 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 1 3 5.4 O=S(=O)(c1cccc2ccccc12)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
CHEMBL162011 62264 0 None -15 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 485 6 1 3 5.4 O=S(=O)(c1cccc2ccccc12)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
73346042 98609 5 None -4073 17 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
CHEMBL2413153 98609 5 None -4073 17 Human 6.4 pKi = 6.4 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 405 9 0 8 0.9 Cn1c(=O)cnn(CCCCN2CCN(c3ccccc3OCCF)CC2)c1=O 10.1016/j.bmc.2013.05.050
44438462 97749 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 506 6 0 6 6.0 CC1CC(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CC1C 10.1016/j.bmcl.2006.12.109
CHEMBL239598 97749 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cellsDisplacement of [3H]5-hydroxytrytamine from human 5HT1B receptor expressed in HEK293 cells
ChEMBL 506 6 0 6 6.0 CC1CC(N2CCN(C3CCc4ccc(OCc5noc(-c6ccc(Cl)cc6)n5)cc43)CC2)CC1C 10.1016/j.bmcl.2006.12.109
182596 125264 16 None -269 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL341391 125264 16 None -269 3 Rat 6.4 pKi = 6.4 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
14083211 84640 6 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@H](C)N)c2c1 10.1021/jm00402a026
CHEMBL2093088 84640 6 None - 1 Rat 6.4 pKi = 6.4 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2[nH]cc(C[C@H](C)N)c2c1 10.1021/jm00402a026
76330157 113024 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260926 113024 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138918 113024 0 None -1 2 Human 5.4 pKi = 5.4 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1ccc(Cl)cc1Cl 10.1007/s00044-009-9164-1
59636715 132468 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 440 6 1 5 3.7 O=C(NC1CC(F)(F)C1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647272 132468 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 440 6 1 5 3.7 O=C(NC1CC(F)(F)C1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
9796627 103428 0 None -14 7 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
CHEMBL263700 103428 0 None -14 7 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 308 4 1 4 3.1 CN(C)CCc1cn(C(=O)c2ccccc2)c2ccc(O)cc12 10.1021/jm010943m
10359357 207279 1 None - 1 Rat 6.4 pKi = 6.4 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 331 1 1 4 3.2 c1ccc2c(c1)OCCc1c(N3CCNCC3)nc3ccccc3c1-2 10.1021/jm00014a021
CHEMBL59871 207279 1 None - 1 Rat 6.4 pKi = 6.4 Binding
The compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligandThe compound was tested for their binding affinity towards 5-hydroxytryptamine 1B receptor from rat striatum using [3H]5-HT as radioligand
ChEMBL 331 1 1 4 3.2 c1ccc2c(c1)OCCc1c(N3CCNCC3)nc3ccccc3c1-2 10.1021/jm00014a021
169764 39888 8 None -602 2 Rat 5.4 pKi = 5.4 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 260 7 2 2 3.5 CCCN(CCC)CCc1c[nH]c2ccc(O)cc12 10.1021/jm00399a031
CHEMBL141706 39888 8 None -602 2 Rat 5.4 pKi = 5.4 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 260 7 2 2 3.5 CCCN(CCC)CCc1c[nH]c2ccc(O)cc12 10.1021/jm00399a031
135398745 9688 112 None -162 65 Rat 6.4 pKi = 6.4 Binding
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 9688 112 None -162 65 Rat 6.4 pKi = 6.4 Binding
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 9688 112 None -162 65 Rat 6.4 pKi = 6.4 Binding
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 9688 112 None -162 65 Rat 6.4 pKi = 6.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C nan
10403260 211065 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 0 3 4.0 CCCN(CCC)C1CCc2ccc3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
CHEMBL71299 211065 0 None -10 4 Human 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 0 3 4.0 CCCN(CCC)C1CCc2ccc3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
44376262 173876 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 7 2 4 4.2 COc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL428991 173876 0 None -5 2 Human 7.4 pKi = 7.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 444 7 2 4 4.2 COc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
59636739 132983 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 469 7 1 6 4.4 Cc1ccc(C(C)NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3650026 132983 0 None - 1 Chinese hamster 7.4 pKi = 7.4 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 469 7 1 6 4.4 Cc1ccc(C(C)NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
91965 214809 96 None 1 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9746 214809 96 None 1 2 Rat 7.4 pKi = 7.4 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 176 1 1 2 1.4 Cc1ccccc1N1CCNCC1 10.1021/jm00125a020
9954663 63298 0 None -20 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 435 6 1 3 4.3 O=S(=O)(c1ccccc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
CHEMBL163639 63298 0 None -20 2 Human 6.4 pKi = 6.4 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 435 6 1 3 4.3 O=S(=O)(c1ccccc1)N1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1 10.1016/j.bmcl.2003.11.023
44395809 129882 0 None -91 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 1 3 3.5 CN1CCC(N2CCc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
CHEMBL361061 129882 0 None -91 4 Human 6.4 pKi = 6.4 Binding
In vitro binding affinity for human 5-hydroxytryptamine 1B receptorIn vitro binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 1 3 3.5 CN1CCC(N2CCc3ccc(NC(=O)c4ccc(F)cc4)cc32)CC1 10.1016/j.bmcl.2004.09.079
9881603 130074 0 None -134 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 258 2 1 2 3.5 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCCN1 10.1016/j.bmcl.2004.06.085
CHEMBL361470 130074 0 None -134 2 Human 5.4 pKi = 5.4 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
ChEMBL 258 2 1 2 3.5 Cc1cc(C(C)(C)C)cc(C)c1CC1=NCCCN1 10.1016/j.bmcl.2004.06.085
10563980 206448 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 1.9 N#CC1=Cc2cccc(OCC3CNCCO3)c2CC1 10.1021/jm970806i
CHEMBL59300 206448 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 270 3 1 4 1.9 N#CC1=Cc2cccc(OCC3CNCCO3)c2CC1 10.1021/jm970806i
11812916 119104 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)cn1 10.1021/jm020938y
CHEMBL329280 119104 0 None 1 4 Human 7.4 pKi = 7.4 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1cc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)cn1 10.1021/jm020938y
150885 105439 34 None -8 3 Rat 7.4 pKi = 7.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
CHEMBL1256286 105439 34 None -8 3 Rat 7.4 pKi = 7.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
CHEMBL277362 105439 34 None -8 3 Rat 7.4 pKi = 7.4 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 190 3 3 2 1.6 CNCCc1c[nH]c2ccc(O)cc12 10.1021/jm00384a001
15124076 52619 0 None -40 3 Rat 7.4 pKi = 7.4 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 438 8 0 5 4.0 CCC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL153136 52619 0 None -40 3 Rat 7.4 pKi = 7.4 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 438 8 0 5 4.0 CCC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
6603907 39789 9 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
CHEMBL1416204 39789 9 None - 1 Rat 7.3 pKi = 7.3 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 2 3 2 1.8 C[C@H](N)Cc1c[nH]c2ccc(O)cc12 10.1021/jm00402a026
24881687 179593 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL451394 179593 0 None -3 2 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
10406614 211195 0 None -457 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 366 7 1 3 4.9 CCCN(CCc1cccs1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL72062 211195 0 None -457 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 366 7 1 3 4.9 CCCN(CCc1cccs1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10064500 210938 0 None -2398 4 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 5 1 1 4.9 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL70606 210938 0 None -2398 4 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 318 5 1 1 4.9 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
9955015 69868 5 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL1744087 69868 5 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL1789131 69868 5 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OC[C@H]1CNCCO1 10.1021/jm970806i
CHEMBL5276321 200673 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat 5-HT1BBinding affinity to rat 5-HT1B
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1COCCN1 10.1016/j.ejmech.2016.07.057
10131024 182940 16 None -47 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 1 1 3.4 CCc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL45929 182940 16 None -47 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 242 3 1 1 3.4 CCc1ccc2[nH]cc(C[C@H]3CCCN3C)c2c1 10.1016/s0960-894x(00)00322-x
31101 7516 40 None -48 35 Rat 7.3 pKi = 7.3 Binding
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 7516 40 None -48 35 Rat 7.3 pKi = 7.3 Binding
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 7516 40 None -48 35 Rat 7.3 pKi = 7.3 Binding
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 7516 40 None -48 35 Rat 7.3 pKi = 7.3 Binding
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 7516 40 None -48 35 Rat 7.3 pKi = 7.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C nan
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(00)00322-x
135 9310 43 None -851 56 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
1796 9310 43 None -851 56 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
4184 9310 43 None -851 56 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
CHEMBL6437 9310 43 None -851 56 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
DB06148 9310 43 None -851 56 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1021/jm00384a001
10912152 108230 0 None -89 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 4 1 1 3.9 CC(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
CHEMBL297660 108230 0 None -89 2 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 256 4 1 1 3.9 CC(C)c1ccc2[nH]cc(CCN3CCCC3)c2c1 10.1016/s0960-894x(00)00322-x
44383728 172125 1 None -15 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 330 4 1 2 5.2 Clc1ccc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)s1 10.1016/s0960-894x(00)00133-5
CHEMBL423610 172125 1 None -15 2 Human 6.3 pKi = 6.3 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 330 4 1 2 5.2 Clc1ccc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)s1 10.1016/s0960-894x(00)00133-5
9826801 114714 0 None -208 12 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL319352 114714 0 None -208 12 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 1 7 3.2 Cn1nnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
11016418 112899 0 None -776 9 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL313424 112899 0 None -776 9 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 488 6 0 7 4.2 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCOC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
2470 10425 50 None -43651 58 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
3300 10425 50 None -43651 58 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
5265 10425 50 None -43651 58 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
99 10425 50 None -43651 58 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
CHEMBL267930 10425 50 None -43651 58 Rat 5.3 pKi = 5.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1021/jm00384a001
71062768 150514 0 None -12 4 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
CHEMBL3900699 150514 0 None -12 4 Mouse 5.3 pKi = 5.3 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 382 6 0 5 2.4 COc1cccc(OC[C@@H]2CN(CC(=O)N3CCc4ccccc43)CCO2)c1 nan
10376496 109676 0 None -147 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 228 3 2 1 3.0 CCCNC1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
CHEMBL305976 109676 0 None -147 4 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 228 3 2 1 3.0 CCCNC1CCc2ccc3[nH]ccc3c2C1 10.1021/jm00012a022
192260 84019 7 None -34 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@H]2C1 10.1021/jm00027a013
CHEMBL2079597 84019 7 None -34 2 Rat 4.3 pKi = 4.3 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@H]2C1 10.1021/jm00027a013
44582678 188353 0 None -33 10 Human 5.3 pKi = 5.3 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL476839 188353 0 None -33 10 Human 5.3 pKi = 5.3 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 401 9 1 4 4.3 COc1c(OCCF)cccc1C(O)C1CCN(CCc2ccc(C)cc2)CC1 10.1016/j.bmc.2009.03.021
9998026 122162 0 None -173 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL335010 122162 0 None -173 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 3 0 4 3.0 c1ccc2c(c1)CC(CN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
10379833 109516 0 None -162 3 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 296 6 1 2 3.7 C=CCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL304984 109516 0 None -162 3 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 296 6 1 2 3.7 C=CCN(CCC)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
1809 6922 32 None -32 37 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
4 6922 32 None -32 37 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
CHEMBL18840 6922 32 None -32 37 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 10.1021/jm00384a001
5 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
5202 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
CHEMBL39 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
DB08839 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00164a046
59636778 133002 0 None - 1 Chinese hamster 8.3 pKi = 8.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 478 5 0 5 3.5 CC(=O)N1CCc2cc(CCN3CCN(c4cc(F)cc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
CHEMBL3650044 133002 0 None - 1 Chinese hamster 8.3 pKi = 8.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 478 5 0 5 3.5 CC(=O)N1CCc2cc(CCN3CCN(c4cc(F)cc5cc(C(=O)N(C)C)oc45)CC3)ccc21 nan
44402894 104985 0 None 3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 551 5 0 7 5.8 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL274256 104985 0 None 3 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 551 5 0 7 5.8 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4noc(C)n4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
44402895 131330 0 None 50 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 533 5 1 6 5.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4ncccn4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL364056 131330 0 None 50 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 533 5 1 6 5.5 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(-c4ncccn4)cc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
9871977 172873 0 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 539 5 1 6 4.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(N4CCCC4=O)nc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL425919 172873 0 None 79 2 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 539 5 1 6 4.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3ccc(N4CCCC4=O)nc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
5 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
5202 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
CHEMBL39 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
DB08839 6927 72 None -11 53 Human 8.3 pKi = 8.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligandBinding affinity against cloned human 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm0341204
49850980 63239 0 None -12 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1632213 63239 0 None -12 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 468 6 1 4 5.3 Cc1ccc2c(N3CCN(CCc4cccc(NC(=O)c5ccc(F)cc5)c4)CC3)cccc2n1 10.1021/jm100714c
9957376 182936 0 None -25 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 457 7 0 4 5.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL459282 182936 0 None -25 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 457 7 0 4 5.7 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
17947861 78225 1 None 1 3 Human 8.3 pKi = 8.3 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 6 2.9 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn(C)c2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
CHEMBL196140 78225 1 None 1 3 Human 8.3 pKi = 8.3 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 444 2 0 6 2.9 CN1CCN(c2nccc3cc4c(cc23)N(C(=O)c2cnn(C)c2C(F)(F)F)CC4)CC1 10.1016/j.bmcl.2005.06.042
134551 7146 27 None -5 21 Rat 8.3 pKi = 8.3 Binding
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 7146 27 None -5 21 Rat 8.3 pKi = 8.3 Binding
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 7146 27 None -5 21 Rat 8.3 pKi = 8.3 Binding
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 7146 27 None -5 21 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C nan
5 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5202 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
CHEMBL39 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
DB08839 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00044a001
5 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
5202 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
CHEMBL39 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
DB08839 6927 72 None -13 53 Rat 8.3 pKi = 8.3 Binding
Evaluated for binding affinity towards 5-hydroxytryptamine 1B receptorEvaluated for binding affinity towards 5-hydroxytryptamine 1B receptor
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00399a031
2543 10479 68 None -3 32 Human 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
5358 10479 68 None -3 32 Human 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
54 10479 68 None -3 32 Human 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
CHEMBL128 10479 68 None -3 32 Human 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
DB00669 10479 68 None -3 32 Human 8.3 pKi = 8.3 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00044a001
10775128 195510 3 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL50492 195510 3 None -2 3 Human 8.3 pKi = 8.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 216 4 1 1 2.8 CCc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
44342767 121737 0 None -8 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL334259 121737 0 None -8 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 4 2 2 5.5 CN1CCC[C@@H]1Cc1c[nH]c2ccc(C3=CCN(/C(S)=N/c4ccccc4)CC3)cc12 10.1016/s0960-894x(03)00779-0
11016395 118330 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1nccc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL328048 118330 0 None -1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 486 6 1 5 4.4 Cn1nccc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
2303 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
4946 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
564 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
63 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
91536 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
CHEMBL27 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
CHEMBL452861 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
DB00571 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00384a001
59636757 132485 0 None - 1 Chinese hamster 7.3 pKi = 7.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 448 7 1 6 3.3 O=C(NCC1CCOCC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647289 132485 0 None - 1 Chinese hamster 7.3 pKi = 7.3 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 448 7 1 6 3.3 O=C(NCC1CCOCC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
2303 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
4946 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
564 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
63 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
91536 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL27 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
CHEMBL452861 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
DB00571 9961 68 None -57 26 Rat 7.3 pKi = 7.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C 10.1021/jm00124a021
44402878 78182 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 506 4 1 5 5.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL195897 78182 0 None 2 3 Human 7.3 pKi = 7.3 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 506 4 1 5 5.6 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cccc(C)n3)c3ccccc13)CC2 10.1016/j.bmcl.2005.07.085
44588721 191125 0 None -6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.3 Cc1ccc2c(OCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL484387 191125 0 None -6 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 419 7 1 6 3.3 Cc1ccc2c(OCCN3CC(COc4ccc5c(c4)NC(=O)CO5)C3)cccc2n1 10.1016/j.bmcl.2008.08.110
10024936 191742 0 None -19 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485395 191742 0 None -19 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 416 5 1 5 3.6 Cc1ccc2c(N3CCN(CCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
24865542 194906 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 1 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL498355 194906 0 None -39 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 445 8 1 4 5.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)C(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
10194820 195643 0 None -158 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 432 7 0 5 3.7 CC(=O)N(C)c1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
CHEMBL506942 195643 0 None -158 3 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 432 7 0 5 3.7 CC(=O)N(C)c1cccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)c1 10.1021/jm8001444
9891618 113901 0 None -501 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
CHEMBL316081 113901 0 None -501 6 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 486 4 1 6 5.0 Cc1c(S(=O)(=O)Nc2ccc3nccc(N4CCN(C)CC4)c3c2)sc2ccc(Cl)cc12 10.1016/s0960-894x(01)00558-3
9891002 114185 0 None -501 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
CHEMBL318018 114185 0 None -501 7 Human 6.3 pKi = 6.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 472 4 2 6 4.6 Cc1sc2ccc(Cl)cc2c1S(=O)(=O)Nc1ccc2nccc(N3CCNCC3)c2c1 10.1016/s0960-894x(01)00558-3
24865539 194424 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
CHEMBL494991 194424 0 None -39 3 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 391 7 0 5 3.7 COc1ccc(CN2CCN(CCOc3cccc4nc(C)ccc34)CC2)cc1 10.1021/jm8001444
1534 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
14975310 84008 0 None -66 2 Rat 5.3 pKi = 5.3 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@@H]2C1 10.1021/jm00027a013
CHEMBL2079544 84008 0 None -66 2 Rat 5.3 pKi = 5.3 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 245 3 0 2 3.1 CCCN1CC[C@H]2c3c(cccc3OC)C[C@@H]2C1 10.1021/jm00027a013
9957068 58718 0 None -1000 5 Human 5.3 pKi = 5.3 Binding
Evaluated for the binding affinity to 5-hydroxytryptamine 1B receptorEvaluated for the binding affinity to 5-hydroxytryptamine 1B receptor
ChEMBL 486 8 1 5 4.3 CS(=O)(=O)Oc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccc(F)cc3)CC1)C2 10.1016/s0960-894x(01)00037-3
CHEMBL158627 58718 0 None -1000 5 Human 5.3 pKi = 5.3 Binding
Evaluated for the binding affinity to 5-hydroxytryptamine 1B receptorEvaluated for the binding affinity to 5-hydroxytryptamine 1B receptor
ChEMBL 486 8 1 5 4.3 CS(=O)(=O)Oc1ccc2c(c1)CN(CC[C@H]1CC[C@H](NC(=O)/C=C/c3ccc(F)cc3)CC1)C2 10.1016/s0960-894x(01)00037-3
10164215 148787 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 504 6 1 8 3.2 COc1cc(N2CCN(C)CC2)c2nc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(N(C)C)c2c1 10.1016/j.bmc.2006.10.037
CHEMBL387545 148787 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 504 6 1 8 3.2 COc1cc(N2CCN(C)CC2)c2nc(C(=O)Nc3ccc(N4CCOCC4)cc3)cc(N(C)C)c2c1 10.1016/j.bmc.2006.10.037
44339072 118155 1 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 5 1 3 2.8 CC(C)C(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL327103 118155 1 None 1 2 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 274 5 1 3 2.8 CC(C)C(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
4376990 199788 5 None -20 11 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5207529 199788 5 None -20 11 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
CHEMBL5222754 199788 5 None -20 11 Human 7.3 pKi = 7.3 Binding
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 372 4 2 4 4.1 COc1cc(OC)c(C2NCCc3c2[nH]c2ccc(Cl)cc32)cc1OC 10.1021/acsmedchemlett.1c00694
1574 6869 60 None -24 21 Rat 6.3 pKi = 6.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
218 6869 60 None -24 21 Rat 6.3 pKi = 6.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
CHEMBL266591 6869 60 None -24 21 Rat 6.3 pKi = 6.3 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 10.1021/jm00164a046
44581972 182379 0 None -17 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458001 182379 0 None -17 10 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 499 6 2 6 4.3 O=C(Nc1cccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)c1)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
10663236 12233 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 11 2 2 5.2 CCCCCCCCCOc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm950498t
CHEMBL107487 12233 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 316 11 2 2 5.2 CCCCCCCCCOc1ccc2[nH]cc(CC(C)N)c2c1 10.1021/jm950498t
3025067 106158 64 None -2 15 Rat 7.3 pKi = 7.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
65853 106158 64 None -2 15 Rat 7.3 pKi = 7.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
CHEMBL282614 106158 64 None -2 15 Rat 7.3 pKi = 7.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 10.1021/jm00020a020
10248619 121908 0 None -138 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 370 3 0 4 3.6 Clc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL334381 121908 0 None -138 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 370 3 0 4 3.6 Clc1cccc2c1CC2CN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9997421 210916 0 None -22 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
CHEMBL70431 210916 0 None -22 3 Human 6.3 pKi = 6.3 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)C1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
1220 6975 55 None -208 44 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
31 6975 55 None -208 44 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
7 6975 55 None -208 44 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
CHEMBL56 6975 55 None -208 44 Human 6.3 pKi = 6.3 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1016/s0960-894x(98)00222-4
1534 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
9287 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
CHEMBL30713 109817 53 None -5 12 Human 6.3 pKi = 6.3 Binding
Displacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysisDisplacement of [3H]GR127543 from human recombinant 5-HT1B receptor expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting analysis
ChEMBL 174 2 2 1 2.1 CC(N)Cc1c[nH]c2ccccc12 10.1016/j.bmcl.2013.03.066
2435 10362 83 None -128 48 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
60149 10362 83 None -128 48 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
98 10362 83 None -128 48 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
CHEMBL12713 10362 83 None -128 48 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
DB06144 10362 83 None -128 48 Human 7.3 pKi = 7.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1021/jm020938y
10021450 109479 0 None -1412 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 360 7 1 2 4.8 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL304767 109479 0 None -1412 4 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 360 7 1 2 4.8 CCCN(CCc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
10973768 114337 0 None -1445 10 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL318901 114337 0 None -1445 10 Human 6.3 pKi = 6.3 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 563 6 1 8 4.4 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCn4c(=O)[nH]c5ccccc5c4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
9976035 27822 0 None -489 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
CHEMBL131184 27822 0 None -489 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.7 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
14519861 65938 0 None -25 2 Rat 5.3 pKi = 5.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 313 11 0 2 5.5 CCCCN(CCCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL169956 65938 0 None -25 2 Rat 5.3 pKi = 5.3 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 313 11 0 2 5.5 CCCCN(CCCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
44304338 107356 0 None -5 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 275 6 0 2 4.0 CCCN(CCC)C1CCc2c(C)ccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
CHEMBL291620 107356 0 None -5 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 275 6 0 2 4.0 CCCN(CCC)C1CCc2c(C)ccc(OC)c2C1 10.1016/S0960-894X(01)81009-X
3228 9920 23 None -6456 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
9909448 9920 23 None -6456 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
CHEMBL71838 9920 23 None -6456 7 Human 5.2 pKi = 5.2 Binding
Displacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay basedDisplacement of [3H]serotonin from recombinant human 5-HT1B receptor expressed in HEK293 cells incubated for 1 hr by competitive radioligand binding assay based
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1016/j.ejmech.2020.113073
3228 9920 23 None -6456 7 Western lowland gorilla 5.2 pKi = 5.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
9909448 9920 23 None -6456 7 Western lowland gorilla 5.2 pKi = 5.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
CHEMBL71838 9920 23 None -6456 7 Western lowland gorilla 5.2 pKi = 5.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 409 6 1 5 2.9 CNC(=O)c1ccc2c(c1)CCO[C@H]2CCN1CCN(CC1)c1ccc(cc1)OC 10.1021/jm980137o
10774567 110599 0 None -5 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(O)c(C)c1CC1=NCCN1 10.1021/jm970513p
CHEMBL309162 110599 0 None -5 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 204 2 2 3 1.6 Cc1ccc(O)c(C)c1CC1=NCCN1 10.1021/jm970513p
44376395 59368 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 7 2 4 4.8 COc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL159278 59368 0 None -9 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 460 7 2 4 4.8 COc1ccc(C(=S)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL5094234 222352 0 None -275 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5096019 222352 0 None -275 8 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
23288790 210743 0 None -691 6 Western lowland gorilla 5.2 pKi = 5.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
CHEMBL69385 210743 0 None -691 6 Western lowland gorilla 5.2 pKi = 5.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 395 6 1 5 2.6 COc1ccc(N2CCN(CCC3OCCc4cc(C(N)=O)ccc43)CC2)cc1 10.1021/jm980137o
9972838 211082 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 1 2 4.4 CCCN(CCC)C1CCc2ccc3[nH]cc(C(C)=O)c3c2C1 10.1021/jm00012a021
CHEMBL71395 211082 0 None -41 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 312 6 1 2 4.4 CCCN(CCC)C1CCc2ccc3[nH]cc(C(C)=O)c3c2C1 10.1021/jm00012a021
44581974 182483 0 None -11 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458220 182483 0 None -11 9 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
2585 7590 103 None -100 22 Rat 6.2 pKi = 6.2 Binding
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 7590 103 None -100 22 Rat 6.2 pKi = 6.2 Binding
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 7590 103 None -100 22 Rat 6.2 pKi = 6.2 Binding
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 7590 103 None -100 22 Rat 6.2 pKi = 6.2 Binding
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 7590 103 None -100 22 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O nan
160463 75963 31 None -3 3 Rat 5.2 pKi = 5.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cc(O)ccc12 10.1021/jm00384a001
CHEMBL19264 75963 31 None -3 3 Rat 5.2 pKi = 5.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2cc(O)ccc12 10.1021/jm00384a001
44338900 116421 1 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 260 5 1 3 2.6 CCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
CHEMBL322349 116421 1 None -3 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 260 5 1 3 2.6 CCC(=O)Oc1ccc2[nH]cc(CCN(C)C)c2c1 10.1021/jm950498t
10915350 170185 0 None -53 3 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(C#N)c4)nc23)CC1 10.1021/jm030020m
CHEMBL419547 170185 0 None -53 3 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 359 3 2 4 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)c4cccc(C#N)c4)nc23)CC1 10.1021/jm030020m
10500422 85250 0 None 15 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
CHEMBL2111779 85250 0 None 15 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]GR-125743 as radioligand
ChEMBL 387 7 1 4 4.6 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1/C=C\CN(C)C 10.1021/jm9702948
130 10273 47 None -1 13 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
3378093 10273 47 None -1 13 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
CHEMBL281350 10273 47 None -1 13 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10.1021/jm970457s
11796257 105456 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 417 4 1 4 3.8 COc1ccc(NC(=O)c2ccc(Br)c(C)c2)cc1N1CCN(C)CC1 10.1021/jm970457s
CHEMBL277467 105456 1 None 1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 417 4 1 4 3.8 COc1ccc(NC(=O)c2ccc(Br)c(C)c2)cc1N1CCN(C)CC1 10.1021/jm970457s
10114480 100371 0 None -3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL246597 100371 0 None -3 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10195275 182471 0 None -12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 0 5 4.6 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL458199 182471 0 None -12 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 458 7 0 5 4.6 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44581603 182837 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 1 4 5.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCNCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL459067 182837 0 None -5 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 443 7 1 4 5.3 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCNCC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10127673 194611 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL496098 194611 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10048343 190998 0 None -10 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 430 6 1 5 4.0 Cc1ccc2c(N3CCN(CCCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL483365 190998 0 None -10 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 430 6 1 5 4.0 Cc1ccc2c(N3CCN(CCCCc4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
10127673 194611 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
CHEMBL496098 194611 0 None -6 3 Human 8.2 pKi = 8.2 Binding
Displacement of [3H]5HT from human recombinant 5HT1B receptorDisplacement of [3H]5HT from human recombinant 5HT1B receptor
ChEMBL 460 9 1 5 4.4 Cc1ccc2c(OCCN3CCC(Cc4cccc(NC(=O)CN(C)C)c4)CC3)cccc2n1 10.1021/jm8001444
10481003 109730 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(C(=O)Nc2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
CHEMBL306384 109730 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 497 6 1 7 5.0 COc1ccc(C(=O)Nc2ccc(-c3ccc(-c4noc(C)n4)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
9891594 111658 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 486 6 1 5 4.4 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=O)N(C)C)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
CHEMBL311150 111658 0 None -1 3 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindololIn vitro binding affinity towards 5-hydroxytryptamine 1B receptor in rat striatal membrane with [125I]- iodocyanopindolol
ChEMBL 486 6 1 5 4.4 COc1ccc(NC(=O)c2ccc(-c3ccc(C(=O)N(C)C)cc3C)cc2)cc1N1CCN(C)CC1 10.1021/jm00041a001
10076876 108489 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
CHEMBL29951 108489 0 None -1 3 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 576 19 0 4 8.7 CCCN(CCC)C1CCc2cccc(OCCCCCCOc3cccc4c3CC(N(CCC)CCC)CC4)c2C1 10.1016/s0960-894x(98)00222-4
2543 10479 68 None -2 32 Western lowland gorilla 8.2 pKi = 8.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
5358 10479 68 None -2 32 Western lowland gorilla 8.2 pKi = 8.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
54 10479 68 None -2 32 Western lowland gorilla 8.2 pKi = 8.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
CHEMBL128 10479 68 None -2 32 Western lowland gorilla 8.2 pKi = 8.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
DB00669 10479 68 None -2 32 Western lowland gorilla 8.2 pKi = 8.2 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm980137o
107 6929 121 None -30 31 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
1833 6929 121 None -30 31 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
CHEMBL8165 6929 121 None -30 31 Rat 8.2 pKi = 8.2 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 10.1021/jm00402a026
11092142 214947 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
CHEMBL98299 214947 0 None 1 4 Human 8.2 pKi = 8.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncnc1-c1ccc2c(c1)c(C1CCN(CCN3CCNC3=O)CC1)cn2-c1ccc(F)cc1 10.1021/jm020938y
9817810 24144 1 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
CHEMBL125745 24144 1 None -2 8 Human 8.2 pKi = 8.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 300 4 1 4 2.4 NCCc1cccc2c1ccn2S(=O)(=O)c1ccccc1 10.1021/jm010943m
59636777 132467 0 None - 1 Chinese hamster 8.2 pKi = 8.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 6 1 5 3.1 O=C(NC1CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647271 132467 0 None - 1 Chinese hamster 8.2 pKi = 8.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 390 6 1 5 3.1 O=C(NC1CC1)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
Binding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligandBinding affinity was evaluated at human recombinant 5-hydroxytryptamine 1B receptor using [3H]5-CT as radioligand
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1016/s0960-894x(98)00222-4
10944016 214678 20 None 1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 220 3 1 3 1.9 CC(C)Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9669 214678 20 None 1 3 Rat 8.2 pKi = 8.2 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 220 3 1 3 1.9 CC(C)Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
4233538 204827 4 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
CHEMBL1201939 204827 4 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
CHEMBL57406 204827 4 None - 1 Rat 7.2 pKi = 7.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortexBinding affinity against 5-hydroxytryptamine 1B receptor in membranes of Rat cerebral cortex
ChEMBL 346 5 1 6 1.2 C1=C(CN2CCOCC2)COc2c1cccc2OCC1CNCCO1 10.1021/jm970806i
44560995 185932 0 None -109 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 185932 0 None -109 3 Human 7.2 pKi = 7.2 Binding
Binding affinity to human 5HT1B receptorBinding affinity to human 5HT1B receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
10198320 211389 1 None -46 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 218 2 2 1 3.1 Cc1cc(C(C)(C)C)cc(C)c1CC(=N)N 10.1021/jm970513p
CHEMBL73281 211389 1 None -46 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 218 2 2 1 3.1 Cc1cc(C(C)(C)C)cc(C)c1CC(=N)N 10.1021/jm970513p
11024618 115330 0 None -89 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 2 4 3.2 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
CHEMBL320198 115330 0 None -89 4 Human 5.2 pKi = 5.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 353 3 2 4 3.2 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)nc23)CC1 10.1021/jm030020m
107992 9331 49 None -12 10 Rat 5.2 pKi = 5.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
165 9331 49 None -12 10 Rat 5.2 pKi = 5.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
CHEMBL269521 9331 49 None -12 10 Rat 5.2 pKi = 5.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
DB12111 9331 49 None -12 10 Rat 5.2 pKi = 5.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]spiperone.
ChEMBL 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 10.1021/jm00145a017
182595 26709 14 None -1000 4 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130276 26709 14 None -1000 4 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
25067564 208079 0 None -1348 6 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
CHEMBL604102 208079 0 None -1348 6 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5HT1B receptorBinding affinity to 5HT1B receptor
ChEMBL 392 3 2 5 3.1 N[C@@H]1CCN(c2ccc3[nH]nc(S(=O)(=O)c4cccc5ccccc45)c3c2)C1 10.1021/jm901674f
9860595 16857 2 None -77 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/s0960-894x(03)00779-0
CHEMBL115415 16857 2 None -77 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/s0960-894x(03)00779-0
9860595 16857 2 None -77 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/j.bmcl.2003.11.023
CHEMBL115415 16857 2 None -77 2 Human 6.2 pKi = 6.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 283 4 1 2 3.0 CN(C)CCc1c[nH]c2ccc(C3=CCN(C)CC3)cc12 10.1016/j.bmcl.2003.11.023
11822996 11831 0 None -32 3 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 308 3 2 4 1.7 CN1CCC(c2c[nH]c3ccc(NS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
CHEMBL105327 11831 0 None -32 3 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 308 3 2 4 1.7 CN1CCC(c2c[nH]c3ccc(NS(C)(=O)=O)nc23)CC1 10.1021/jm030020m
14519859 136987 2 None -13 2 Rat 5.2 pKi = 5.2 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 285 9 0 2 4.7 CCCN(CCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL367935 136987 2 None -13 2 Rat 5.2 pKi = 5.2 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 285 9 0 2 4.7 CCCN(CCC)CCCOc1cccc2ccccc12 10.1021/jm00124a021
3823 56995 42 None -38 11 Rat 5.2 pKi = 5.2 Binding
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 56995 42 None -38 11 Rat 5.2 pKi = 5.2 Binding
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 56995 42 None -38 11 Rat 5.2 pKi = 5.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 nan
10091074 123444 0 None -776 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
CHEMBL337078 123444 0 None -776 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 5 0 4 4.1 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCCO3)CC1 10.1021/jm00020a020
10065239 211068 0 None -21 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 6 0 3 4.1 CCCN(CCC)C1CCc2cc(F)c3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
CHEMBL71319 211068 0 None -21 4 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 330 6 0 3 4.1 CCCN(CCC)C1CCc2cc(F)c3c(c(C=O)cn3C)c2C1 10.1021/jm00012a021
44376722 62268 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 6 2 3 4.5 Cc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162012 62268 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 428 6 2 3 4.5 Cc1ccc(C(=O)NN2CC=C(c3ccc4[nH]cc(CCN5CCCC5)c4c3)CC2)cc1 10.1016/j.bmcl.2003.11.023
44339071 15207 1 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 4 1 3 3.2 CN(C)CCc1c[nH]c2ccc(OC(=O)C(C)(C)C)cc12 10.1021/jm950498t
CHEMBL109360 15207 1 None 1 2 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 288 4 1 3 3.2 CN(C)CCc1c[nH]c2ccc(OC(=O)C(C)(C)C)cc12 10.1021/jm950498t
59636760 132475 0 None - 1 Chinese hamster 7.2 pKi = 7.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1cccnc1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3647279 132475 0 None - 1 Chinese hamster 7.2 pKi = 7.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 0 6 3.9 CN(Cc1cccnc1)C(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
10150796 74382 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 401 6 1 5 3.6 Cc1ccc2c(OCCN3CCN(Cc4cccc5[nH]cnc45)CC3)cccc2n1 10.1021/jm049039v
CHEMBL190298 74382 0 None -251 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 401 6 1 5 3.6 Cc1ccc2c(OCCN3CCN(Cc4cccc5[nH]cnc45)CC3)cccc2n1 10.1021/jm049039v
44443098 100704 0 None -15 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 522 8 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(Cc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL248231 100704 0 None -15 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 522 8 0 6 4.7 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(Cc4ccccc4)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10238762 181691 0 None -15 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456458 181691 0 None -15 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 4.2 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCN(C)CC5=O)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10216744 181692 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 7 0 3 6.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccccc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL456459 181692 0 None -7 3 Human 7.2 pKi = 7.2 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 436 7 0 3 6.5 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccccc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
7096 214257 119 None 7 4 Rat 7.2 pKi = 7.2 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00125a020
CHEMBL9434 214257 119 None 7 4 Rat 7.2 pKi = 7.2 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 162 1 1 2 1.1 c1ccc(N2CCNCC2)cc1 10.1021/jm00125a020
2247 7293 81 None -35 42 Rat 6.2 pKi = 6.2 Binding
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 7293 81 None -35 42 Rat 6.2 pKi = 6.2 Binding
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 7293 81 None -35 42 Rat 6.2 pKi = 6.2 Binding
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 7293 81 None -35 42 Rat 6.2 pKi = 6.2 Binding
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 7293 81 None -35 42 Rat 6.2 pKi = 6.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 nan
7694 10284 36 None -316 4 Human 6.2 pKi = 6.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
9910352 10284 36 None -316 4 Human 6.2 pKi = 6.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
CHEMBL2219578 10284 36 None -316 4 Human 6.2 pKi = 6.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 2 3 4.8 N#Cc1ccc2c(c1)CN(CC2)CC[C@@H]1CC[C@H](CC1)NC(=O)c1cc2c([nH]1)cccc2 10.1021/jm000090i
10045226 28537 0 None -489 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 6 0 4 4.1 c1ccc2c(c1)CC2CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL131900 28537 0 None -489 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 6 0 4 4.1 c1ccc2c(c1)CC2CCCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
9890119 214836 0 None -630 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
CHEMBL97596 214836 0 None -630 7 Human 6.2 pKi = 6.2 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 452 4 2 5 4.3 O=S(=O)(Nc1ccc2nccc(N3CCNCC3)c2c1)c1ccc2c(Cl)cccc2c1 10.1016/s0960-894x(01)00558-3
11191906 18539 0 None -12 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181665 18539 0 None -12 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
CHEMBL187928 18539 0 None -12 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 537 12 1 3 7.3 O=C(/C=C/c1ccccc1)N(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)Cc1cccnc1 10.1016/j.bmcl.2005.06.024
9827938 18543 0 None -25 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL1181680 18543 0 None -25 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
CHEMBL188486 18543 0 None -25 12 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HTBinding affinity towards human 5-hydroxytryptamine receptor 1B expressed in CHO cells using the radioligand [3H]5-HT
ChEMBL 517 13 1 3 6.3 CN(C)CCN(Cc1ccc(-c2ccc(CNCCc3ccccc3)cc2)cc1)C(=O)/C=C/c1ccccc1 10.1016/j.bmcl.2005.06.024
10028436 10305 5 None -316 12 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
3237 10305 5 None -316 12 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
CHEMBL95104 10305 5 None -316 12 Human 6.2 pKi = 6.2 Binding
Compound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligandCompound was tested for its binding affinity for human cloned 5-hydroxytryptamine 1B receptor in CHO using [3H]5-HT as a radioligand
ChEMBL 487 7 1 4 4.9 Clc1ccc(cc1)OC1CCN(CC1)CC[C@H]1CCCN1S(=O)(=O)c1ccc2c(c1)[nH]cc2 10.1016/s0960-894x(02)00690-x
10238160 130971 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4cc(Cl)ccc4Cl)CC3)cccc2n1 10.1021/jm049039v
CHEMBL363413 130971 0 None -158 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 429 6 0 4 5.0 Cc1ccc2c(OCCN3CCN(Cc4cc(Cl)ccc4Cl)CC3)cccc2n1 10.1021/jm049039v
44439167 97332 0 None -63 10 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
CHEMBL238732 97332 0 None -63 10 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 483 6 1 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cc(F)c5c(c4)NC(=O)CO5)CC3)cc(Cl)cc2n1 10.1016/j.bmcl.2006.11.031
44588772 191899 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 6 3.8 Cc1ccc2c(OCC3CCN(CC(=O)c4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
CHEMBL485630 191899 0 None -2 3 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 445 6 1 6 3.8 Cc1ccc2c(OCC3CCN(CC(=O)c4ccc5c(c4)NC(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2008.08.110
9935387 106218 0 None -794 14 Human 6.2 pKi = 6.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL282971 106218 0 None -794 14 Human 6.2 pKi = 6.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@@H]2C1 10.1016/s0960-894x(02)00172-5
9913554 107769 0 None -794 14 Human 6.2 pKi = 6.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
CHEMBL29433 107769 0 None -794 14 Human 6.2 pKi = 6.2 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 491 5 1 6 5.0 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN2CCC[C@H]2C1 10.1016/s0960-894x(02)00172-5
1220 6975 55 None -7413 44 Rat 4.2 pKi = 4.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
31 6975 55 None -7413 44 Rat 4.2 pKi = 4.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
7 6975 55 None -7413 44 Rat 4.2 pKi = 4.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
CHEMBL56 6975 55 None -7413 44 Rat 4.2 pKi = 4.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00384a001
71459604 90568 0 None -11 14 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
CHEMBL2205811 90568 0 None -11 14 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 309 4 1 3 2.0 COc1cccc(CCN2C3C4C5CC6C7C5C3C7C2(O)C64)c1 10.1016/j.bmcl.2012.08.046
10767427 91169 1 None -1258 4 Human 5.2 pKi = 5.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
CHEMBL2113352 91169 1 None -1258 4 Human 5.2 pKi = 5.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
CHEMBL2219586 91169 1 None -1258 4 Human 5.2 pKi = 5.2 Binding
Binding activity against human 5-hydroxytryptamine 1B receptorBinding activity against human 5-hydroxytryptamine 1B receptor
ChEMBL 491 7 1 5 4.1 CS(=O)(=O)c1cccc(/C=C/C(=O)N[C@H]2CC[C@H](CCN3CCc4cc(C#N)ccc4C3)CC2)c1 10.1021/jm000090i
44304328 209688 0 None -4 2 Rat 5.2 pKi = 5.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 311 6 0 2 4.8 CCCN(CCC)C1CCc2c(c(OC)cc3ccccc23)C1 10.1016/S0960-894X(01)81009-X
CHEMBL62776 209688 0 None -4 2 Rat 5.2 pKi = 5.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 311 6 0 2 4.8 CCCN(CCC)C1CCc2c(c(OC)cc3ccccc23)C1 10.1016/S0960-894X(01)81009-X
1220 6975 55 None -208 44 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
31 6975 55 None -208 44 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
7 6975 55 None -208 44 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
CHEMBL56 6975 55 None -208 44 Human 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10.1021/jm00012a021
44376278 175883 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 6 2 3 5.1 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
CHEMBL440008 175883 0 None -2 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 472 6 2 3 5.1 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)C12CC3CC(CC(C3)C1)C2 10.1016/j.bmcl.2003.11.023
10733070 175247 0 None 37 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 301 1 0 3 3.6 CN1CCN(c2cc3c4c(cccc4n2)-c2ccccc2-3)CC1 10.1021/jm981112s
CHEMBL43512 175247 0 None 37 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 301 1 0 3 3.6 CN1CCN(c2cc3c4c(cccc4n2)-c2ccccc2-3)CC1 10.1021/jm981112s
CHEMBL5081379 221525 0 None -97 9 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CCCNCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
11727140 116170 0 None -58 4 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 326 3 2 3 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCCC4)nc23)CC1 10.1021/jm030020m
CHEMBL321967 116170 0 None -58 4 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 326 3 2 3 3.5 CN1CCC(c2c[nH]c3ccc(NC(=O)C4CCCC4)nc23)CC1 10.1021/jm030020m
21830793 98610 10 None -4265 46 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
CHEMBL2413154 98610 10 None -4265 46 Human 6.2 pKi = 6.2 Binding
Binding affinity to 5HT1B receptor (unknown origin)Binding affinity to 5HT1B receptor (unknown origin)
ChEMBL 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 10.1016/j.bmc.2013.05.050
10338821 27571 0 None -1445 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 5 0 4 3.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL130976 27571 0 None -1445 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 5 0 4 3.7 c1ccc2c(c1)CC2CCCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
44376541 172167 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
CHEMBL423789 172167 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 464 6 2 3 5.4 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
59636738 132989 0 None - 1 Chinese hamster 7.2 pKi = 7.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1ccnc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)c1 nan
CHEMBL3650032 132989 0 None - 1 Chinese hamster 7.2 pKi = 7.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1ccnc(CCN2CCN(c3cccc4cc(C(=O)N(C)C)oc34)CC2)c1 nan
11393666 199765 0 None -1698 19 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5201983 199765 0 None -1698 19 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
CHEMBL5222597 199765 0 None -1698 19 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysisDisplacement of [125I]CYP from rat brain 5HT1B receptor measured after 120 mins by scintillation counting analysis
ChEMBL 340 2 1 2 4.6 CC1(C)CN([C@@H]2C[C@@H](c3ccccc3)c3ccc(Cl)cc32)CCN1 10.1016/j.bmcl.2022.128879
283 9904 57 None -6606 12 Rat 5.2 pKi = 5.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
4847 9904 57 None -6606 12 Rat 5.2 pKi = 5.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
CHEMBL18331 9904 57 None -6606 12 Rat 5.2 pKi = 5.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 10.1021/jm00384a001
76322956 112981 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL2260927 112981 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
CHEMBL3138744 112981 0 None -1 2 Human 5.2 pKi = 5.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 233 4 1 2 3.0 CNC(C)COc1cc(Cl)ccc1Cl 10.1007/s00044-009-9164-1
9826761 118799 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL328940 118799 0 None 1 4 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1ncc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
125957 126938 8 None -1 2 Rat 7.2 pKi = 7.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
CHEMBL351530 126938 8 None -1 2 Rat 7.2 pKi = 7.2 Binding
Intrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HTIntrinsic affinity towards serotonin receptor from rat frontal cortex by displacement of [3H]5-HT
ChEMBL 256 0 1 2 2.4 FC(F)(F)c1ccc2c(c1)N1CCNCC1CC2 10.1021/jm00145a017
10432483 30037 0 None -426 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 6 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)CC2 10.1021/jm00020a020
CHEMBL133188 30037 0 None -426 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 6 3.7 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)CC2 10.1021/jm00020a020
10917920 118223 0 None -85 10 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
CHEMBL327527 118223 0 None -85 10 Human 7.2 pKi = 7.2 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 487 6 1 6 3.8 Cn1cnc(-c2ccc3c(c2)c(C2CCN(CCN4CCNC4=O)CC2)cn3-c2ccc(F)cc2)n1 10.1021/jm020938y
44376272 127007 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 6 2 3 4.8 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
CHEMBL352181 127007 0 None -7 2 Human 7.2 pKi = 7.2 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 430 6 2 3 4.8 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccccc1 10.1016/j.bmcl.2003.11.023
10130620 110426 3 None -64 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 216 2 1 2 2.5 CC(C)(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
CHEMBL308727 110426 3 None -64 2 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 216 2 1 2 2.5 CC(C)(C)c1ccc(CC2=NCCN2)cc1 10.1021/jm970513p
9998873 26338 0 None -1047 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.4 c1ccc2c(c1)CC(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL129993 26338 0 None -1047 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 0 4 3.4 c1ccc2c(c1)CC(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
72550645 120866 0 None 1 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
CHEMBL3326993 120866 0 None 1 8 Human 8.2 pKi = 8.2 Binding
Binding affinity to 5-HT1B (unknown origin)Binding affinity to 5-HT1B (unknown origin)
ChEMBL 505 11 1 4 6.0 COc1ccccc1N1CCN(CCCCCC(=O)NCc2ccccc2-c2ccccc2Cl)CC1 10.1016/j.bmc.2014.07.026
59636779 132992 0 None - 1 Chinese hamster 8.2 pKi = 8.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 446 5 0 5 3.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cccc(C(F)(F)F)n4)CC3)c2o1 nan
CHEMBL3650035 132992 0 None - 1 Chinese hamster 8.2 pKi = 8.2 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 446 5 0 5 3.9 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cccc(C(F)(F)F)n4)CC3)c2o1 nan
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
The compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor betaThe compound was tested for binding affinity against cloned human 5-hydroxytryptamine 1D receptor beta
ChEMBL 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10.1021/jm00018a020
20810 15957 22 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 202 3 2 2 1.9 CC(=O)c1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL110317 15957 22 None -5 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 202 3 2 2 1.9 CC(=O)c1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
59636713 132474 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 466 7 1 7 3.4 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
CHEMBL3647278 132474 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 466 7 1 7 3.4 N#Cc1ccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)cn1 nan
2543 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
5358 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
54 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
CHEMBL128 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
DB00669 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human 5-hydroxytryptamine 1B receptorBinding affinity towards cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/s0960-894x(03)00779-0
2543 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
5358 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
54 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
CHEMBL128 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
DB00669 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1016/j.bmcl.2003.11.023
59636722 132999 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccnc1CCN1CCN(c2cccc3cc(C(=O)N(C)C)oc23)CC1 nan
CHEMBL3650041 132999 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 408 6 0 6 2.9 COc1cccnc1CCN1CCN(c2cccc3cc(C(=O)N(C)C)oc23)CC1 nan
188006 12240 14 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 188 3 2 1 2.2 CCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
CHEMBL107511 12240 14 None -2 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor betaDisplacement of [3H]-5-HT from human 5-hydroxytryptamine 1D receptor beta
ChEMBL 188 3 2 1 2.2 CCc1ccc2[nH]cc(CCN)c2c1 10.1021/jm950498t
44402893 76584 0 None 63 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 470 4 1 5 4.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cc(C)ncc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL193616 76584 0 None 63 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 470 4 1 5 4.8 COc1cc2c(cc1N1C[C@H](C)N[C@H](C)C1)N(C(=O)c1ccc(-c3cc(C)ncc3C)cc1)CC2 10.1016/j.bmcl.2005.07.085
71458050 85792 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 6 2.5 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL2113097 85792 0 None 3 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 6 2.5 COc1cc2c(cc1N1CCN(C)CC1)N(C(=O)Cc1cccc([N+](=O)[O-])c1)CC2 10.1016/j.bmcl.2005.07.085
44402888 147310 0 None 25 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 446 3 1 4 4.6 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL381035 147310 0 None 25 2 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 446 3 1 4 4.6 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1F)CC2 10.1016/j.bmcl.2005.07.085
44402871 175376 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 462 3 1 4 5.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
CHEMBL435936 175376 0 None 10 3 Human 8.1 pKi = 8.1 Binding
Binding affinity against cloned human 5-hydroxytryptamine 1B receptorBinding affinity against cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 462 3 1 4 5.1 COc1cc2c(cc1N1C[C@H](C)N(C)[C@H](C)C1)N(C(=O)Nc1cccc(Cl)c1Cl)CC2 10.1016/j.bmcl.2005.07.085
49852105 63162 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 346 4 1 4 3.5 Cc1ccc2c(N3CCN(CCc4cccc(N)c4)CC3)cccc2n1 10.1021/jm100714c
CHEMBL1631534 63162 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5-HT1B receptor expressed in CHO cells
ChEMBL 346 4 1 4 3.5 Cc1ccc2c(N3CCN(CCc4cccc(N)c4)CC3)cccc2n1 10.1021/jm100714c
44443093 161472 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 446 6 0 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
CHEMBL399719 161472 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells
ChEMBL 446 6 0 6 3.1 Cc1ccc2c(OCCN3CCN(Cc4ccc5c(c4)N(C)C(=O)CO5)CC3)cccc2n1 10.1016/j.bmcl.2007.06.078
10288132 183796 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccncc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL462916 183796 0 None -7 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 437 7 0 4 5.9 Cc1ccc2c(OCCN3CCC(Cc4cccc(-c5ccncc5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10127877 196341 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL514429 196341 0 None -12 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 472 7 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(N5CCCN(C)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
44580741 199449 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
CHEMBL521873 199449 0 None -15 3 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 416 4 1 5 3.6 Cc1ccc2c(N3CCN(CCc4ccc5c(c4)NC(=O)CO5)[C@H](C)C3)cccc2n1 10.1016/j.bmcl.2008.08.084
75 10287 7 None -3 3 Human 8.1 pKi = 8.1 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
9870500 10287 7 None -3 3 Human 8.1 pKi = 8.1 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
CHEMBL191971 10287 7 None -3 3 Human 8.1 pKi = 8.1 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 10.1016/j.bmcl.2005.06.042
44404264 79317 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 4 1 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5C[C@H](C)N[C@H](C)C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
CHEMBL199144 79317 0 None 1 3 Human 8.1 pKi = 8.1 Binding
Mean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligandMean binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT or [3H]-8-OH-DPAT as the radioligand
ChEMBL 505 4 1 7 4.2 CCc1c(C(=O)N2CCc3cc4ccnc(N5C[C@H](C)N[C@H](C)C5)c4cc32)cnn1-c1ccc(C#N)cc1 10.1016/j.bmcl.2005.06.042
10403999 66824 0 None -27 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 324 4 1 2 5.3 CC1CCC(C)N1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL173656 66824 0 None -27 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 324 4 1 2 5.3 CC1CCC(C)N1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
10068933 110578 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
CHEMBL309021 110578 0 None -3 4 Human 7.2 pKi = 7.2 Binding
Binding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligandBinding affinity for 5-hydroxytryptamine 1B receptor in C6-glial transfected cell type using [3H]5-CT as radioligand
ChEMBL 389 8 1 4 4.5 COc1ccc(C(=O)Nc2ccc(-c3ccncc3)cc2)cc1CCCN(C)C 10.1021/jm9702948
168293874 198958 0 None -16 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
CHEMBL5204071 198958 0 None -16 11 Human 7.2 pKi = 7.2 Binding
Binding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constantBinding affinity to 5HT1B receptor (unknown origin) assessed as inhibition constant
ChEMBL 312 2 3 3 3.3 COc1ccc(C2NCCc3c2[nH]c2ccc(F)cc32)c(O)c1 10.1021/acsmedchemlett.1c00694
73350823 109307 0 None -45 9 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL2424668 109307 0 None -45 9 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
CHEMBL3040578 109307 0 None -45 9 Human 6.2 pKi = 6.2 Binding
Binding affinity to human 5HT1B receptor by competitive binding assayBinding affinity to human 5HT1B receptor by competitive binding assay
ChEMBL 509 8 1 5 3.7 O=C(Cc1ccc(OC2CCNCC2)cc1OCCF)N1CCC(N2C(=O)CCc3ccccc32)CC1 10.1016/j.bmcl.2013.07.045
10068239 29243 0 None -257 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 4 0 4 4.1 c1ccc2c(c1)CCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL132514 29243 0 None -257 2 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 378 4 0 4 4.1 c1ccc2c(c1)CCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
10091445 125263 0 None -316 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 384 4 0 4 4.0 Clc1cccc2c1CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL341390 125263 0 None -316 3 Rat 6.2 pKi = 6.2 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 384 4 0 4 4.0 Clc1cccc2c1CC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
73213195 111236 0 None -24 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 111236 0 None -24 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
76312088 112988 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
CHEMBL2260929 112988 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
CHEMBL3138771 112988 0 None 3 2 Human 7.2 pKi = 7.2 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 321 4 1 2 3.2 CNC(C)COc1c(Br)cccc1Br 10.1007/s00044-009-9164-1
9816035 210912 1 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 2 1 2 2.8 Cc1cc(C(C)(C)C)ccc1CC1=NCCN1 10.1021/jm970513p
CHEMBL70409 210912 1 None -104 2 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
ChEMBL 230 2 1 2 2.8 Cc1cc(C(C)(C)C)ccc1CC1=NCCN1 10.1021/jm970513p
71457690 90573 0 None -6 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
CHEMBL2205817 90573 0 None -6 5 Human 5.2 pKi = 5.2 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1cccnc1 10.1016/j.bmcl.2012.08.046
10266598 127149 1 None -37 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 296 4 1 2 4.5 c1csc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)c1 10.1016/s0960-894x(00)00133-5
CHEMBL353256 127149 1 None -37 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 296 4 1 2 4.5 c1csc(-c2ccc3[nH]cc(CCN4CCCC4)c3c2)c1 10.1016/s0960-894x(00)00133-5
73213195 111236 0 None -24 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
CHEMBL3104092 111236 0 None -24 12 Human 6.2 pKi = 6.2 Binding
Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)Displacement of [3H]5-CT from 5-HT1B receptor (unknown origin)
ChEMBL 288 0 0 2 3.6 CN1CCc2c(c3cccc4c3n2Cc2ccccc2C4)C1 10.1016/j.bmcl.2013.12.024
9947817 11819 0 None -131 9 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL105261 11819 0 None -131 9 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 286 3 2 3 2.7 CCC(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
9863333 211144 0 None -5128 9 Western lowland gorilla 5.1 pKi = 5.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
CHEMBL71724 211144 0 None -5128 9 Western lowland gorilla 5.1 pKi = 5.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
ChEMBL 352 5 0 4 3.5 COc1ccc(N2CCN(CCC3OCCc4ccccc43)CC2)cc1 10.1021/jm980137o
899056 69840 4 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@H](C)N)c[nH]c2c1 10.1021/jm00402a026
CHEMBL1788282 69840 4 None - 1 Rat 5.1 pKi = 5.1 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1ccc2c(C[C@H](C)N)c[nH]c2c1 10.1021/jm00402a026
44461443 212132 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 414 5 1 3 4.8 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
CHEMBL79693 212132 0 None -5 3 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 414 5 1 3 4.8 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2cccc3ccccc23)CC1 10.1016/j.bmcl.2004.03.003
66847540 132991 0 None - 1 Chinese hamster 7.1 pKi = 7.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 403 5 0 6 2.8 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cc(C#N)ccn4)CC3)c2o1 nan
CHEMBL3650034 132991 0 None - 1 Chinese hamster 7.1 pKi = 7.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 403 5 0 6 2.8 CN(C)C(=O)c1cc2cccc(N3CCN(CCc4cc(C#N)ccn4)CC3)c2o1 nan
14975318 84018 0 None -144 2 Rat 5.1 pKi = 5.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL2079596 84018 0 None -144 2 Rat 5.1 pKi = 5.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL5074190 221093 0 None -29 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None COc1ccccc1-c1cc(CCN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
70530 103732 104 None -2 3 Rat 7.1 pKi = 7.1 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL266250 103732 104 None -2 3 Rat 7.1 pKi = 7.1 Binding
Binding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptorBinding affinity determined in radioreceptor binding assay by using [3H]5-HT radioligand against 5-hydroxytryptamine 1B receptor
ChEMBL 178 1 2 3 0.8 Oc1ccccc1N1CCNCC1 10.1021/jm00125a020
50878551 97520 61 None -7 18 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL2391541 97520 61 None -7 18 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 270 8 1 2 3.4 C=CCN(CC=C)CCc1c[nH]c2ccc(OC)cc12 10.1016/j.bmcl.2015.12.053
1355 8792 88 None -1 16 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
142 8792 88 None -1 16 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
CHEMBL478 8792 88 None -1 16 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
DB12110 8792 88 None -1 16 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 196 1 1 2 1.8 Clc1cccc(c1)N1CCNCC1 10.1021/jm00384a001
15724480 126357 0 None -117 3 Rat 7.1 pKi = 7.1 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 452 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL346168 126357 0 None -117 3 Rat 7.1 pKi = 7.1 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 452 7 0 5 4.4 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCCCC3=O)n2C)CC1 10.1021/jm00081a018
11111280 115975 0 None -38 3 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 2 4 3.6 COc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
CHEMBL321562 115975 0 None -38 3 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 364 4 2 4 3.6 COc1ccccc1C(=O)Nc1ccc2[nH]cc(C3CCN(C)CC3)c2n1 10.1021/jm030020m
76322958 113001 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
CHEMBL2260930 113001 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
CHEMBL3138809 113001 0 None -1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 257 6 1 3 3.5 CNC(C)COc1cccc(Oc2ccccc2)c1 10.1007/s00044-009-9164-1
86221574 173466 2 None -95 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
CHEMBL4282117 173466 2 None -95 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 375 5 2 2 3.4 O=C(NCCc1c[nH]c2ccccc12)C1CCN(C(=O)c2ccccc2)CC1 10.1039/C8MD00204E
11145333 171374 0 None -6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
CHEMBL421573 171374 0 None -6 4 Human 7.1 pKi = 7.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
ChEMBL 484 6 1 5 4.4 O=C1NCCN1CCN1CCC(c2cn(-c3ccc(F)cc3)c3ccc(-c4ncccn4)cc23)CC1 10.1021/jm020938y
10513501 109396 0 None 14 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1cc2ccccc2c2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
CHEMBL304210 109396 0 None 14 2 Rat 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 227 1 1 2 2.7 COc1cc2ccccc2c2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
44376362 171675 0 None -10 2 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 4 2 2 3.2 C1=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CCNC1 10.1016/j.bmcl.2003.11.023
CHEMBL422192 171675 0 None -10 2 Human 6.1 pKi = 6.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 4 2 2 3.2 C1=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CCNC1 10.1016/j.bmcl.2003.11.023
44286629 174927 0 None -245 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 437 5 0 5 5.0 CN1CCN(c2nc3ccccc3c(-c3ccccc3)c2COC(=O)c2ccccc2)CC1 10.1021/jm981112s
CHEMBL43304 174927 0 None -245 3 Rat 5.1 pKi = 5.1 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor of rat striatumBinding affinity against 5-hydroxytryptamine 1B receptor of rat striatum
ChEMBL 437 5 0 5 5.0 CN1CCN(c2nc3ccccc3c(-c3ccccc3)c2COC(=O)c2ccccc2)CC1 10.1021/jm981112s
9845181 214940 3 None -5495 13 Human 5.1 pKi = 5.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
CHEMBL98241 214940 3 None -5495 13 Human 5.1 pKi = 5.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor receptor
ChEMBL 423 4 0 4 3.3 C[C@H](CN1CCN(c2cc(F)c(F)cc2F)CC1)N1C(=O)CC2(CCCC2)CC1=O 10.1021/jm020938y
21048816 82275 0 None -1096 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cells
ChEMBL 385 7 0 3 4.9 CC(C)(CCCN1CCCC(c2ccccc2)C1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.11.067
CHEMBL204269 82275 0 None -1096 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from the cloned human 5-HT1B receptor expressed in CHO cells
ChEMBL 385 7 0 3 4.9 CC(C)(CCCN1CCCC(c2ccccc2)C1)S(=O)(=O)c1ccccc1 10.1016/j.bmcl.2005.11.067
10023444 123482 0 None -117 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 392 4 0 4 4.5 c1ccc2c(c1)CCCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
CHEMBL337279 123482 0 None -117 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 392 4 0 4 4.5 c1ccc2c(c1)CCCCC2CCN1CCN(c2cccc3c2OCCO3)CC1 10.1021/jm00020a020
14083210 67096 2 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@@H](C)N)c12 10.1021/jm00402a026
CHEMBL1744072 67096 2 None - 1 Rat 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenateDisplacement of [3H]5-HT from 5-HT1B receptor of rat frontal cortex homogenate
ChEMBL 204 3 2 2 2.1 COc1cccc2[nH]cc(C[C@@H](C)N)c12 10.1021/jm00402a026
44581973 182380 0 None -363 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
CHEMBL458002 182380 0 None -363 10 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5HT from 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from 5HT1B receptor expressed in CHO cells
ChEMBL 513 6 2 6 4.6 Cc1ccc(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cc1NC(=O)c1ccc(-c2ccccc2)cc1 10.1021/jm800962k
71061724 152330 0 None -7 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
CHEMBL3915107 152330 0 None -7 5 Mouse 5.1 pKi = 5.1 Binding
Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.Radioligand Binding Assay: The detailed experimental protocols for the radioligand and functional receptor assays are available on the NIMH PDSP website at http://pdsp.med.unc.edu/UNC-CH %20Protocol %20Book.pdf. A. Serotonin receptors: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT3, 5-HT5A, 5-HT6 and 5-HT7. Assay Buffer: Standard Binding Buffer (50 mM Tris-HCl, 10 mM MgCl2, 1 mM EDTA, pH 7.4) Membrane Fraction Source: Transiently or stably transfected cell lines (e.g., HEK293, COS, CHO, NIH3T3). Protocol adapted from Roth et al. (1986), J. Pharmacol. Exp. Ther., 238(2): 480-485; and Roth et al. (1994), J. Pharmacol. Exp. Ther., 268(3): 1403-1410. Adrenergic Receptors: alpha1A, alpha1B, alpha2A, alpha2B, alpha2C, beta1, beta2, beta3 Assay Buffers: For alpha1 receptors, alpha1 Binding Buffer (20 mM Tris-HCl, 145 mM NaCl, pH 7.4); for alpha2 receptors, alpha2 Binding Buffer (50 mM Tris-HCl, 5 mM MgCl2, pH 7.7); for beta receptors.
ChEMBL 386 5 0 4 3.0 O=C(CN1CCO[C@H](COc2cccc(Cl)c2)C1)N1CCc2ccccc21 nan
10356544 210770 0 None -61 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 284 5 1 1 4.5 CCCN(CCC)C1CCc2ccc3[nH]cc(C)c3c2C1 10.1021/jm00012a021
CHEMBL69562 210770 0 None -61 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 284 5 1 1 4.5 CCCN(CCC)C1CCc2ccc3[nH]cc(C)c3c2C1 10.1021/jm00012a021
24882193 195428 0 None -263 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
CHEMBL503468 195428 0 None -263 2 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 10.1021/jm7011722
11270107 75021 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 420 7 0 6 4.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(C)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
CHEMBL191605 75021 0 None -39 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 420 7 0 6 4.0 Cc1ccc2c(OCCN3CCN(Cc4ccc(C)c([N+](=O)[O-])c4)CC3)cccc2n1 10.1021/jm049039v
44581235 183795 0 None -25 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 521 8 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(S(C)(=O)=O)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
CHEMBL462915 183795 0 None -25 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5HT from human 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5HT from human 5HT1B receptor expressed in CHO cells
ChEMBL 521 8 0 5 5.0 Cc1ccc2c(OCCN3CCC(Cc4cccc(C5CCN(S(C)(=O)=O)CC5)c4)CC3)cccc2n1 10.1016/j.bmcl.2008.11.052
10341516 122300 0 None -251 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 410 6 0 6 3.3 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
CHEMBL335297 122300 0 None -251 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 410 6 0 6 3.3 COc1cc2c(cc1OC)C(CCN1CCN(c3cccc4c3OCCO4)CC1)C2 10.1021/jm00020a020
276 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
5312149 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
CHEMBL431298 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1021/jm980532e
6918648 108336 1 None -1288 14 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
CHEMBL29846 108336 1 None -1288 14 Human 6.1 pKi = 6.1 Binding
Compound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HTCompound was tested for its binding affinity against human cloned 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1021/jm980532e
10161027 98751 0 None -39 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2006.11.031
CHEMBL241499 98751 0 None -39 3 Human 6.1 pKi = 6.1 Binding
Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cellsDisplacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells
ChEMBL 449 6 1 5 4.3 Cc1ccc2c(OCCN3CCC(Cc4ccc5c(c4)NC(=O)CO5)CC3)ccc(F)c2n1 10.1016/j.bmcl.2006.11.031
276 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
5312149 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
CHEMBL431298 10286 50 None -537 13 Human 6.1 pKi = 6.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 451 5 2 6 4.1 COc1ccc(cc1N1CCNCC1)NS(=O)(=O)c1sc2c(c1C)cc(cc2)Cl 10.1016/s0960-894x(02)00172-5
6918648 108336 1 None -1288 14 Human 6.1 pKi = 6.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
CHEMBL29846 108336 1 None -1288 14 Human 6.1 pKi = 6.1 Binding
The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligandThe compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand
ChEMBL 465 5 1 6 4.4 COc1ccc(NS(=O)(=O)c2sc3ccc(Cl)cc3c2C)cc1N1CCN(C)CC1 10.1016/s0960-894x(02)00172-5
19066205 18154 0 None 8 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
CHEMBL108722 18154 0 None 8 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
CHEMBL1179986 18154 0 None 8 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1cccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)c1 10.1016/S0960-894X(97)10164-0
2543 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
5358 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
54 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
CHEMBL128 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
DB00669 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 nan
2736460 214315 57 None 2 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 190 2 1 2 1.7 CCc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9467 214315 57 None 2 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 190 2 1 2 1.7 CCc1ccccc1N1CCNCC1 10.1021/jm00125a020
59636734 133001 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cc(F)cc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
CHEMBL3650043 133001 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 396 5 0 5 3.0 CN(C)C(=O)c1cc2cc(F)cc(N3CCN(CCc4ccccn4)CC3)c2o1 nan
19066200 18153 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
CHEMBL108645 18153 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
CHEMBL1179985 18153 0 None 27 3 Human 8.1 pKi = 8.1 Binding
Affinity for 5-hydroxytryptamine 1B receptor subtypeAffinity for 5-hydroxytryptamine 1B receptor subtype
ChEMBL 439 5 1 6 2.8 COc1ccc(N2CCN(C(=O)Nc3ccc(OC)c(N4CCN(C)CC4)c3)CC2)cc1 10.1016/S0960-894X(97)10164-0
14479835 215106 1 None 2 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 218 4 1 2 2.4 CCCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
CHEMBL9921 215106 1 None 2 3 Rat 8.1 pKi = 8.1 Binding
Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.Binding affinity at rat 5-hydroxytryptamine 1B receptor by [3H]5-HT displacement.
ChEMBL 218 4 1 2 2.4 CCCCc1ccccc1N1CCNCC1 10.1021/jm00125a020
2176 9901 68 None -741 27 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
4828 9901 68 None -741 27 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
91 9901 68 None -741 27 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
CHEMBL500 9901 68 None -741 27 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
DB00960 9901 68 None -741 27 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C 10.1021/jm00384a001
10904295 11481 0 None -6 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1021/jm030020m
CHEMBL103503 11481 0 None -6 4 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 352 3 2 3 3.8 CN1CCC(c2c[nH]c3cnc(NC(=O)c4ccc(F)cc4)cc23)CC1 10.1021/jm030020m
52899 104029 34 None -8 5 Rat 6.1 pKi = 6.1 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm00164a046
CHEMBL268800 104029 34 None -8 5 Rat 6.1 pKi = 6.1 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 204 3 2 2 2.0 COc1ccc2[nH]c(C)c(CCN)c2c1 10.1021/jm00164a046
10220230 114199 2 None -7 3 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 2 3 2.0 CN1CCC(c2c[nH]c3ccc(N)nc23)CC1 10.1021/jm030020m
CHEMBL318105 114199 2 None -7 3 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 230 1 2 3 2.0 CN1CCC(c2c[nH]c3ccc(N)nc23)CC1 10.1021/jm030020m
14975320 84020 0 None -478 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
CHEMBL2079598 84020 0 None -478 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 424 6 0 4 4.1 COc1cccc2c1[C@@H]1CCN(CCCCN3C(=O)CC4(CCCC4)CC3=O)C[C@H]1C2 10.1021/jm00027a013
2914436 169169 3 None -10 2 Rat 5.1 pKi = 5.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 301 9 1 3 3.7 CCCN(CCC)CC(O)COc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL416564 169169 3 None -10 2 Rat 5.1 pKi = 5.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 301 9 1 3 3.7 CCCN(CCC)CC(O)COc1cccc2ccccc12 10.1021/jm00124a021
11723305 176044 0 None -162 4 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL441256 176044 0 None -162 4 Human 7.1 pKi = 7.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 316 6 1 2 4.1 CCCN(CCC)C1CCc2cc(F)c3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
44376263 63007 0 None -13 2 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 6 2 3 4.9 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
CHEMBL162724 63007 0 None -13 2 Human 7.1 pKi = 7.1 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 448 6 2 3 4.9 O=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1ccc(Cl)cc1 10.1016/j.bmcl.2003.11.023
59636752 132460 0 None - 1 Chinese hamster 7.1 pKi = 7.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 475 6 1 6 2.9 CC(=O)N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
CHEMBL3647264 132460 0 None - 1 Chinese hamster 7.1 pKi = 7.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 475 6 1 6 2.9 CC(=O)N1CCC(NC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)CC1 nan
49783209 24381 0 None -1412 26 Human 6.1 pKi = 6.1 Binding
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
CHEMBL1258223 24381 0 None -1412 26 Human 6.1 pKi = 6.1 Binding
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 396 7 1 6 3.8 CCCCN1CCC(COC(=O)c2cc(Cl)c(NC)c3c2OCCO3)CC1 10.1021/jm100668r
11067619 11907 0 None -112 4 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 334 3 2 3 3.6 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccc4)nc23)CC1 10.1021/jm030020m
CHEMBL105743 11907 0 None -112 4 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 334 3 2 3 3.6 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccccc4)nc23)CC1 10.1021/jm030020m
151 9194 44 None -89 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
20 9194 44 None -89 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
5311258 9194 44 None -89 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
CHEMBL101690 9194 44 None -89 4 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F 10.1021/jm7011722
134138168 154469 0 None -75 10 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
CHEMBL3931889 154469 0 None -75 10 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL 275 4 0 2 4.1 COc1ccccc1-c1cc(CN(C)C)ccc1Cl 10.1021/acs.jmedchem.1c00110
213 10625 55 None -6 43 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
2717 10625 55 None -6 43 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
5533 10625 55 None -6 43 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
CHEMBL621 10625 55 None -6 43 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
DB00656 10625 55 None -6 43 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 nan
76326516 113006 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL2260933 113006 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL3138820 113006 0 None 1 2 Human 6.1 pKi = 6.1 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL5091373 222346 0 None -39 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
CHEMBL5095981 222346 0 None -39 9 Human 7.1 pKi = 7.1 Binding
Binding affinity to 5-HT1BR (unknown origin)Binding affinity to 5-HT1BR (unknown origin)
ChEMBL None None None CNCCc1ccc(Cl)c(-c2ccccc2OC)c1 10.1021/acs.jmedchem.1c00110
122483223 144887 0 None -11 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3764650 144887 0 None -11 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
CHEMBL3765874 144887 0 None -11 7 Human 6.1 pKi = 6.1 Binding
Binding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assayBinding affinity to recombinant 5-HT1B receptor (unknown origin) after 1.5 hrs by radioligand displacement assay
ChEMBL 455 8 0 5 5.8 COc1ccccc1N1CCN(CCCCCC(=O)n2c3ccccc3c3ccccc32)CC1 10.1016/j.ejmech.2016.01.043
44269068 105230 0 None -954 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 0 5 2.9 COc1cccc2c1C1CCN(CCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
CHEMBL275773 105230 0 None -954 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 426 5 0 5 2.9 COc1cccc2c1C1CCN(CCCN3C(=O)c4ccccc4S3(=O)=O)CC1C2 10.1021/jm00027a013
2351 10059 64 None -10 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
2820 10059 64 None -10 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
5035 10059 64 None -10 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
CHEMBL81 10059 64 None -10 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
DB00481 10059 64 None -10 21 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O nan
152 7152 29 None -57 19 Rat 7.1 pKi = 7.1 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
2107 7152 29 None -57 19 Rat 7.1 pKi = 7.1 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
CHEMBL275854 7152 29 None -57 19 Rat 7.1 pKi = 7.1 Binding
Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.Binding affinity was determined against 5-hydroxytryptamine 1B receptor was determined in male Sprague-Dawley rat brain.
ChEMBL 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N 10.1021/jm00164a046
9910257 173451 0 None -87 3 Rat 7.1 pKi = 7.1 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 424 7 0 5 3.6 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
CHEMBL428175 173451 0 None -87 3 Rat 7.1 pKi = 7.1 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 424 7 0 5 3.6 CC(C)Oc1ccccc1N1CCN(Cc2ccc(CN3CCCCC3=O)n2C)CC1 10.1021/jm00081a018
9997422 211055 0 None -50 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
CHEMBL71247 211055 0 None -50 4 Human 6.1 pKi = 6.1 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 341 7 2 3 2.8 CCCN(CCC)[C@@H]1CCc2ccc3[nH]cc(C(=O)C(N)=O)c3c2C1 10.1021/jm00012a021
41305446 174031 1 None -15 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
CHEMBL4292719 174031 1 None -15 5 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting methodDisplacement of [3H]GR127543 from human 5HT1B receptor expressed in HEK cell membranes after 1.5 hrs by liquid scintillation counting method
ChEMBL 398 5 1 2 4.5 O=C(NCc1ccccc1)C1CCN(C(=O)c2ccc(-c3ccccc3)cc2)CC1 10.1039/C8MD00204E
1212 8443 50 None -144 65 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
204 8443 50 None -144 65 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
3372 8443 50 None -144 65 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
CHEMBL726 8443 50 None -144 65 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
DB00623 8443 50 None -144 65 Rat 6.1 pKi = 6.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F nan
122197405 140254 0 None -47 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL3706925 140254 0 None -47 3 Human 7.1 pKi = 7.1 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 440 5 1 5 4.0 C[C@H]1CN(c2cccc3cc(C#N)ccc23)CCN1CC[C@H]1OCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
11223004 208993 0 None -28 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
CHEMBL609742 208993 0 None -28 5 Human 7.1 pKi = 7.1 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 389 5 3 3 3.9 O=S(=O)(Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1)c1ccccc1Cl 10.1021/jm049243i
130442480 182049 0 None -107 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
CHEMBL4572614 182049 0 None -107 24 Human 5.1 pKi = 5.1 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 410 3 0 6 5.7 Cc1ncc2nccn2c1-c1ccc(Oc2nccc3occc23)cc1C(F)(F)F 10.1021/acs.jmedchem.9b00351
44582675 196480 0 None -15 15 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
CHEMBL515472 196480 0 None -15 15 Human 6.1 pKi = 6.1 Binding
Inhibition of human cloned 5HT1B receptor by competitive binding experimentInhibition of human cloned 5HT1B receptor by competitive binding experiment
ChEMBL 405 9 1 4 4.2 COc1c(OCCF)cccc1[C@H](O)C1CCN(CCc2ccc(F)cc2)CC1 10.1016/j.bmc.2009.03.021
9907305 36967 0 None -1513 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 368 5 1 3 3.2 COc1cccc2c1C1CCN(CCNC(=O)c3ccc(F)cc3)CC1C2 10.1021/jm00027a013
CHEMBL13904 36967 0 None -1513 2 Rat 6.1 pKi = 6.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 368 5 1 3 3.2 COc1cccc2c1C1CCN(CCNC(=O)c3ccc(F)cc3)CC1C2 10.1021/jm00027a013
90469115 192621 4 None -295 17 Human 6.1 pKi = 6.1 Binding
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
CHEMBL4867565 192621 4 None -295 17 Human 6.1 pKi = 6.1 Binding
Binding affinity to human 5-HT1B receptorBinding affinity to human 5-HT1B receptor
ChEMBL 410 3 1 6 3.0 O=S(=O)(c1cccc(F)c1)n1ccc2c(N3CCNCC3)nc3ccccc3c21 10.1021/acs.jmedchem.1c00224
64622 103629 6 None -2238 5 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 425 8 1 4 3.9 COc1ccccc1N1CCN(CCCCNC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm00112a043
CHEMBL26533 103629 6 None -2238 5 Rat 6.1 pKi = 6.1 Binding
Binding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligandBinding affinity towards 5-hydroxytryptamine 1B receptor using [3H]5-HT as radioligand
ChEMBL 425 8 1 4 3.9 COc1ccccc1N1CCN(CCCCNC(=O)C23C[C@H]4C[C@@H](C2)C[C@@H](C3)C4)CC1 10.1021/jm00112a043
127036932 144126 0 None -29 22 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3752900 144126 0 None -29 22 Human 6.1 pKi = 6.1 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 274 7 1 1 4.0 C=CCN(CC=C)CCc1c[nH]c2ccc(Cl)cc12 10.1016/j.bmcl.2015.12.053
59636704 132461 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 1 6 4.1 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccccn1 nan
CHEMBL3647265 132461 0 None - 1 Chinese hamster 8.1 pKi = 8.1 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 455 7 1 6 4.1 CC(NC(=O)c1cc2cccc(N3CCN(CCc4ccccn4)CC3)c2o1)c1ccccn1 nan
2543 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
5358 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
54 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
CHEMBL128 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
DB00669 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation countingDisplacement of [3H]5-hydroxytryptamine from human cloned 5HT1B receptor expressed in CHOK1 cells by liquid scintillation counting
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm7011722
59636741 132476 0 None - 1 Chinese hamster 8.0 pKi = 8.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
CHEMBL3647280 132476 0 None - 1 Chinese hamster 8.0 pKi = 8.0 Binding
Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.Inhibition Assay: Assays that were used to measure affinity of the compounds of the present invention for 5-HT1A and 5-HT1B receptors are described in J. Recept Signal Transduct. Res. 22:483-495 (2002) and Naunyn-Schmiedeberg's Arch Pharmacol. 356:328-334 (1997) and incorporated by reference herein. These assays were be used with some modifications:For the binding assay stably transfected chinese hamster ovary (CHO) cell lines expressing 5-HT1A receptors or 5-HT1B receptors were harvested by centrifugation at 300x g for 10 min and resuspended in 10 mM Tris-HCl, 5 mM EDTA at pH 7.4. The cells were pooled, recentrifuged and resuspended before homogenisation using a Dounce homogeniser ("type B"). Cell membranes were centrifuged at 48 000x g for 10 min and then resuspended in harvesting buffer using an Ultra-Turrax T8 (IKA Labortechnik, Germany), aliquots were stored frozen in -70 C.Frozen membrane preparations were thawed, homogenized with an Ultra-Turrax and mixed with SPA beads.
ChEMBL 465 7 1 6 4.0 N#Cc1cccc(CNC(=O)c2cc3cccc(N4CCN(CCc5ccccn5)CC4)c3o2)c1 nan
150 9287 21 None -6 16 Rat 8.0 pKi = 8.0 Binding
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 9287 21 None -6 16 Rat 8.0 pKi = 8.0 Binding
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 9287 21 None -6 16 Rat 8.0 pKi = 8.0 Binding
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 9287 21 None -6 16 Rat 8.0 pKi = 8.0 Binding
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 9287 21 None -6 16 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO nan
46232642 207613 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
CHEMBL601012 207613 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
23533306 91956 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 465 4 2 6 2.5 CN1CCN(c2cc(F)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)CC1 10.1016/j.bmc.2006.10.037
CHEMBL225363 91956 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cellsDisplacement of [3H]GR125743 from 5HT1B receptor transfected in CHO cells
ChEMBL 465 4 2 6 2.5 CN1CCN(c2cc(F)cc3c(=O)cc(C(=O)Nc4ccc(N5CCOCC5)cc4)[nH]c23)CC1 10.1016/j.bmc.2006.10.037
71459954 85957 0 None -9 7 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
CHEMBL2113386 85957 0 None -9 7 Human 8.0 pKi = 8.0 Binding
Inhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cellsInhibition of [3H]-8-OH-DPAT binding to human 5-hydroxytryptamine 1B receptor expressed in CHO cells
ChEMBL 495 6 3 3 4.0 O=S(=O)(Cc1ccccc1I)Nc1ccc2[nH]cc(C[C@H]3CCCN3)c2c1 10.1021/jm049243i
46232642 207613 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
CHEMBL601012 207613 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to 5HT1B receptor expressed in CHO cellsBinding affinity to 5HT1B receptor expressed in CHO cells
ChEMBL 457 4 3 5 3.9 Cc1n[nH]c(C)c1-c1ccc(C)c2c(=O)cc(C(=O)Nc3ccc(N4CCOCC4)cc3)[nH]c12 10.1021/jm901200t
2543 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805945
5358 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805945
54 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805945
CHEMBL128 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805945
DB00669 10479 68 None -3 32 Human 8.0 pKi = 8.0 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm9805945
44403106 78190 0 None 1 4 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 438 6 1 6 3.3 COc1ccccc1N1CCC(C(=O)Nc2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.bmcl.2005.07.024
CHEMBL195927 78190 0 None 1 4 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligandIn vitro binding affinity towards cloned human 5-HT1B receptor using [3H]5-carboximidotryptamine as radioligand
ChEMBL 438 6 1 6 3.3 COc1ccccc1N1CCC(C(=O)Nc2ccc(OC)c(N3CCN(C)CC3)c2)CC1 10.1016/j.bmcl.2005.07.024
44383737 139299 0 None -5 2 Human 8.0 pKi = 8 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 340 6 1 3 4.6 COC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
CHEMBL369798 139299 0 None -5 2 Human 8.0 pKi = 8 Binding
Binding affinity for human 5-hydroxytryptamine 1B receptorBinding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 340 6 1 3 4.6 COC[C@@H]1CCCN1CCc1c[nH]c2ccc(-c3cccs3)cc12 10.1016/s0960-894x(00)00133-5
145 6928 49 None -47 30 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
1832 6928 49 None -47 30 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
CHEMBL7257 6928 49 None -47 30 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
DB14010 6928 49 None -47 30 Rat 7.1 pKi = 7.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 10.1021/jm00384a001
14519863 121979 1 None -58 3 Rat 5.1 pKi = 5.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm00124a021
CHEMBL334465 121979 1 None -58 3 Rat 5.1 pKi = 5.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
ChEMBL 299 10 0 2 5.1 CCCCN(CCCC)CCOc1cccc2ccccc12 10.1021/jm00124a021
10197933 103808 39 None -7 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 177 1 1 2 1.5 COc1cccc2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
CHEMBL26688 103808 39 None -7 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in rat striatal membranes using [3H]5-HT as radioligand
ChEMBL 177 1 1 2 1.5 COc1cccc2c1CC(N)CC2 10.1016/S0960-894X(01)81009-X
44431533 94801 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
CHEMBL234448 94801 0 None -1 4 Human 7.0 pKi = 7.0 Binding
Displacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cellsDisplacement of [3H]GR-125743 from human 5HT1B expressed in LM(tk-) cells
ChEMBL 447 5 1 4 4.3 C[C@@H]1CN(c2cccc3cc(F)ccc23)CCN1CC[C@H]1OCCc2cc(C(N)=O)ccc21 10.1016/j.bmcl.2007.03.101
10257 7525 31 None -141 19 Rat 6.0 pKi = 6.0 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
144 7525 31 None -141 19 Rat 6.0 pKi = 6.0 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
CHEMBL416526 7525 31 None -141 19 Rat 6.0 pKi = 6.0 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
DB01445 7525 31 None -141 19 Rat 6.0 pKi = 6.0 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
ChEMBL 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C 10.1021/jm00384a001
11747350 114109 0 None -45 10 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
CHEMBL317535 114109 0 None -45 10 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligandBinding affinity against 5-hydroxytryptamine 1B receptor in CHO cells using [3H]5-HT as radioligand
ChEMBL 260 5 1 3 2.4 CCOC(=O)c1[nH]c2ccccc2c1CCN(C)C 10.1021/jm010943m
76312090 113026 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL2260934 113026 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
CHEMBL3138934 113026 0 None 6 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assayBinding affinity to Homo sapiens (human) 5HT1B receptor by radioligand binding assay
ChEMBL 364 5 0 3 4.4 CN1CCN([C@H](COc2cccc(Cl)c2Cl)c2ccccc2)CC1 10.1007/s00044-009-9164-1
9996017 28018 0 None -114 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 318 3 0 3 3.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
CHEMBL131324 28018 0 None -114 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 318 3 0 3 3.9 c1ccc2c(c1)CC2CN1CCN(c2cccc3ccoc23)CC1 10.1021/jm00020a020
6918542 211703 24 None -2238 10 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptorCompound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
CHEMBL76237 211703 24 None -2238 10 Human 5.0 pKi = 5.0 Binding
Compound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptorCompound was evaluated for its binding affinity for human 5-hydroxytryptamine 1B receptor
ChEMBL 358 6 0 5 3.0 COc1ccc2c(c1)c(CCN(C)C)cn2S(=O)(=O)c1ccccc1 10.1016/s0960-894x(00)00453-4
11120893 11294 0 None -204 4 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccoc4)nc23)CC1 10.1021/jm030020m
CHEMBL102250 11294 0 None -204 4 Human 6.0 pKi = 6.0 Binding
In vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptorIn vitro binding affinity by radioligand binding assay using cell line expressing human 5-hydroxytryptamine 1B receptor
ChEMBL 324 3 2 4 3.2 CN1CCC(c2c[nH]c3ccc(NC(=O)c4ccoc4)nc23)CC1 10.1021/jm030020m
75201901 173204 19 None -691 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4277264 173204 19 None -691 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 356 3 0 6 4.9 Cc1cc(Oc2nccc3occc23)ccc1-c1c(C)ncc2nccn12 10.1021/acs.jmedchem.9b00351
130442572 178687 0 None -199 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4469848 178687 0 None -199 24 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 395 3 0 5 6.0 FC(F)(F)c1cc(Oc2nccc3occc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10361292 123434 0 None -1737 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)Cc2ccccc21 10.1021/jm00020a020
CHEMBL337036 123434 0 None -1737 2 Rat 6.0 pKi = 6.0 Binding
Binding affinity at 5-hydroxytryptamine 1B receptorBinding affinity at 5-hydroxytryptamine 1B receptor
ChEMBL 362 4 0 4 3.6 C1=C(CCN2CCN(c3cccc4c3OCCO4)CC2)Cc2ccccc21 10.1021/jm00020a020
4189 213701 96 None -41 34 Rat 5.0 pKi = 5.0 Binding
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 213701 96 None -41 34 Rat 5.0 pKi = 5.0 Binding
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 213701 96 None -41 34 Rat 5.0 pKi = 5.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 nan
9948210 109898 1 None -1479 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL307786 109898 1 None -1479 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 298 6 1 2 4.0 CCCN(CCC)[C@H]1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a021
CHEMBL4777443 220825 0 None -45 14 Human 6.0 pKi = 6.0 Binding
Selectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR1BSelectivity interaction (GPCR panel (PDSP screen)) EUB0000741a HTR1B
ChEMBL None None None CC(C)(C)OC(=O)N1CCCC1CN[C@H]1CC[C@@](c2cc(F)ccc2F)(S(=O)(=O)c2ccc(Cl)cc2)CC1 10.6019/CHEMBL5212743
10401862 109448 1 None -257 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
CHEMBL304573 109448 1 None -257 4 Human 6.0 pKi = 6.0 Binding
Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.Binding affinity against 5-hydroxytryptamine 1D receptor beta expressed in CHO-K1 cells, using [3H]5-HT as the radioligand.
ChEMBL 288 5 1 1 4.3 CCCN(CCC)[C@H]1CCc2cc(F)c3[nH]ccc3c2C1 10.1021/jm00012a021
44376363 62126 0 None -6 2 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
CHEMBL161894 62126 0 None -6 2 Human 7.0 pKi = 7.0 Binding
Binding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptorBinding affinity was evaluated at the cloned human 5-hydroxytryptamine 1B receptor
ChEMBL 480 6 2 3 5.9 S=C(NN1CC=C(c2ccc3[nH]cc(CCN4CCCC4)c3c2)CC1)c1cccc2ccccc12 10.1016/j.bmcl.2003.11.023
15724503 52971 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 400 5 0 4 3.5 Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)ccc1CN1CCCCC1=O 10.1021/jm00081a018
CHEMBL153451 52971 0 None -2 3 Rat 7.0 pKi = 7.0 Binding
The compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortexThe compound was tested for its binding affinity towards 5-hydroxytryptamine 1B receptor by displacing [3H]serotonin radioligand in rat cerebral cortex
ChEMBL 400 5 0 4 3.5 Cn1c(CN2CCN(c3cccc(Cl)c3)CC2)ccc1CN1CCCCC1=O 10.1021/jm00081a018
127036953 144293 0 None -95 22 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
CHEMBL3754166 144293 0 None -95 22 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT 1B (unknown origin) by competition binding assayBinding affinity to 5-HT 1B (unknown origin) by competition binding assay
ChEMBL 318 7 1 1 4.1 C=CCN(CC=C)CCc1c[nH]c2ccc(Br)cc12 10.1016/j.bmcl.2015.12.053
71452384 90572 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
CHEMBL2205816 90572 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Binding affinity to 5-HT1B receptorBinding affinity to 5-HT1B receptor
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmcl.2012.08.046
71452384 90572 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Inhibition of 5-HT1B receptor (unknown origin) by PDSP assayInhibition of 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
CHEMBL2205816 90572 0 None -4 5 Human 6.0 pKi = 6.0 Binding
Inhibition of 5-HT1B receptor (unknown origin) by PDSP assayInhibition of 5-HT1B receptor (unknown origin) by PDSP assay
ChEMBL 280 3 1 3 1.4 OC12C3C4CC5C6C4C1C6C(C53)N2CCc1ccccn1 10.1016/j.bmc.2013.07.045
135398737 7745 93 None -691 90 Rat 6.0 pKi = 6.0 Binding
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 7745 93 None -691 90 Rat 6.0 pKi = 6.0 Binding
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 7745 93 None -691 90 Rat 6.0 pKi = 6.0 Binding
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 7745 93 None -691 90 Rat 6.0 pKi = 6.0 Binding
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 7745 93 None -691 90 Rat 6.0 pKi = 6.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 nan
44461248 212138 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 407 5 2 3 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)C1 10.1016/j.bmcl.2004.03.003
CHEMBL79725 212138 0 None -3 3 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor in L-M(tk-) cells using [3H]GR-125743 as radioligand
ChEMBL 407 5 2 3 3.9 NC(=O)c1ccc2c(c1)CCOC2CCN1CCC(c2c[nH]c3cc(F)ccc23)C1 10.1016/j.bmcl.2004.03.003
14975317 84010 0 None -138 2 Rat 4.0 pKi = 4.0 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
CHEMBL2079546 84010 0 None -138 2 Rat 4.0 pKi = 4.0 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
ChEMBL 410 5 0 4 3.8 COc1cccc2c1[C@@H]1CCN(CCCN3C(=O)CC4(CCCC4)CC3=O)C[C@@H]1C2 10.1021/jm00027a013
118464425 145087 0 None -257 9 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
CHEMBL3770981 145087 0 None -257 9 Human 5.0 pKi = 5.0 Binding
Displacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting methodDisplacement of [3H]GR127543 from 5-HT1B receptor (unknown origin) after 1.5 hrs by microbeta scintillation counting method
ChEMBL 357 3 2 7 2.8 CCOC(=O)c1cccc(NC2=NC(N(C)C)=NC3(CCCCC3)N2)c1 10.1021/acs.jmedchem.5b01631
146025727 178464 0 None -371 27 Human 5.0 pKi = 5 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
CHEMBL4466483 178464 0 None -371 27 Human 5.0 pKi = 5 Binding
Displacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting methodDisplacement of [3H]5-CT from recombinant human 5HT1B receptor stably expressed in HEK cells measured after 90 mins by microbeta scintillation counting method
ChEMBL 411 3 0 5 6.4 FC(F)(F)c1cc(Oc2nccc3ccsc23)ccc1-c1cccc2nccn12 10.1021/acs.jmedchem.9b00351
10383010 170278 0 None -371 4 Human 6.0 pKi = 6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 346 6 1 2 4.8 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
CHEMBL420191 170278 0 None -371 4 Human 6.0 pKi = 6 Binding
In vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligandIn vitro binding affinity against cloned mammalian 5-hydroxytryptamine 1D receptor beta expressed in CHO cells, by using [3H]5-HT as radioligand
ChEMBL 346 6 1 2 4.8 CCCN(Cc1ccccc1)C1CCc2ccc3[nH]cc(C=O)c3c2C1 10.1021/jm00012a022
1524 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 None -2511 51 Human 8.3 pIC50 = 8.3 Binding
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
135398737 7745 93 None -691 90 Rat 8.3 pIC50 = 8.3 Binding
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -691 90 Rat 8.3 pIC50 = 8.3 Binding
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -691 90 Rat 8.3 pIC50 = 8.3 Binding
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -691 90 Rat 8.3 pIC50 = 8.3 Binding
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -691 90 Rat 8.3 pIC50 = 8.3 Binding
Affinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HTAffinity towards 5-hydroxytryptamine 1B receptor in membranes from rat frontal cortex using [3H]5-HT
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
123606 7140 70 None -1 3 Human 7.9 pIC50 = 7.9 Binding
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
128 7140 70 None -1 3 Human 7.9 pIC50 = 7.9 Binding
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
7110 7140 70 None -1 3 Human 7.9 pIC50 = 7.9 Binding
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
CHEMBL1505 7140 70 None -1 3 Human 7.9 pIC50 = 7.9 Binding
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
DB00918 7140 70 None -1 3 Human 7.9 pIC50 = 7.9 Binding
Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.Affinity of almotriptan at recombinant h5-HT<sub>1B</sub> receptors expressed in HeLa cells, determined in a radioligand displacement assay using [<sup>125</sup>I]GTI as tracer.
Guide to Pharmacology 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C 11134654
40 8329 58 None -2 5 Human 8.1 pKd = 8.1 Binding
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
77993 8329 58 None -2 5 Human 8.1 pKd = 8.1 Binding
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
995 8329 58 None -2 5 Human 8.1 pKd = 8.1 Binding
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
CHEMBL1510 8329 58 None -2 5 Human 8.1 pKd = 8.1 Binding
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
DB00216 8329 58 None -2 5 Human 8.1 pKd = 8.1 Binding
GRAC: human 5-HT1B probeGRAC: human 5-HT1B probe
Drug Central 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 None
5 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
5202 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5202 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
CHEMBL39 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
CHEMBL39 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
DB08839 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
DB08839 6927 72 None -11 53 Human 8.0 pKd = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8863519
117 7141 19 None -1 2 Human 8.8 pKd = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
120 7141 19 None -1 2 Human 8.8 pKd = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
66004 7141 19 None -1 2 Human 8.8 pKd = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
CHEMBL88240 7141 19 None -1 2 Human 8.8 pKd = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 9605573
1220 6975 55 None -208 44 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
31 6975 55 None -208 44 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
7 6975 55 None -208 44 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
CHEMBL56 6975 55 None -208 44 Human 8.9 pKd = 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC 10431754
None 222717 0 3H-5HT -3 21 Human 11.2 pKi = 11.2 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 222717 0 3H-5HT -3 21 Human 11.2 pKi = 11.2 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 222717 0 3H-5HT -18 21 Rat 10.7 pKi = 10.7 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
11954224 222732 0 3H-5HT -12 59 Rat 10.5 pKi = 10.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
71299720 222730 0 3H-5HT 1 17 Human 10.4 pKi = 10.4 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
11797998 42466 0 UNDEFINED 1 3 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 None
CHEMBL144030 42466 0 UNDEFINED 1 3 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 454 10 4 4 4.8 NCCc1c[nH]c2ccc(OCc3ccc(COc4ccc5[nH]cc(CCN)c5c4)cc3)cc12 None
24881753 143980 0 UNDEFINED 14 2 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL374973 143980 0 UNDEFINED 14 2 Human 10.0 pKi = 10 Binding
NoneNone
PDSP KiDatabase 666 16 4 4 9.1 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
1809 6922 32 3H-5HT -15 37 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107780 8625 54 3H-5HT 1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-5HT 1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-5HT 1 18 Human 9.9 pKi = 9.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1809 6922 32 3H-5HT -15 37 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 9.8 pKi = 9.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4106 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -11 33 Human 9.7 pKi = 9.7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1809 6922 32 3H-5HT -15 37 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
132 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
124 9755 47 3H-5HT 1 32 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-5HT 1 32 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-5HT 1 32 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-5HT 1 32 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-5HT 1 32 Human 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
132 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-5HT -54 15 Rat 9.6 pKi = 9.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
11954224 222732 0 3H-GR125743 -32 59 Human 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
None 222725 0 3H-GR-125743 2 24 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
1809 6922 32 3H-GR-125743 -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-125743 -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-125743 -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-5HT -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -32 37 Rat 9.5 pKi = 9.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 222725 0 3H-5HT 2 24 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 222725 0 3H-5HT 2 24 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
152662 222736 0 3H-5HT 109 7 Rat 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
107780 8625 54 3H-GR-125743 1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-GR-125743 1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-GR-125743 1 18 Human 9.4 pKi = 9.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
152662 222736 0 125I-CYP 109 7 Rat 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
24881204 195201 0 UNDEFINED 3 2 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL502138 195201 0 UNDEFINED 3 2 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 680 17 4 4 9.5 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
None 222717 0 3H-5HT -3 21 Human 9.3 pKi = 9.3 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
5 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
24881754 195071 0 UNDEFINED 3 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL500284 195071 0 UNDEFINED 3 2 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 694 18 4 4 9.9 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
5 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
12312583 222796 0 3H-5HT 1 3 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 254 1 2 2 2.0 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)CO None
9832057 59089 0 UNDEFINED 1 3 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 None
CHEMBL158941 59089 0 UNDEFINED 1 3 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 692 16 2 6 4.8 CN(C)CCc1c[nH]c2ccc(CS(=O)(=O)N(C)Cc3ccc(CN(C)S(=O)(=O)Cc4ccc5[nH]cc(CCN(C)C)c5c4)cc3)cc12 None
1809 6922 32 3H-5HT -15 37 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 9.2 pKi = 9.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 222717 0 125I-CYP -18 21 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
107 6929 121 3H-5HT -16 31 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -16 31 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -16 31 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
44279525 112289 0 UNDEFINED -1 3 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 None
CHEMBL31217 112289 0 UNDEFINED -1 3 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 444 8 2 5 4.0 CN1CCN(c2cccc3ccc(OCCOc4ccc5[nH]cc(CCN)c5c4)cc23)CC1 None
24881689 176911 0 UNDEFINED 1 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL444404 176911 0 UNDEFINED 1 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 554 8 4 4 6.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
1809 6922 32 3H-GR-125743 -8 37 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-125743 -8 37 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-125743 -8 37 Guinea pig 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
24881203 180010 0 UNDEFINED 1 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL452387 180010 0 UNDEFINED 1 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 624 13 4 4 8.0 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
124 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
24881264 195086 0 UNDEFINED 13 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL500488 195086 0 UNDEFINED 13 2 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 709 19 4 4 10.3 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
124 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-5HT -2 32 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
5 6927 72 3H-GR-125743 -13 53 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-125743 -13 53 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-125743 -13 53 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-125743 -13 53 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1809 6922 32 3H-5HT -15 37 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
133 9274 52 3H-5HT -40 43 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5HT -40 43 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5HT -40 43 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5HT -40 43 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5HT -40 43 Rat 9.1 pKi = 9.1 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
None 222725 0 3H-5HT 2 24 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
107780 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
2865 10915 73 3H-Alniditan -12 53 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-Alniditan -12 53 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-Alniditan -12 53 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-Alniditan -12 53 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-Alniditan -12 53 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
107780 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 35S-GTPGammaS 1 18 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
28 10269 46 35S-GTPGammaS 13 10 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 10269 46 35S-GTPGammaS 13 10 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 10269 46 35S-GTPGammaS 13 10 Human 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
None 222725 0 125I-ICYP 2 24 Rat 9.0 pKi = 9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
132 8058 13 3H-GR-125743 -54 15 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-GR-125743 -54 15 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-GR-125743 -54 15 Rat 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
5 6927 72 3H-5HT -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 UNDEFINED -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 UNDEFINED -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 UNDEFINED -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 UNDEFINED -11 53 Human 9.0 pKi = 9.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2543 10479 68 3H-Alniditan -3 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-Alniditan -3 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-Alniditan -3 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-Alniditan -3 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-Alniditan -3 32 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
12312583 222796 0 3H-5HT 1 3 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 254 1 2 2 2.0 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)CO None
107780 8625 54 3H-5HT 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-5HT 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-5HT 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107780 8625 54 3H-GR-125743 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-GR-125743 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-GR-125743 1 18 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
24881752 178538 0 UNDEFINED -1 2 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL446745 178538 0 UNDEFINED -1 2 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 638 14 4 4 8.4 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
24881202 179365 0 UNDEFINED -1 2 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL448902 179365 0 UNDEFINED -1 2 Human 8.9 pKi = 8.9 Binding
NoneNone
PDSP KiDatabase 596 11 4 4 7.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CCCCCCC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
None 222717 0 3H-GR-125743 -25 21 Guinea pig 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1809 6922 32 3H-5HT -15 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 222725 0 125I-ICYP 2 24 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
107 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -30 31 Rat 8.8 pKi = 8.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
132 8058 13 125I-CYP -54 15 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 125I-CYP -54 15 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 125I-CYP -54 15 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2543 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1809 6922 32 3H-5HT -97 37 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -97 37 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -97 37 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
None 222725 0 3H-5HT -7 24 Mouse 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
71299720 222730 0 3H-5HT 1 17 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
11954224 222732 0 None -12 59 Rat 8.0 pKi = 8 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1342 6824 49 3H-5HT -4 19 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 3H-5HT -4 19 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 3H-5HT -4 19 Human 8.0 pKi = 8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
4106 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 223122 0 3H-GR-125743 1 2 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 228 2 1 3 2.6 C1CNCCC1SC2=NC(=CC=C2)Cl None
4106 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -102 33 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
None 223262 0 125I-ICYP -58 3 Rat 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase None None None None None
4106 9280 22 3H-GR-125743 -27 33 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-GR-125743 -27 33 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-GR-125743 -27 33 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-GR-125743 -27 33 Guinea pig 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2543 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
137 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 7158 52 3H-5HT -154 12 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
4106 9280 22 3H-GR-125743 -102 33 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-GR-125743 -102 33 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-GR-125743 -102 33 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-GR-125743 -102 33 Rat 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
24881617 195105 0 UNDEFINED -165 2 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500737 195105 0 UNDEFINED -165 2 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 756 13 4 4 10.1 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
152 7152 29 125I-CYP -57 19 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
2107 7152 29 125I-CYP -57 19 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
CHEMBL275854 7152 29 125I-CYP -57 19 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.8 CC(Cc1c[nH]c2c1cc(O)cc2)N None
41 8440 0 3H-5CT -794 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
41 8440 0 3H-GR-125743 -794 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-5CT -794 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
72036 8440 0 3H-GR-125743 -794 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-5CT -794 17 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
CHEMBL1765294 8440 0 3H-GR-125743 -794 17 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 195 0 1 3 0.9 Fc1cccc2c1O[C@H]1CNC[C@@H]1O2 None
173 10036 95 3H-5HT -11 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -11 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -11 23 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
2605 10555 30 3H-GR-125743 -218 10 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 3H-GR-125743 -218 10 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 3H-GR-125743 -218 10 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 3H-GR-125743 -218 10 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 3H-GR-125743 -218 10 Guinea pig 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
18922713 105274 0 3H-5HT -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
CHEMBL276031 105274 0 3H-5HT -12882 9 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 298 6 1 2 4.0 CCCN(CCC)C1Cc2c[nH]c3ccc(C(C)=O)c(c23)C1 None
24840389 121991 4 3H-GR-125743 -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
CHEMBL334529 121991 4 3H-GR-125743 -741 16 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 415 9 0 4 4.6 CCCN(CCC)C1CCc2cc(CS(=O)(=O)c3ccc(OC)cc3)ccc2C1 None
12016890 197555 6 3H-CYANOPINDOLOL -1698 12 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
CHEMBL5183389 197555 6 3H-CYANOPINDOLOL -1698 12 Rat 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 318 4 1 3 2.6 NC(=O)c1ccc(F)c2c1CC(N(C1CCC1)C1CCC1)CO2 None
54841 209906 52 3H-5HT 1 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
CHEMBL641 209906 52 3H-5HT 1 30 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 255 6 1 2 3.7 CNCC[C@@H](Oc1ccccc1C)c1ccccc1 None
None 223158 0 UNDEFINED -1122 11 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 243 3 1 4 2.7 CCC1=CC2=C(O1)C=CC3=C2N(N=C3)CC(C)N None
None 224015 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 768 9 4 4 9.4 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC(C(F)(F)F)N5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
None 224016 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 507 13 3 3 6.9 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CCCCCCCCCC(=O)O None
None 224017 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 422 7 2 3 4.7 CN(C)CCCN1CCC(CC1)C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F None
None 224018 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 448 6 2 3 5.2 C1CCN(CC1)CCN2CCC(CC2)C3=CNC4=C3C=C(C=C4)NC(=O)C5=CC=C(C=C5)F None
None 224019 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 381 5 3 3 3.7 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CCO None
None 224020 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 427 5 2 2 5.9 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC5=CC=CC=C5 None
None 224021 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 449 10 2 2 7.1 CCCCCCCCN1CCC(CC1)C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F None
None 224022 0 UNDEFINED 1 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 743 10 5 5 7.3 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC(C(=O)N)N5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
3075702 224111 0 125I-CYP -2 37 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 198 3 1 3 1.5 C1CNC1COC2=CN=C(C=C2)Cl None
1574 6869 60 125I-CYP -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1574 6869 60 3H-5HT -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 125I-CYP -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 3H-5HT -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 125I-CYP -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 3H-5HT -24 21 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1192 6935 47 3H-5HT -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1794 6935 47 3H-5HT -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
CHEMBL501701 6935 47 3H-5HT -162 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N None
1220 6975 55 125I-CYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 6975 55 125I-ICYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1220 6975 55 3H-5HT -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 125I-CYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 125I-ICYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 125I-CYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 125I-ICYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 125I-CYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 125I-ICYP -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -7413 44 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
179 7188 115 3H-5HT -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-5HT -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-5HT -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-5HT -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-5HT -4365 50 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
242 7258 124 3H-5CT -380 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-5CT -380 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-5CT -380 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-5CT -380 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-5CT -380 51 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
2249 7300 111 125I-CYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249 7300 111 125I-ICYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2249 7300 111 3H-5HT -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 7300 111 125I-CYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 7300 111 125I-ICYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
255 7300 111 3H-5HT -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 7300 111 125I-CYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 7300 111 125I-ICYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
548 7300 111 3H-5HT -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 7300 111 125I-CYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 7300 111 125I-ICYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
CHEMBL24 7300 111 3H-5HT -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 7300 111 125I-CYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 7300 111 125I-ICYP -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
DB00335 7300 111 3H-5HT -295 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 8 3 4 0.5 OC(COc1ccc(cc1)CC(=O)N)CNC(C)C None
2369 7409 80 125I-ICYP -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2369 7409 80 3H-5HT -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 7409 80 125I-ICYP -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
356 7409 80 3H-5HT -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 7409 80 125I-ICYP -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
549 7409 80 3H-5HT -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 7409 80 125I-ICYP -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
CHEMBL423 7409 80 3H-5HT -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 7409 80 125I-ICYP -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
DB00195 7409 80 3H-5HT -3235 8 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 307 11 2 4 2.4 OC(COc1ccc(cc1)CCOCC1CC1)CNC(C)C None
2477 7532 59 125I-CYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477 7532 59 125I-ICYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2477 7532 59 3H-5HT -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 125I-CYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 125I-ICYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 3H-5HT -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 125I-CYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 125I-ICYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 3H-5HT -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 125I-CYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 125I-ICYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 3H-5HT -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 125I-CYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 125I-ICYP -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 3H-5HT -16 29 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
2398 7741 62 3H-GR-125743 -1230 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2801 7741 62 3H-GR-125743 -1230 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
701 7741 62 3H-GR-125743 -1230 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
CHEMBL415 7741 62 3H-GR-125743 -1230 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
DB01242 7741 62 3H-GR-125743 -1230 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C None
2803 7742 58 125I-ICYP -602 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
516 7742 58 125I-ICYP -602 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
704 7742 58 125I-ICYP -602 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
CHEMBL134 7742 58 125I-ICYP -602 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
DB00575 7742 58 125I-ICYP -602 19 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl None
141 8209 35 3H-5-CT -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 8209 35 3H-5-CT -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 8209 35 3H-5-CT -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 8209 35 3H-5-CT -114 22 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
681 8247 72 125I-CYP -1995 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
940 8247 72 125I-CYP -1995 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
947 8247 72 125I-CYP -1995 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
CHEMBL59 8247 72 125I-CYP -1995 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
DB00988 8247 72 125I-CYP -1995 38 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O None
1353 8692 93 3H-5HT -5248 85 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-5HT -5248 85 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-5HT -5248 85 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-5HT -5248 85 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-5HT -5248 85 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
1204 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1247 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
1375 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
774 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
CHEMBL90 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
DB05381 8713 119 3H-5HT -1949 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 111 2 2 2 -0.1 NCCc1cnc[nH]1 None
12575 8769 30 125I-CYP -6606 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
54459 8769 30 125I-CYP -6606 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
CHEMBL10316 8769 30 125I-CYP -6606 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
DB12551 8769 30 125I-CYP -6606 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 204 1 1 4 0.8 C1CN=C(N1)C2COC3=CC=CC=C3O2 None
42 8844 57 3H-5HT -1778 18 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 8844 57 125I-CYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 8844 57 125I-ICYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
42 8844 57 3H-5HT -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 8844 57 3H-5HT -1778 18 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 8844 57 125I-CYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 8844 57 125I-ICYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
56971 8844 57 3H-5HT -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 8844 57 3H-5HT -1778 18 Bovine 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 8844 57 125I-CYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 8844 57 125I-ICYP -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL8412 8844 57 3H-5HT -1778 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 401 6 0 7 1.2 O=C1c2ccccc2S(=O)(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
1524 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1524 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-GR-125743 -7585 51 Guinea pig 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 125I-ICYP -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-5HT -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-GR-125743 -512 51 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1531 9046 69 125I-CYP -676 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 9046 69 125I-CYP -676 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 9046 69 125I-CYP -676 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 9046 69 125I-CYP -676 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 9046 69 125I-CYP -676 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
206 9271 16 125I-CYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 9271 16 125I-ICYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
206 9271 16 3H-5HT -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 125I-CYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 125I-ICYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 3H-5HT -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 125I-CYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 125I-ICYP -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 3H-5HT -7585 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
1786 9298 85 3H-5-CT -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
1786 9298 85 125I-ICYP -524 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 9298 85 3H-5-CT -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
4171 9298 85 125I-ICYP -524 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 9298 85 3H-5-CT -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
553 9298 85 125I-ICYP -524 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 9298 85 3H-5-CT -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
CHEMBL13 9298 85 125I-ICYP -524 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 9298 85 3H-5-CT -524 11 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
DB00264 9298 85 125I-ICYP -524 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 9 2 4 1.6 COCCc1ccc(cc1)OCC(CNC(C)C)O None
135 9310 43 3H-5HT -851 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-5HT -851 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-5HT -851 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-5HT -851 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-5HT -851 56 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
484 9633 51 125I-ICYP -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
951 9633 51 125I-ICYP -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
CHEMBL432 9633 51 125I-ICYP -100 35 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 2 4 4 0.1 NCC(c1ccc(c(c1)O)O)O None
283 9904 57 3H-5HT -6606 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 9904 57 3H-5HT -6606 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 9904 57 3H-5HT -6606 12 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
2202 9906 96 3H-GR-125743 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
4850 9906 96 3H-GR-125743 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
49 9906 96 3H-GR-125743 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
CHEMBL1371770 9906 96 3H-GR-125743 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
DB12478 9906 96 3H-GR-125743 -316 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 None
2220 9908 82 125I-ICYP -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 9908 82 125I-ICYP -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 9908 82 125I-ICYP -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 9908 82 125I-ICYP -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 9908 82 125I-ICYP -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
3486 9931 56 125I-ICYP -204 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
4883 9931 56 125I-ICYP -204 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
555 9931 56 125I-ICYP -204 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
CHEMBL6995 9931 56 125I-ICYP -204 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
DB01297 9931 56 125I-ICYP -204 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 266 7 3 4 1.4 OC(COc1ccc(cc1)NC(=O)C)CNC(C)C None
2303 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 3H-5HT -1174 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
243 9976 91 3H-Alniditan -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3052762 9976 91 3H-Alniditan -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
3502 9976 91 3H-Alniditan -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
CHEMBL117287 9976 91 3H-Alniditan -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
DB06480 9976 91 3H-Alniditan -1096 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N None
2 10035 23 3H-GR-125743 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
54562 10035 23 3H-GR-125743 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
CHEMBL240773 10035 23 3H-GR-125743 -2089 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 2 1 2 2.0 CCCN1CCC[C@H]2[C@H]1Cc1cn[nH]c1C2 None
5074 10105 80 125I-CYP -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5074 10105 80 3H-GR-125743 -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 125I-CYP -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 3H-GR-125743 -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 125I-CYP -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 3H-GR-125743 -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 125I-CYP -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 3H-GR-125743 -4168 30 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2402 10143 62 3H-GR-125743 -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
5095 10143 62 3H-GR-125743 -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
7295 10143 62 3H-GR-125743 -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
CHEMBL589 10143 62 3H-GR-125743 -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
DB00268 10143 62 3H-GR-125743 -549 24 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O None
128563 10237 33 3H-5-CT -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
128563 10237 33 3H-GR-125743 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 3H-5-CT -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
1666 10237 33 3H-GR-125743 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 3H-5-CT -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
CHEMBL445332 10237 33 3H-GR-125743 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 3H-5-CT -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
DB12327 10237 33 3H-GR-125743 -2398 42 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 432 3 0 8 3.0 COC(=O)[C@@H]1C[C@H](OC(=O)C)C(=O)[C@H]2[C@@]1(C)CC[C@@H]1[C@]2(C)C[C@H](OC1=O)c1cocc1 None
221 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
3277600 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
CHEMBL323356 10264 71 UNDEFINED -478 14 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 286 2 2 4 3.6 O=C(Nc1snc(c1)C)Nc1ccc2c(c1)ccn2C None
2464 10412 58 125I-ICYP -165 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
5253 10412 58 125I-ICYP -165 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
7297 10412 58 125I-ICYP -165 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
CHEMBL471 10412 58 125I-ICYP -165 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
DB00489 10412 58 125I-ICYP -165 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 272 6 3 4 1.1 CC(NCC(c1ccc(cc1)NS(=O)(=O)C)O)C None
2470 10425 50 3H-5HT -95499 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 10425 50 125I-ICYP -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 10425 50 3H-5HT -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5HT -95499 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 125I-ICYP -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5HT -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5HT -95499 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 125I-ICYP -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5HT -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5HT -95499 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 125I-ICYP -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5HT -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5HT -95499 58 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 125I-ICYP -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5HT -43651 58 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5268 10428 40 125I-CYP -31622 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
53 10428 40 125I-CYP -31622 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
CHEMBL300555 10428 40 125I-CYP -31622 18 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 379 3 1 5 2.3 O=C1NCN(C21CCN(CC2)CC1COc2c(O1)cccc2)c1ccccc1 None
1267 10576 49 3H-5HT -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
3035905 10576 49 3H-5HT -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
CHEMBL260374 10576 49 3H-5HT -4168 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 292 2 2 2 2.8 S=C(N1CCC(CC1)c1cnc[nH]1)NC1CCCCC1 None
213 10625 55 3H-GR-125743 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 3H-GR-125743 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 3H-GR-125743 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 3H-GR-125743 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 3H-GR-125743 -912 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
1150 10650 121 125I-CYP -204 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 10650 121 125I-CYP -204 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 10650 121 125I-CYP -204 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 10650 121 125I-CYP -204 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
185 10778 60 3H-GR-125743 -30902 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
5311271 10778 60 3H-GR-125743 -30902 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
CHEMBL74355 10778 60 3H-GR-125743 -30902 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
DB16351 10778 60 3H-GR-125743 -30902 37 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 373 7 1 4 3.8 COc1cccc(c1OC)[C@@H](C1CCN(CC1)CCc1ccc(cc1)F)O None
102 10899 48 3H-5HT -186 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -186 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -186 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -186 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -186 49 Mouse 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
108182 10903 22 3H-5HT -32 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
245 10903 22 3H-5HT -32 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
CHEMBL18041 10903 22 3H-5HT -32 17 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 309 3 2 4 1.8 COc1cc(N)c(cc1C(=O)NC1CN2CCC1CC2)Cl None
2662 18156 131 3H-GR-125743 -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
CHEMBL118 18156 131 3H-GR-125743 -41 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 381 3 1 4 3.5 Cc1ccc(-c2cc(C(F)(F)F)nn2-c2ccc(S(N)(=O)=O)cc2)cc1 None
5090 22333 106 3H-GR-125743 -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
CHEMBL122 22333 106 3H-GR-125743 -1348 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 0 4 2.6 CS(=O)(=O)c1ccc(C2=C(c3ccccc3)C(=O)OC2)cc1 None
671690 33870 35 125I-ICYP -10 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
CHEMBL1365455 33870 35 125I-ICYP -10 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 2 0 3 3.8 CN1[C@H]2CC[C@@H]1CC(OC(=O)c1cc(Cl)cc(Cl)c1)C2 None
10297 33885 30 3H-GR-125743 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
CHEMBL136560 33885 30 3H-GR-125743 -38 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 C[C@H](N)[C@H](O)c1ccccc1 None
127151 42104 18 3H-GR-125743 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
3022645 42104 18 3H-GR-125743 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
CHEMBL14370 42104 18 3H-GR-125743 -1584 10 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 313 6 1 4 3.2 CCOc1ccccc1OC(c1ccccc1)C1CNCCO1 None
156391 53574 99 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL1200806 53574 99 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
CHEMBL154 53574 99 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 COc1ccc2cc([C@H](C)C(=O)O)ccc2c1 None
5475158 73987 25 3H-5HT -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 73987 25 3H-5HT -1023 14 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
10624 77075 19 3H-GR-125743 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
138543650 77075 19 3H-GR-125743 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
CHEMBL194378 77075 19 3H-GR-125743 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
DB11664 77075 19 3H-GR-125743 -776 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 5 3 3 1.7 CN(C)CCc1c[nH]c2cccc(OP(=O)(O)O)c12 None
108107 86719 38 3H-5HT -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
156592250 86719 38 3H-5HT -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL1256878 86719 38 3H-5HT -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
CHEMBL212579 86719 38 3H-5HT -15 16 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 319 3 4 5 0.5 N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1 None
442108 91411 6 3H-5-CT -1 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
CHEMBL222287 91411 6 3H-5-CT -1 12 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 310 2 1 2 3.9 CC[C@H]1C[C@H]2C[C@H]3c4[nH]c5ccc(OC)cc5c4CCN(C2)[C@@H]13 None
2244 101008 100 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
CHEMBL25 101008 100 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 180 2 1 3 1.3 CC(=O)Oc1ccccc1C(=O)O None
104870 105656 47 3H-GR-125743 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
5374 105656 47 3H-GR-125743 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
CHEMBL279085 105656 47 3H-GR-125743 -549 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 None
55191 106393 64 125I-CYP -446 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
CHEMBL284092 106393 64 125I-CYP -446 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
DB12184 106393 64 125I-CYP -446 9 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 359 6 0 6 1.6 CC1(C)CC(=O)N(CCCCN2CCN(c3ncccn3)CC2)C(=O)C1 None
44208932 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
CHEMBL381689 147485 7 UNDEFINED -89125 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 475 5 1 3 6.8 Cc1ccc(Cn2nc(C(=O)NC3C4(C)CCC(C4)C3(C)C)cc2-c2ccc(Cl)c(C)c2)cc1 None
1615 174570 24 3H-GR-125743 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
CHEMBL43048 174570 24 3H-GR-125743 -26 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 193 3 1 3 1.6 CNC(C)Cc1ccc2c(c1)OCO2 None
43815 193699 64 3H-5HT -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL1708 193699 64 3H-5HT -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
CHEMBL490 193699 64 3H-5HT -1995 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 4 1 4 3.3 Fc1ccc([C@@H]2CCNC[C@H]2COc2ccc3c(c2)OCO3)cc1 None
24882267 195106 0 UNDEFINED -776 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 840 19 4 4 12.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500749 195106 0 UNDEFINED -776 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 840 19 4 4 12.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24882192 195581 0 UNDEFINED -125 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 714 10 4 4 8.9 O=C(Nc1ccc2[nH]cc(C3CCN(CCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL505954 195581 0 UNDEFINED -125 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 714 10 4 4 8.9 O=C(Nc1ccc2[nH]cc(C3CCN(CCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24881552 195890 0 UNDEFINED -45 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 700 9 4 4 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL510280 195890 0 UNDEFINED -45 2 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 700 9 4 4 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
3672 199312 136 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
CHEMBL521 199312 136 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 206 4 1 1 3.1 CC(C)Cc1ccc(C(C)C(=O)O)cc1 None
54676228 200394 112 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
CHEMBL527 200394 112 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 331 2 2 5 1.6 CN1C(C(=O)Nc2ccccn2)=C(O)c2ccccc2S1(=O)=O None
2771 201796 74 3H-5CT -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 201796 74 3H-GR-125743 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
2771 201796 74 3H-5HT -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-5CT -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-GR-125743 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL1200781 201796 74 3H-5HT -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-5CT -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-GR-125743 -120 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
CHEMBL549 201796 74 3H-5HT -120 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 None
4495 203314 92 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
CHEMBL56367 203314 92 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 308 5 1 5 2.8 CS(=O)(=O)Nc1ccc([N+](=O)[O-])cc1Oc1ccccc1 None
54677470 207330 115 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL1256873 207330 115 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
CHEMBL599 207330 115 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 351 2 2 6 2.0 Cc1cnc(NC(=O)C2=C(O)c3ccccc3S(=O)(=O)N2C)s1 None
162265 209053 22 3H-GR-125743 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
4786 209053 22 3H-GR-125743 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
CHEMBL61006 209053 22 3H-GR-125743 -239 44 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 151 2 2 2 1.1 CC(N)C(O)c1ccccc1 None
3036864 209533 19 125I-CYP -41686 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1256645 209533 19 125I-CYP -41686 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL1814790 209533 19 125I-CYP -41686 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
CHEMBL62 209533 19 125I-CYP -41686 27 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 287 1 1 2 3.7 CN1CCc2cc(Cl)c(O)cc2[C@@H](c2ccccc2)C1 None
5281600 209804 92 3H-5CT -173 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-5CT -173 32 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
5656 209845 87 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
5656 209845 87 3H-GR-125743 -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 3H-5HT -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
CHEMBL637 209845 87 3H-GR-125743 -79 43 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 277 5 1 3 3.0 COc1ccc(C(CN(C)C)C2(O)CCCCC2)cc1 None
1973 210262 15 3H-CYANOPINDOLOL -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL1394464 210262 15 3H-CYANOPINDOLOL -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
CHEMBL66089 210262 15 3H-CYANOPINDOLOL -3 36 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 462 3 1 7 3.9 Nc1ncnc2nc(-c3ccc(N4CCOCC4)nc3)cc(-c3cccc(Br)c3)c12 None
1614 210434 24 3H-5HT -81 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
CHEMBL6731 210434 24 3H-5HT -81 10 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 2 1 3 1.3 CC(N)Cc1ccc2c(c1)OCO2 None
202478 211466 20 3H-GR-125743 -52 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
CHEMBL7393 211466 20 3H-GR-125743 -52 25 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@H](c2cccc(O)c2)C1 None
3821 211497 17 3H-GR125743 -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
CHEMBL742 211497 17 3H-GR125743 -1 18 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 237 2 1 2 2.9 CNC1(c2ccccc2Cl)CCCCC1=O None
4158 212120 21 3H-GR-125743 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL1722 212120 21 3H-GR-125743 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
CHEMBL796 212120 21 3H-GR-125743 -141 21 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 233 3 1 3 2.1 COC(=O)C(c1ccccc1)C1CCCCN1 None
4054 212280 72 3H-GR-125743 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL1699 212280 72 3H-GR-125743 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
CHEMBL807 212280 72 3H-GR-125743 -1 36 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 179 0 1 1 2.7 CC12CC3CC(C)(C1)CC(N)(C3)C2 None
119607 212982 113 3H-GR-125743 -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
CHEMBL865 212982 113 3H-GR-125743 -97 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 314 3 1 4 3.0 Cc1onc(-c2ccccc2)c1-c1ccc(S(N)(=O)=O)cc1 None
16231 214288 57 3H-5HT -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
CHEMBL945 214288 57 3H-5HT -7 17 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 229 1 5 6 -1.1 N=C(N)NC(=O)c1nc(Cl)c(N)nc1N None
16212426 222710 0 125I-CYP -1 4 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 403 2 7 8 -0.8 CN1CC(=O)N=C1N.C1=C(C=C(C2=C1C(=CN2)CCN)O)O.OS(=O)(=O)O None
57174031 222719 0 3H-5HT -1778 20 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 125I-CYP -1778 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 125I-ICYP -1778 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
57174031 222719 0 3H-5HT -1778 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 284 2 1 3 3.0 CN1C2CCC1CC(C2)OC(=O)C3=CNC4=CC=CC=C43 None
None 222722 0 3H-5HT -7943 11 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(CC)C(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C None
138107169 222731 0 125I-CYP -19054 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 125I-CYP -19054 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
77590 222734 0 3H-5HT -138 6 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 124 4 0 2 0.8 COCCOCCl None
None 222772 0 3H-5-CT -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 329 2 0 4 3.6 CC1=NC=CN1CC2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl None
104911 222798 0 3H-GR-125743 -38018 37 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
None 222799 0 3H-8-OH-DPAT -154 7 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 265 5 1 2 3.5 CCCN(CCC)C1CCC2=C(C=CC(=C2C1)O)F None
None 222907 0 125I-ICYP -1 13 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 164 3 1 3 0.8 C1CNC1COC2=CN=CC=C2 None
None 222914 0 3H-KETANSERIN -3162 23 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
25137849 222958 0 3H-GR-125743 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
71290 222958 0 3H-GR-125743 -4 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 165 3 2 2 1.3 CC(C(C1=CC=CC=C1)O)NC None
62857 222960 0 3H-5HT -154 7 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 345 6 1 2 4.9 CNCCC(C1=CC=CC=C1)OC2=CC=C(C=C2)C(F)(F)F.Cl None
None 223033 0 3H-5HT -8317 20 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 416 9 3 4 2.8 C1=CC(=CC=C1CCNC(N)SCCCC2=CN=CN2)I None
None 223090 0 3H-GR-125743 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 240 7 4 6 -0.8 C(C(C(=O)O)N)SSCC(C(=O)O)N None
None 223091 0 3H-GR-125743 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 4 2 3 0.2 CSCCC(C(=O)O)N None
None 223092 0 3H-GR-125743 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 135 3 3 3 -0.3 C(CS)C(C(=O)O)N None
None 223093 0 3H-GR-125743 -1 34 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 121 2 3 3 -0.7 C(C(C(=O)O)N)S None
None 223095 0 3H-GR-125743 -1 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 153 3 3 3 -1.4 C(C(C(=O)O)N)S(=O)O None
None 223096 0 3H-GR-125743 -1 39 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 169 3 3 4 -1.7 C(C(C(=O)O)N)S(=O)(=O)O None
None 223097 0 3H-GR-125743 -1 30 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 183 4 3 4 -1.3 C(CS(=O)(=O)O)C(C(=O)O)N None
None 223104 0 3H-GR-125743 -13 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.2 CC(C(=O)C1=CC=CC=C1)N None
1576 223105 0 3H-GR-125743 -16 40 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 163 3 1 2 1.5 CC(C(=O)C1=CC=CC=C1)NC None
None 223121 0 3H-GR-125743 -1862 19 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 246 2 1 4 1.6 CCCN1CCCC2C1CC3=CN=C(N=C3C2)N None
135269 223168 0 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 222 5 1 3 2.5 CCCCC(=O)OC1=CC=CC=C1C(=O)O None
23681059 223169 0 3H-GR-125743 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 230 3 1 2 3.0 CC(C1=CC2=C(C=C1)C=C(C=C2)OC)C(=O)O None
5018304 223170 0 3H-GR-125743 -1 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 317 4 1 3 0.0 C1=CC=C(C(=C1)CC(=O)[O-])NC2=C(C=CC=C2Cl)Cl.[Na+] None
84003 223171 0 3H-GR-125743 -1 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 376 6 5 7 -0.0 C1CN2C(=CC=C2C(=O)C3=CC=CC=C3)C1C(=O)O.C(C(CO)(CO)N)O None
123619 223172 0 3H-GR-125743 -1412 27 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 358 3 0 4 4.2 CC1=NC=C(C=C1)C2=NC=C(C=C2C3=CC=C(C=C3)S(=O)(=O)C)Cl None
119828 223173 0 3H-GR-125743 -1 29 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 370 5 1 5 3.5 CCC(=O)NS(=O)(=O)C1=CC=C(C=C1)C2=C(ON=C2C3=CC=CC=C3)C None
None 223174 0 3H-GR-125743 -7 28 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 517 8 2 5 5.2 CC1=C(C2=C(N1C(=O)C3=CC=C(C=C3)Cl)C=CC(=C2)OC)CC(=O)NCCC4=CC=C(C=C4)NC(=O)C None
688390 223264 0 125I-ICYP -21 3 Rat 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 267 5 2 4 2.5 C[C@H]([C@H](C1=C(C=CC(=C1)OC)OC)O)NC(C)(C)C None
None 223268 0 3H-GR-125743 -4570 26 Human 5.0 pKi = 5 Binding
NoneNone
PDSP KiDatabase 347 6 0 3 5.0 CC(=O)N(CC1=CC=CC=C1OC)C2=CC=CC=C2OC3=CC=CC=C3 None
1150 10650 121 125I-CYP -204 25 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 10650 121 125I-CYP -204 25 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 10650 121 125I-CYP -204 25 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 10650 121 125I-CYP -204 25 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
None 224014 0 UNDEFINED -4 2 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 726 10 4 4 9.0 C1CN(CCC1C2=CNC3=C2C=C(C=C3)NC(=O)C4=CC=C(C=C4)F)CC=CCN5CCC(CC5)C6=CNC7=C6C=C(C=C7)NC(=O)C8=CC=C(C=C8)F None
115 10563 80 125I-ICYP 1 27 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-ICYP 1 27 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-ICYP 1 27 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
11297 74119 18 125I-CYP -26 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
11297 74119 18 3H-5HT -26 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
CHEMBL18855 74119 18 125I-CYP -26 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
CHEMBL18855 74119 18 3H-5HT -26 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2cccc(O)c12 None
3033677 209723 40 125I-CYP -5370 9 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
CHEMBL2355519 209723 40 125I-CYP -5370 9 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
CHEMBL62919 209723 40 125I-CYP -5370 9 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 411 5 1 5 3.8 O=C(c1ccc(F)cc1)C1CCN(CCn2c(=S)[nH]c3ccccc3c2=O)CC1 None
2995 211184 53 3H-5CT -3 23 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 3H-5CT -3 23 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 3H-5CT -3 23 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 211184 53 3H-5CT -3 23 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
None 222735 0 125I-CYP -141 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
None 222735 0 3H-5HT -141 6 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 149 2 1 2 1.9 CCC(=O)C1=CC=C(C=C1)N None
None 223057 0 3H-5CT -12022 12 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 426 6 0 6 3.4 C1CCC2C(C1)C(=O)N(C2=O)CCCCN3CCN(CC3)C4=NSC5=CC=CC=C54 None
None 222750 0 3H-5HT -2344 15 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
115237 62359 119 3H-GR-125743 -93 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-GR-125743 -93 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-GR-125743 -93 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
100 10577 58 3H-GR-125743 -13 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 3H-GR-125743 -13 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 3H-GR-125743 -13 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 3H-GR-125743 -13 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 3H-GR-125743 -13 54 Human 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
71299720 222730 0 125I-ICYP -44 17 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
2337 10030 77 3H-GR-125743 -26 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-GR-125743 -26 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-GR-125743 -26 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-GR-125743 -26 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-GR-125743 -26 62 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
7153 104796 77 125I-ICYP -10 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 125I-ICYP -10 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
31101 7516 40 125I-CYP -48 35 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 125I-CYP -48 35 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 125I-CYP -48 35 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 125I-CYP -48 35 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 125I-CYP -48 35 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
127404 104360 22 125I-CYP -2 4 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
127404 104360 22 3H-5HT -2 4 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
CHEMBL27077 104360 22 125I-CYP -2 4 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
CHEMBL27077 104360 22 3H-5HT -2 4 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 274 7 2 4 2.2 CC(C)NCC(O)COc1ccccc1-n1cccc1 None
None 223123 0 3H-GR-125743 -26 2 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 338 6 3 5 1.7 C1CNC(=NC1)NCCCNCC2CCC3=CC=CC=C3O2.Cl None
1222 8445 49 3H-Alniditan -134 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 3H-Alniditan -134 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 3H-Alniditan -134 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 3H-Alniditan -134 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 3H-Alniditan -134 32 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
115 10563 80 3H-5HT -2 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT -2 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT -2 27 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
71299720 222730 0 125I-CYP -44 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
71299720 222730 0 3H-5HT -44 17 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
1809 6922 32 3H-GR-125743 -15 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-125743 -15 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-125743 -15 37 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
115237 62359 119 3H-Alniditan -93 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-Alniditan -93 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-Alniditan -93 54 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1342 6824 49 3H-5HT -4 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 3H-5HT -4 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 3H-5HT -4 19 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
None 222725 0 3H-5HT -8 24 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 222725 0 3H-5HT -8 24 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 223122 0 3H-GR-125743 -1 2 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 228 2 1 3 2.6 C1CNCCC1SC2=NC(=CC=C2)Cl None
4106 9280 22 125I-ICYP -102 33 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-ICYP -102 33 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-ICYP -102 33 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-ICYP -102 33 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1220 6975 55 3H-5HT -208 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
135398737 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2176 9901 68 3H-8-OH-DPAT -1737 27 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-8-OH-DPAT -1737 27 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-8-OH-DPAT -1737 27 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-8-OH-DPAT -1737 27 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-8-OH-DPAT -1737 27 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
10060720 212451 14 3H-5HT -46 4 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 251 7 1 3 2.9 CCCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8214 212451 14 3H-5HT -46 4 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 251 7 1 3 2.9 CCCCc1cc(OC)c(CC(C)N)cc1OC None
None 223229 0 UNDEFINED -8 28 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 322 5 2 3 4.1 CC(CC1=CNC2=C1C=C(C=C2)OCC3=CC=CS3)N.Cl None
24881618 195566 0 UNDEFINED -125 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL505750 195566 0 UNDEFINED -125 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 798 16 4 4 11.2 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
24881619 195817 0 UNDEFINED -9 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL509314 195817 0 UNDEFINED -9 2 Human 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 826 18 4 4 12.0 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
11957541 8241 40 3H-5HT -288 16 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
1229 8241 40 3H-5HT -288 16 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
147 8241 40 3H-5HT -288 16 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
170617 8241 40 3H-5HT -288 16 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
CHEMBL6616 8241 40 3H-5HT -288 16 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 321 4 1 3 2.2 COc1cc(I)c(cc1CC(N)C)OC None
133 9274 52 125I-ICYP -40 43 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 125I-ICYP -40 43 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 125I-ICYP -40 43 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 125I-ICYP -40 43 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 125I-ICYP -40 43 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
206 9271 16 3H-5HT -549 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 3H-5HT -549 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 3H-5HT -549 25 Human 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
123707 223263 0 125I-ICYP -295 3 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 416 9 3 6 1.8 CC1=C(C=C(C=C1)C(CNCCOC2=CC=CC=C2OC)O)S(=O)(=O)N.Cl None
122 8219 9 3H-5HT -5 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 8219 9 3H-5HT -5 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 8219 9 3H-5HT -5 11 Human 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
2865 10915 73 3H-5HT -263 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-5HT -263 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-5HT -263 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-5HT -263 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-5HT -263 53 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
135398737 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5HT -691 90 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2176 9901 68 125I-ICYP -741 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-ICYP -741 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-ICYP -741 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-ICYP -741 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-ICYP -741 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
115 10563 80 125I-CYP 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 10563 80 3H-5HT 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-CYP 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-CYP 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2389 10104 118 3H-5HT -6456 66 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-5HT -6456 66 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-5HT -6456 66 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-5HT -6456 66 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-5HT -6456 66 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1346 6871 117 125I-ICYP -40 9 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
280 6871 117 125I-ICYP -40 9 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
9899402 6871 117 125I-ICYP -40 9 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
CHEMBL9666 6871 117 125I-ICYP -40 9 Rat 6.9 pKi = 6.9 Binding
NoneNone
PDSP KiDatabase 192 2 1 3 1.1 COc1ccccc1N1CCNCC1 None
135398745 9688 112 3H-5HT -162 65 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-5HT -162 65 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-5HT -162 65 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-5HT -162 65 Rat 5.9 pKi = 5.9 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5 6927 72 125I-ICYP -13 53 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-ICYP -13 53 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-ICYP -13 53 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-ICYP -13 53 Rat 7.9 pKi = 7.9 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
180 7189 56 3H-MESULERGINE -281 40 Cat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 3H-MESULERGINE -281 40 Cat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 3H-MESULERGINE -281 40 Cat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 3H-MESULERGINE -281 40 Cat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 3H-MESULERGINE -281 40 Cat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
71299720 222730 0 3H-5HT -44 17 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
127 9900 52 3H-GR-125743 -3388 15 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 9900 52 3H-GR-125743 -3388 15 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 9900 52 3H-GR-125743 -3388 15 Guinea pig 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
2726 7706 68 3H-GR-125743 -54 72 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2726 7706 68 3H-5HT -147 72 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-GR-125743 -54 72 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 3H-5HT -147 72 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-GR-125743 -54 72 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 3H-5HT -147 72 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-GR-125743 -54 72 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 3H-5HT -147 72 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-GR-125743 -54 72 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 3H-5HT -147 72 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
107 6929 121 3H-5HT -30 31 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -30 31 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -30 31 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
5 6927 72 3H-5HT -11 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 125I-ICYP -13 53 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-ICYP -13 53 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-ICYP -13 53 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-ICYP -13 53 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
133 9274 52 3H-GR-125743 -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-GR-125743 -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-GR-125743 -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-GR-125743 -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-GR-125743 -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2220 9908 82 3H-5HT -1023 14 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 9908 82 3H-5HT -1023 14 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 9908 82 3H-5HT -1023 14 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 9908 82 3H-5HT -1023 14 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 9908 82 3H-5HT -1023 14 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
1621 9207 17 125I-CYP -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 125I-CYP -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 125I-CYP -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 125I-CYP -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 125I-CYP -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
11954259 222758 0 3H-GR-125743 -501 43 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 443 5 0 5 3.5 CN1CCN(CC1)CCC=C2C3=CC=CC=C3SC4=C2C=C(C=C4)S(=O)(=O)N(C)C None
2176 9901 68 125I-ICYP -741 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-ICYP -741 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-ICYP -741 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-ICYP -741 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-ICYP -741 27 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
102 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -2691 49 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
134 9292 24 125I-CYP -251 67 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 125I-CYP -251 67 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 125I-CYP -251 67 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 125I-CYP -251 67 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 125I-CYP -251 67 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1342 6824 49 125I-CYP -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
1342 6824 49 3H-5HT -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 125I-CYP -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 3H-5HT -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 125I-CYP -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 3H-5HT -50 19 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
102 10899 48 35S-GTPGammaS -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
102 10899 48 3H-GR-125743 -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 35S-GTPGammaS -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-GR-125743 -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 35S-GTPGammaS -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-GR-125743 -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 35S-GTPGammaS -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-GR-125743 -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 35S-GTPGammaS -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-GR-125743 -64 49 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
1588 9105 27 3H-5-CT -42 44 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 3H-5-CT -42 44 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 3H-5-CT -42 44 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 3H-5-CT -42 44 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 3H-5-CT -42 44 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
24881201 193628 0 UNDEFINED -4 2 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
CHEMBL489453 193628 0 UNDEFINED -4 2 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 526 6 4 4 5.2 CN1CCC(c2c[nH]c3ccc(NC(=O)CC(=O)Nc4ccc5[nH]cc(C6CCN(C)CC6)c5c4)cc23)CC1 None
138107169 222731 0 3H-5HT -141 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-5HT -141 23 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
4106 9280 22 3H-5HT -11 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -11 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -11 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -11 33 Human 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2181 9902 46 3H-Alniditan -70 34 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 3H-Alniditan -70 34 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 3H-Alniditan -70 34 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 3H-Alniditan -70 34 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 3H-Alniditan -70 34 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
277 8083 62 3H-5CT -1905 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-5CT -1905 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-5CT -1905 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-5CT -1905 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-5CT -1905 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
134 9292 24 3H-5HT -14 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -14 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -14 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -14 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -14 67 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
7153 104796 77 3H-5CT -11 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5CT -11 33 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
45266826 224470 0 [3H] 5-CT -2 8 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 177 3 1 2 1.8 CC1=CC=C(C=C1)C(=O)C(C)NC None
133 9274 52 125I-ICYP -40 43 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 125I-ICYP -40 43 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 125I-ICYP -40 43 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 125I-ICYP -40 43 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 125I-ICYP -40 43 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1353 8692 93 3H-GR-125743 -66 85 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-GR-125743 -66 85 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-GR-125743 -66 85 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-GR-125743 -66 85 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-GR-125743 -66 85 Human 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
133 9274 52 125I-ICYP -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 125I-ICYP -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 125I-ICYP -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 125I-ICYP -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 125I-ICYP -40 43 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
165193 222724 0 3H-5HT -154 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -154 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -154 30 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2176 9901 68 125I-CYP -741 27 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-CYP -741 27 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-CYP -741 27 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-CYP -741 27 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-CYP -741 27 Rat 7.8 pKi = 7.8 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1621 9207 17 3H-5HT -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-5HT -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-5HT -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-5HT -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-5HT -97 44 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2543 10479 68 3H-GR-125743 -48 32 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-125743 -48 32 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-125743 -48 32 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-125743 -48 32 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-125743 -48 32 Guinea pig 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
4631 201751 29 125I-ICYP -22 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
CHEMBL546 201751 29 125I-ICYP -22 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
DB01580 201751 29 125I-ICYP -22 7 Rat 6.8 pKi = 6.8 Binding
NoneNone
PDSP KiDatabase 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C None
132787 10203 45 3H-5HT -1000 6 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
26 10203 45 3H-5HT -1000 6 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
32 10203 45 3H-5HT -1000 6 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
CHEMBL49247 10203 45 3H-5HT -1000 6 Rat 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 336 2 0 4 2.7 C1COc2c(O1)cccc2N1CCN(CC1)C1Cc2c(C1)cccc2 None
179 7188 115 3H-5CT -43 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 3H-5CT -43 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 3H-5CT -43 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 3H-5CT -43 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 3H-5CT -43 50 Human 5.8 pKi = 5.8 Binding
NoneNone
PDSP KiDatabase 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
24882268 179336 0 UNDEFINED -11 2 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL448555 179336 0 UNDEFINED -11 2 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 788 15 4 6 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
None 222717 0 3H-5HT -3 21 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
1588 9105 27 3H-GR-125743 -42 44 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 3H-GR-125743 -42 44 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 3H-GR-125743 -42 44 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 3H-GR-125743 -42 44 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 3H-GR-125743 -42 44 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2605 10555 30 3H-5HT -7 10 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 3H-5HT -7 10 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 3H-5HT -7 10 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 3H-5HT -7 10 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 3H-5HT -7 10 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
134 9292 24 125I-ICYP -251 67 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 125I-ICYP -251 67 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 125I-ICYP -251 67 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 125I-ICYP -251 67 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 125I-ICYP -251 67 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
3337 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
164 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
134 9292 24 3H-GR-125743 -158 67 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-GR-125743 -158 67 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-GR-125743 -158 67 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-GR-125743 -158 67 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-GR-125743 -158 67 Guinea pig 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1809 6922 32 3H-5HT -32 37 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -32 37 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -32 37 Rat 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
102 10899 48 3H-5-CT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5-CT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5-CT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5-CT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5-CT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3337 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 213146 27 3H-GR-125743 -74 40 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
173 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1524 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 125I-CYP -512 51 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
1531 9046 69 125I-ICYP -676 16 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
3869 9046 69 125I-ICYP -676 16 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
7207 9046 69 125I-ICYP -676 16 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
CHEMBL429 9046 69 125I-ICYP -676 16 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
DB00598 9046 69 125I-ICYP -676 16 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 328 8 5 4 2.9 CC(CCc1ccccc1)NCC(c1ccc(c(c1)C(=N)O)O)O None
2543 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
11954224 222732 0 125I-CYP -12 59 Rat 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
71299720 222730 0 3H-5HT 1 17 Human 8.7 pKi = 8.7 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
5 6927 72 3H-GR-125743 -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-125743 -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-125743 -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-125743 -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 222717 0 3H-5HT -3 21 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
134 9292 24 3H-GR-125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
134 9292 24 3H-GR125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-GR-125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-GR125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-GR-125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-GR125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-GR-125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-GR125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-GR-125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-GR125743 -14 67 Human 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
5 6927 72 3H-5CT -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5CT -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5CT -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5CT -5 53 Guinea pig 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
132 8058 13 3H-5HT -125 15 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-5HT -125 15 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-5HT -125 15 Mouse 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
124 9755 47 3H-5HT -2 32 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 3H-5HT -2 32 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 3H-5HT -2 32 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 3H-5HT -2 32 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 3H-5HT -2 32 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
None 222725 0 3H-5HT 2 24 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 6927 72 3H-5HT -13 53 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 222717 0 3H-GR-125743 -18 21 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
132 8058 13 125I-ICYP -54 15 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 125I-ICYP -54 15 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 125I-ICYP -54 15 Rat 8.6 pKi = 8.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
71299720 222730 0 3H-5HT 1 17 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
152662 222736 0 125I-CYP 109 7 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
None 222717 0 125I-ICYP -18 21 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
2389 10104 118 3H-Alniditan -93 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-Alniditan -93 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-Alniditan -93 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-Alniditan -93 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-Alniditan -93 66 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
173 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
21163 222709 0 3H-5HT -4 5 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 192 2 4 3 1.1 C1=C2C(=CC(=C1O)O)NC=C2CCN None
2337 10030 77 3H-Alniditan -26 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-Alniditan -26 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-Alniditan -26 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-Alniditan -26 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-Alniditan -26 62 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
164 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
85875 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
CHEMBL8600 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
DB01528 8242 19 3H-5HT -89 10 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 209 4 1 3 1.9 COc1cc(C)c(cc1CC(N)C)OC None
None 223101 0 3H-5HT -69 6 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 390 4 1 4 3.2 C1CN(CCN1CCN2C3=CC=CC=C3NC2=O)C4=CC=C(C=C4)C(F)(F)F None
132 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
135398737 7745 93 3H-5CT -151 90 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5CT -151 90 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5CT -151 90 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5CT -151 90 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5CT -151 90 Human 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
7153 104796 77 3H-5HT -11 33 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -11 33 Human 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
132 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-5HT -602 15 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
102 10899 48 3H-5HT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -64 49 Human 7.7 pKi = 7.7 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
141 8209 35 125I-CYP -25 22 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
6089 8209 35 125I-CYP -25 22 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
CHEMBL12420 8209 35 125I-CYP -25 22 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
DB01488 8209 35 125I-CYP -25 22 Rat 5.7 pKi = 5.7 Binding
NoneNone
PDSP KiDatabase 188 3 1 1 2.3 CN(CCc1c[nH]c2c1cccc2)C None
173 10036 95 125I-ICYP -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 125I-ICYP -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 125I-ICYP -2 23 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
1588 9105 27 125I-CYP -58 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 125I-CYP -58 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 125I-CYP -58 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 125I-CYP -58 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 125I-CYP -58 44 Rat 6.7 pKi = 6.7 Binding
NoneNone
PDSP KiDatabase 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
132 8058 13 3H-GR-125743 -6456 15 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 3H-GR-125743 -6456 15 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 3H-GR-125743 -6456 15 Guinea pig 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
115237 62359 119 3H-Alniditan -93 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-Alniditan -93 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-Alniditan -93 54 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
5 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 6928 49 3H-5HT -8 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 6928 49 3H-5HT -8 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 6928 49 3H-5HT -8 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 6928 49 3H-5HT -8 30 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
15897 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
542051 212879 6 3H-5HT -2630 7 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8569 212879 6 3H-5HT -2630 7 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 237 6 1 3 2.5 CCCc1cc(OC)c(CC(C)N)cc1OC None
127 9900 52 125I-ICYP -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 9900 52 125I-ICYP -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 9900 52 125I-ICYP -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
5 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-CYP -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
15897 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-GR-125743 -95 36 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
115 10563 80 3H-5HT -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT -2 27 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
123686 8762 51 3H-5HT -2630 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
12581 8762 51 3H-5HT -2630 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
CHEMBL11268 8762 51 3H-5HT -2630 9 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 354 9 4 5 1.7 C1=CC=C(C=C1)NC(=O)NCCNCC(COC2=CC=CC=C2C#N)O None
27402 212465 18 3H-5HT -46 6 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
CHEMBL8224 212465 18 3H-5HT -46 6 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 223 5 1 3 2.2 CCc1cc(OC)c(CC(C)N)cc1OC None
173 10036 95 125I-ICYP -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 125I-ICYP -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 125I-ICYP -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
134 9292 24 3H-5HT -14 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -14 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -14 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -14 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -14 67 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
127 9900 52 3H-GR-125743 -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 9900 52 3H-GR-125743 -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 9900 52 3H-GR-125743 -95 15 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
133 9274 52 3H-5HT -40 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5HT -40 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5HT -40 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5HT -40 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5HT -40 43 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135398737 7745 93 3H-5HT -691 90 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5HT -691 90 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5HT -691 90 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5HT -691 90 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5HT -691 90 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
None 222723 0 3H-5HT -229 7 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 455 6 5 5 1.6 CCC(CO)NC(=O)C1CN(C2CC3=CNC4=CC=CC(=C34)C2=C1)C.C(=CC(=O)O)C(=O)O None
138107169 222731 0 3H-5HT -141 23 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-5HT -141 23 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
7153 104796 77 UNDEFINED -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 UNDEFINED -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1524 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-GR-125743 -2511 51 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
7153 104796 77 125I-ICYP -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 125I-ICYP -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
1220 6975 55 3H-5HT -208 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
2601 10552 33 3H-GR-125743 -87 21 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 3H-GR-125743 -87 21 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 3H-GR-125743 -87 21 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 3H-GR-125743 -87 21 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 3H-GR-125743 -87 21 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1220 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
115 10563 80 125I-ICYP 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-ICYP 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-ICYP 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
102 10899 48 3H-5HT -64 49 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -64 49 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -64 49 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -64 49 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -64 49 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
173 10036 95 3H-5HT -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -2 23 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
7153 104796 77 125I-CYP -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 125I-CYP -10 33 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5074 10105 80 3H-GR-125743 -478 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 3H-GR-125743 -478 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 3H-GR-125743 -478 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 3H-GR-125743 -478 30 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
2303 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 3H-5HT -1174 26 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
115 10563 80 3H-5HT 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
1353 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2389 10104 118 3H-5HT -6456 66 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-5HT -6456 66 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-5HT -6456 66 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-5HT -6456 66 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-5HT -6456 66 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
1342 6824 49 125I-CYP -50 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 125I-CYP -50 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 125I-CYP -50 19 Rat 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
165193 222724 0 3H-GR-125743 -11748 30 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-GR-125743 -11748 30 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-GR-125743 -11748 30 Guinea pig 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2543 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-125743 -3 32 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT -2 27 Human 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
133 9274 52 3H-GR-125743 -52 43 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-GR-125743 -52 43 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-GR-125743 -52 43 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-GR-125743 -52 43 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-GR-125743 -52 43 Guinea pig 7.6 pKi = 7.6 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
135 9310 43 125I-ICYP -851 56 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 125I-ICYP -851 56 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 125I-ICYP -851 56 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 125I-ICYP -851 56 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 125I-ICYP -851 56 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2105 9828 37 3H-GR-125743 -100 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 3H-GR-125743 -100 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 3H-GR-125743 -100 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 3H-GR-125743 -100 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 3H-GR-125743 -100 32 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
4452 9538 19 3H-5CT -95499 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
983 9538 19 3H-5CT -95499 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
CHEMBL20734 9538 19 3H-5CT -95499 18 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl None
1220 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
1353 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-Alniditan -66 85 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
135398745 9688 112 3H-5HT -162 65 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-5HT -162 65 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-5HT -162 65 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-5HT -162 65 Rat 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
3337 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 213146 27 3H-GR-125743 -74 40 Human 5.6 pKi = 5.6 Binding
NoneNone
PDSP KiDatabase 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
60820 11080 14 UNDEFINED -144543 12 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 None
CHEMBL10085 11080 14 UNDEFINED -144543 12 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 421 6 0 4 4.4 CC(C)Oc1ccccc1N1CCN(Cc2cccc(C(=O)N3CCCCC3)c2)CC1 None
5074 10105 80 3H-GR-125743 -478 30 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 3H-GR-125743 -478 30 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 3H-GR-125743 -478 30 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 3H-GR-125743 -478 30 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
4209 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 125I-ICYP -4073 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
6437377 222733 0 125I-CYP -2398 5 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 500 6 3 7 3.2 CC(C)N1C=C2CC3C(CC(CN3C)C(=O)OC(C)C(C)O)C4=C2C1=CC=C4.C(=CC(=O)O)C(=O)O None
25058166 222739 0 3H-GR-125743 -1479 26 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
6852389 222739 0 3H-GR-125743 -1479 26 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 267 0 2 3 2.9 CN1CCC2=CC=CC3=C2C1CC4=C3C(=C(C=C4)O)O None
5 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 9280 22 3H-5HT -11 33 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -11 33 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -11 33 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -11 33 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
107780 8625 54 3H-5HT -4 18 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-5HT -4 18 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-5HT -4 18 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
115 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
115 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
1809 6922 32 3H-5HT -32 37 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -32 37 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -32 37 Rat 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2543 10479 68 3H-5HT -3 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.5 pKi = 8.5 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
134 9292 24 3H-5HT -14 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -14 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -14 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -14 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -14 67 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
130 10273 47 3H-GR-125743 1 13 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 10273 47 3H-GR-125743 1 13 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 10273 47 3H-GR-125743 1 13 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
None 222717 0 3H-5HT -18 21 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 222725 0 125I-CYP 2 24 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
None 222725 0 3H-5HT 2 24 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
1621 9207 17 3H-GR-125743 -97 44 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-GR-125743 -97 44 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-GR-125743 -97 44 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-GR-125743 -97 44 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-GR-125743 -97 44 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3036780 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 3H-Alniditan -32 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 222725 0 125I-CYP 2 24 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
6971132 222788 0 3H-5-CT 1 14 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 268 1 2 2 2.1 CN1CC(C=C2C1CC3=CNC4=CC=CC2=C34)C(=O)O None
5 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
130 10273 47 3H-GR-125743 -8 13 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 10273 47 3H-GR-125743 -8 13 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 10273 47 3H-GR-125743 -8 13 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107 6929 121 3H-5HT -30 31 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -30 31 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -30 31 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
165193 222724 0 3H-5HT -154 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -154 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -154 30 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
152662 222736 0 125I-CYP 109 7 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
173 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
173 10036 95 125I-CYP -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
173 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 125I-CYP -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
5011 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 125I-CYP -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
CHEMBL18772 10036 95 3H-5HT -2 23 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 213 1 1 3 1.6 N1CCN(CC1)c1ccc2c(n1)cccc2 None
134 9292 24 3H-GR-125743 -251 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-GR-125743 -251 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-GR-125743 -251 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-GR-125743 -251 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-GR-125743 -251 67 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2220 9908 82 125I-CYP -1023 14 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
27400 9908 82 125I-CYP -1023 14 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
93 9908 82 125I-CYP -1023 14 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
CHEMBL294951 9908 82 125I-CYP -1023 14 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
DB06153 9908 82 125I-CYP -1023 14 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 None
4106 9280 22 3H-GR-125743 -11 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-GR-125743 -11 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-GR-125743 -11 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-GR-125743 -11 33 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
135398745 9688 112 3H-5CT -199 65 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-5CT -199 65 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-5CT -199 65 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-5CT -199 65 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
5311189 211620 11 3H-GR-125743 -35 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
CHEMBL7549 211620 11 3H-GR-125743 -35 27 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 219 3 1 2 3.0 CCCN1CCC[C@@H](c2cccc(O)c2)C1 None
24881686 195168 0 UNDEFINED -8 2 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL501645 195168 0 UNDEFINED -8 2 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 832 18 4 7 8.5 O=C(Nc1ccc2[nH]cc(C3CCN(CCOCCOCCOCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
71299720 222730 0 125I-ICYP -44 17 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
None 222725 0 3H-GR-125743 -22 24 Guinea pig 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
5 6927 72 125I-ICYP -13 53 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-ICYP -13 53 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-ICYP -13 53 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-ICYP -13 53 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
145 6928 49 3H-5HT -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 6928 49 3H-5HT -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 6928 49 3H-5HT -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 6928 49 3H-5HT -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
None 223018 0 3H-GR-125743 -4677 29 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
115237 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
135398737 7745 93 3H-5HT -691 90 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-5HT -691 90 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-5HT -691 90 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-5HT -691 90 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-5HT -691 90 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
107 6929 121 3H-5HT -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1212 8443 50 3H-GR-125743 -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 3H-GR-125743 -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 3H-GR-125743 -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 3H-GR-125743 -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 3H-GR-125743 -93 65 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
7153 104796 77 125I-CYP -10 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
7153 104796 77 3H-5HT -10 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 125I-CYP -10 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -10 33 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
446220 140299 14 3H-GR-125743 -23 45 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 3H-GR-125743 -23 45 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
2176 9901 68 3H-5HT -741 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-5HT -741 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-5HT -741 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-5HT -741 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-5HT -741 27 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
15897 9637 0 3H-GR-125743 -95 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
215 9637 0 3H-GR-125743 -95 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
CHEMBL1979333 9637 0 3H-GR-125743 -95 36 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 203 2 1 1 2.6 CC(Cc1cccc(c1)C(F)(F)F)N None
107 6929 121 3H-GR-125743 -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-125743 -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-125743 -16 31 Human 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
None 222729 0 125I-ICYP - 1 Rat 7.5 pKi = 7.5 Binding
NoneNone
PDSP KiDatabase 310 7 2 4 2.6 CC(C)NCC(COC1=CC=CC=C1N2C=CC=C2)O.Cl None
115237 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 3H-5HT -14454 54 Rat 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
119570 9933 96 3H-GR-125743 -398 39 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-GR-125743 -398 39 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-GR-125743 -398 39 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-GR-125743 -398 39 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-GR-125743 -398 39 Human 5.5 pKi = 5.5 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
145 6928 49 125I-ICYP -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 6928 49 125I-ICYP -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 6928 49 125I-ICYP -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 6928 49 125I-ICYP -47 30 Rat 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
11831220 199337 8 UNDEFINED -8 2 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 None
CHEMBL521235 199337 8 UNDEFINED -8 2 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 229 1 2 2 2.6 CN1CCC(c2c[nH]c3ccc(N)cc23)CC1 None
31101 7516 40 3H-GR-125743 -128 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 3H-GR-125743 -128 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 3H-GR-125743 -128 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 3H-GR-125743 -128 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 3H-GR-125743 -128 35 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
133 9274 52 3H-5HT -23 43 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5HT -23 43 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5HT -23 43 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5HT -23 43 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5HT -23 43 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
165193 222724 0 3H-GR-125743 -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-GR-125743 -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-GR-125743 -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
7153 104796 77 3H-5HT -11 33 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -11 33 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
2181 9902 46 3H-5HT -3090 34 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 3H-5HT -3090 34 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 3H-5HT -3090 34 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 3H-5HT -3090 34 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 3H-5HT -3090 34 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4595 183494 106 3H-Serotonin -7 14 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 183494 106 3H-Serotonin -7 14 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
5074 10105 80 3H-GR-125743 -645 30 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 3H-GR-125743 -645 30 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 3H-GR-125743 -645 30 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 3H-GR-125743 -645 30 Guinea pig 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5 6927 72 3H-GR-125743 -11 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-125743 -11 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-125743 -11 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-125743 -11 53 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107 6929 121 3H-GR-125743 -16 31 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-GR-125743 -16 31 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-GR-125743 -16 31 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1220 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
24882266 195066 0 UNDEFINED -2 2 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL500230 195066 0 UNDEFINED -2 2 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 812 17 4 4 11.6 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
1220 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
134 9292 24 125I-ICYP -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 125I-ICYP -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 125I-ICYP -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 125I-ICYP -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 125I-ICYP -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1613 9127 53 3H-GR-125743 -13 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 3H-GR-125743 -13 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 3H-GR-125743 -13 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 3H-GR-125743 -13 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 3H-GR-125743 -13 44 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3682 196216 12 125I-ICYP -7585 8 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL1256784 196216 12 125I-ICYP -7585 8 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
CHEMBL513389 196216 12 125I-ICYP -7585 8 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 277 6 2 3 2.6 Cc1ccc(OCC(O)C(C)NC(C)C)c2c1CCC2 None
1621 9207 17 125I-ICYP -97 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 125I-ICYP -97 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 125I-ICYP -97 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 125I-ICYP -97 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 125I-ICYP -97 44 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
165193 222724 0 125I-ICYP -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-ICYP -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-ICYP -154 30 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
1342 6824 49 125I-ICYP -50 19 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 125I-ICYP -50 19 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 125I-ICYP -50 19 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
5 6927 72 3H-5HT -41 53 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -41 53 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -41 53 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -41 53 Mouse 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4106 9280 22 3H-5HT -11 33 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -11 33 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -11 33 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -11 33 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
2543 10479 68 3H-GR-125743 -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-125743 -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-125743 -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-125743 -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-125743 -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
138107169 222731 0 3H-5HT -141 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-5HT -141 23 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
135398737 7745 93 3H-Alniditan -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-Alniditan -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-Alniditan -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-Alniditan -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-Alniditan -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
202 8290 77 3H-5HT -1 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 8290 77 3H-5HT -1 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 8290 77 3H-5HT -1 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 8290 77 3H-5HT -1 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 8290 77 3H-5HT -1 33 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
107 6929 121 125I-CYP -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
107 6929 121 3H-5HT -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 125I-CYP -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 125I-CYP -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -30 31 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
135398737 7745 93 3H-GR-125743 -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-GR-125743 -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-GR-125743 -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-GR-125743 -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-GR-125743 -151 90 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
1809 6922 32 125I-ICYP -32 37 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-ICYP -32 37 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-ICYP -32 37 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107 6929 121 125I-ICYP -30 31 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 125I-ICYP -30 31 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 125I-ICYP -30 31 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2865 10915 73 3H-GR-125743 -12 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-GR-125743 -12 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-GR-125743 -12 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-GR-125743 -12 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-GR-125743 -12 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
None 222725 0 125I-ICYP 2 24 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
1809 6922 32 3H-5HT -15 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
5 6927 72 35S-GTPGammaS -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 35S-GTPGammaS -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 35S-GTPGammaS -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 35S-GTPGammaS -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
None 222717 0 125I-ICYP -18 21 Rat 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 583 4 3 6 2.1 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CC6C(CC7=CNC8=CC=CC6=C78)N(C5)C None
None 223123 0 3H-GR-125743 26 2 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 338 6 3 5 1.7 C1CNC(=NC1)NCCCNCC2CCC3=CC=CC=C3O2.Cl None
5 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -11 53 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107780 8625 54 3H-GR-125743 -4 18 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-GR-125743 -4 18 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-GR-125743 -4 18 Guinea pig 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107780 8625 54 3H-GR-125743 1 18 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-GR-125743 1 18 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-GR-125743 1 18 Human 8.4 pKi = 8.4 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
441383 27105 57 None -19 17 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL1306 27105 57 None -19 17 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
176 7186 66 None -10 31 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2157 7186 66 None -10 31 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
2566 7186 66 None -10 31 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
CHEMBL633 7186 66 None -10 31 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
DB01118 7186 66 None -10 31 Rat 8.4 pKi = 8.4 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 645 11 0 4 6.9 CCCCc1oc2c(c1C(=O)c1cc(I)c(c(c1)I)OCCN(CC)CC)cccc2 None
11954224 222732 0 3H-GR-125743 -32 59 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
31703 201496 63 None -2 3 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL359744 201496 63 None -2 3 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
CHEMBL53463 201496 63 None -2 3 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 None
107 6929 121 3H-5HT -16 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 3H-5HT -16 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 3H-5HT -16 31 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
2812 11551 101 None -51 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
CHEMBL104 11551 101 None -51 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 344 4 0 2 5.4 Clc1ccccc1C(c1ccccc1)(c1ccccc1)n1ccnc1 None
None 222725 0 125I-ICYP 2 24 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 346 5 4 4 2.5 COC1=CC2=C(C=C1)NC=C2C3=CCNCC3.C(CC(=O)O)C(=O)O None
133 9274 52 125I-CYP -40 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 125I-CYP -40 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 125I-CYP -40 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 125I-CYP -40 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 125I-CYP -40 43 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
102 10899 48 3H-5HT -64 49 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -64 49 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -64 49 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -64 49 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -64 49 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2389 10104 118 3H-5HT -6456 66 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-5HT -6456 66 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-5HT -6456 66 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-5HT -6456 66 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-5HT -6456 66 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
135409468 8816 69 3H-GR-125743 -144 39 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
333 8816 69 3H-GR-125743 -144 39 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
CHEMBL845 8816 69 3H-GR-125743 -144 39 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 312 1 2 4 1.7 Clc1ccc2c(c1)NC(=c1c(=N2)cccc1)N1CCNCC1 None
5281600 209804 92 3H-GR-125743 -173 32 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
CHEMBL63354 209804 92 3H-GR-125743 -173 32 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 538 3 6 10 5.1 O=c1cc(-c2ccc(O)c(-c3c(O)cc(O)c4c(=O)cc(-c5ccc(O)cc5)oc34)c2)oc2cc(O)cc(O)c12 None
122 8219 9 3H-5HT -5 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
156314 8219 9 3H-5HT -5 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL1332062 8219 9 3H-5HT -5 11 Human 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N None
2176 9901 68 3H-5HT -1737 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-5HT -1737 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-5HT -1737 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-5HT -1737 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-5HT -1737 27 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
182596 125264 16 3H-5HT -269 3 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
CHEMBL341391 125264 16 3H-5HT -269 3 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 364 4 0 4 3.7 c1ccc2c(c1)CCC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
1978 7038 60 125I-ICYP -645 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
40 7038 60 125I-ICYP -645 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
7107 7038 60 125I-ICYP -645 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
CHEMBL642 7038 60 125I-ICYP -645 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
DB01193 7038 60 125I-ICYP -645 6 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 336 10 3 5 3.0 CCCC(=Nc1ccc(c(c1)C(=O)C)OCC(CNC(C)C)O)O None
182585 22219 15 3H-5HT -1 4 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 None
CHEMBL12152 22219 15 3H-5HT -1 4 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 386 7 1 5 2.9 O=C1CC2(CCCC2)CC(=O)N1CCCCNCC1COc2ccccc2O1 None
2142 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 125I-CYP -741 37 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4106 9280 22 125I-ICYP -102 33 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-ICYP -102 33 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-ICYP -102 33 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-ICYP -102 33 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
103 10925 61 3H-5CT -48 53 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-5CT -48 53 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-5CT -48 53 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-5CT -48 53 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-5CT -48 53 Human 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1524 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 3H-GR-125743 -2511 51 Human 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
134 9292 24 3H-5HT -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -251 67 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2543 10479 68 3H-5HT -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 10563 80 125I-CYP 1 27 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-CYP 1 27 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-CYP 1 27 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2543 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
44668 222721 0 3H-5HT -1 4 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 228 3 2 1 3.1 C1CNCCC1CCC2=CNC3=CC=CC=C32 None
138107169 222731 0 3H-5HT -19054 23 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-5HT -19054 23 Rat 5.4 pKi = 5.4 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
2543 10479 68 125I-CYP -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 125I-CYP -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 125I-CYP -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 125I-CYP -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 125I-CYP -17 32 Rat 6.4 pKi = 6.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -17 32 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 10563 80 3H-5HT 1 27 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 7.4 pKi = 7.4 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
107 6929 121 125I-ICYP -30 31 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
1833 6929 121 125I-ICYP -30 31 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
CHEMBL8165 6929 121 125I-ICYP -30 31 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 None
152662 222736 0 3H-5HT 109 7 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 276 5 3 3 2.6 CC1=CC2=C(N1)C=CC=C2OCC(CNC(C)(C)C)O None
24881687 179593 0 UNDEFINED -3 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL451394 179593 0 UNDEFINED -3 2 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 776 10 4 4 10.2 O=C(Nc1ccc2[nH]cc(C3CCN(Cc4cccc(CN5CCC(c6c[nH]c7ccc(NC(=O)c8ccc(F)cc8)cc67)CC5)c4)CC3)c2c1)c1ccc(F)cc1 None
138107169 222731 0 3H-5HT -141 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 3H-5HT -141 23 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
165193 222724 0 125I-CYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
165193 222724 0 3H-5HT -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-CYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-CYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
2543 10479 68 125I-ICYP -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 10479 68 3H-5HT -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 125I-ICYP -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 125I-ICYP -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 125I-ICYP -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 125I-ICYP -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -17 32 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
135 9310 43 3H-5HT -851 56 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 3H-5HT -851 56 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 3H-5HT -851 56 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 3H-5HT -851 56 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 3H-5HT -851 56 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2176 9901 68 3H-5HT -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-5HT -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-5HT -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-5HT -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-5HT -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
None 223120 0 3H-GR-125743 -630 19 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 451 8 2 4 3.2 CCNC(=O)N(CCCN(C)C)C(=O)C1CC2C(CC3=CNC4=CC=CC2=C34)N(C1)CC=C None
277 8083 62 125I-CYP -501 50 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 125I-CYP -501 50 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 125I-CYP -501 50 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 125I-CYP -501 50 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 125I-CYP -501 50 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2470 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3198 212292 76 None -44 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL1201049 212292 76 None -44 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
CHEMBL808 212292 76 None -44 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 380 6 0 3 5.8 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)cc1 None
102 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
165193 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
102 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5HT -64 49 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
165193 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -154 30 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
4189 213701 96 None -41 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL1559 213701 96 None -41 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
CHEMBL91 213701 96 None -41 34 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 414 6 0 3 6.5 Clc1ccc(COC(Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 None
1884 9512 58 3H-GR-125743 -3 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 9512 58 3H-GR-125743 -3 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 9512 58 3H-GR-125743 -3 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 9512 58 3H-GR-125743 -3 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 9512 58 3H-GR-125743 -3 5 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
1809 6922 32 3H-5HT -15 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -15 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -15 37 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 125I-CYP -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
1809 6922 32 3H-5HT -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-CYP -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-5HT -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-CYP -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-5HT -32 37 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
3036780 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 3H-GR-125743 -32 53 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
3823 56995 42 None -38 11 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 56995 42 None -38 11 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 56995 42 None -38 11 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
5 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
133 9274 52 3H-5HT -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5HT -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5HT -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5HT -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5HT -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
132 8058 13 125I-CYP -54 15 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 125I-CYP -54 15 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 125I-CYP -54 15 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2470 10425 50 None -43651 58 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 None -43651 58 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 None -43651 58 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 None -43651 58 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 None -43651 58 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
135 9310 43 None -851 56 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -851 56 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -851 56 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -851 56 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -851 56 Rat 8.3 pKi = 8.3 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
5 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
4595 183494 106 None -7 14 Rat 8.3 pKi = 8.3 Binding
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
CHEMBL46 183494 106 None -7 14 Rat 8.3 pKi = 8.3 Binding
The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.The binding affinity was measured on 5-hydroxytryptamine 1B receptor using [3H]- serotonin as radioligand.
Drug Central 293 2 0 4 3.1 Cc1nccn1CC1CCc2c(c3ccccc3n2C)C1=O None
446220 140299 14 None -23 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
CHEMBL370805 140299 14 None -23 45 Human 8.3 pKi = 8.3 Binding
NoneNone
Drug Central 303 3 0 5 1.9 COC(=O)[C@H]1[C@@H](OC(=O)c2ccccc2)C[C@@H]2CC[C@H]1N2C None
133 9274 52 3H-GR-125743 -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-GR-125743 -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-GR-125743 -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-GR-125743 -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-GR-125743 -23 43 Human 8.3 pKi = 8.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
3117 214620 103 None -3 16 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
CHEMBL964 214620 103 None -3 16 Rat 8.3 pKi = 8.3 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC None
4106 9280 22 3H-GR-125743 -11 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-GR-125743 -11 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-GR-125743 -11 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-GR-125743 -11 33 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
1524 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 None -512 51 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
66265 100788 15 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL248702 100788 15 None -1 19 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCN[C@@H](C)Cc1cccc(C(F)(F)F)c1 None
2726 7706 68 None -147 72 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -147 72 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -147 72 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -147 72 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -147 72 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
2605 10555 30 3H-GR-125743 -7 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
36920 10555 30 3H-GR-125743 -7 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
571 10555 30 3H-GR-125743 -7 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
CHEMBL434200 10555 30 3H-GR-125743 -7 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
DB13775 10555 30 3H-GR-125743 -7 10 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 295 5 2 4 2.9 OC(COc1cccc2c1SCCC2)CNC(C)(C)C None
180 7189 56 None -389 40 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 None -389 40 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 None -389 40 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 None -389 40 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 None -389 40 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2337 10030 77 None -26 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 None -26 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 None -26 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 None -26 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 None -26 62 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2726 7706 68 None -54 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
621 7706 68 None -54 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
83 7706 68 None -54 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL71 7706 68 None -54 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
DB00477 7706 68 None -54 72 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C None
1971 9641 38 None -18 30 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
2404 9641 38 None -18 30 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
4543 9641 38 None -18 30 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
CHEMBL445 9641 38 None -18 30 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
DB00540 9641 38 None -18 30 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 None
3191 109635 97 None -17 25 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
CHEMBL305660 109635 97 None -17 25 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
DB11742 109635 97 None -17 25 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 None
6761 74574 19 None -43 18 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
CHEMBL1909072 74574 19 None -43 18 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 401 5 1 4 4.5 NC(=O)C1CCN(CCCN2c3ccccc3Sc3ccc(Cl)cc32)CC1 None
277 8083 62 None -501 50 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 None -501 50 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 None -501 50 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 None -501 50 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 None -501 50 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2274 9947 58 None -39 31 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
4917 9947 58 None -39 31 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
7279 9947 58 None -39 31 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
CHEMBL728 9947 58 None -39 31 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
DB00433 9947 58 None -39 31 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 None
1222 8445 49 None -134 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 None -134 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 None -134 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 None -134 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 None -134 32 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
4106 9280 22 3H-5HT -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 3H-5HT -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 3H-5HT -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 3H-5HT -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
102 10899 48 3H-5CT -125 49 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 3H-5CT -125 49 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 3H-5CT -125 49 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 3H-5CT -125 49 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 3H-5CT -125 49 Guinea pig 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3652 10869 79 3H-5HT -3 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 10869 79 3H-5HT -3 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 10869 79 3H-5HT -3 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 10869 79 3H-5HT -3 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 10869 79 3H-5HT -3 18 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
1222 8445 49 3H-5HT -8317 32 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3396 8445 49 3H-5HT -8317 32 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
85 8445 49 3H-5HT -8317 32 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL46516 8445 49 3H-5HT -8317 32 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
DB04842 8445 49 3H-5HT -8317 32 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 475 7 1 3 5.3 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
1353 8692 93 3H-5HT -5248 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 3H-5HT -5248 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 3H-5HT -5248 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 3H-5HT -5248 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 3H-5HT -5248 85 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2337 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
2435 10362 83 3H-5CT -128 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-5CT -128 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-5CT -128 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-5CT -128 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-5CT -128 48 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
7153 104796 77 3H-5HT -11 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -11 33 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
68604 84980 29 125I-CYP -11748 5 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 None
CHEMBL2105437 84980 29 125I-CYP -11748 5 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 401 5 0 6 2.9 Cc1nc2n(c(=O)c1CCN1CCC(C(=O)c3ccc(F)cc3)CC1)CCS2 None
135398745 9688 112 3H-GR-125743 -199 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-GR-125743 -199 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-GR-125743 -199 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-GR-125743 -199 65 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1574 6869 60 3H-5HT -8 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 3H-5HT -8 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 3H-5HT -8 21 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2176 9901 68 125I-CYP -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-CYP -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-CYP -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-CYP -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-CYP -741 27 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
10257 7525 31 3H-5HT -141 19 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 7525 31 3H-5HT -141 19 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 7525 31 3H-5HT -141 19 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 7525 31 3H-5HT -141 19 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
133 9274 52 3H-5HT -40 43 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-5HT -40 43 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-5HT -40 43 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-5HT -40 43 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-5HT -40 43 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
103 10925 61 3H-Alniditan -48 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-Alniditan -48 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-Alniditan -48 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-Alniditan -48 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-Alniditan -48 53 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3025067 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
4106 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
4106 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-CYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
134 9292 24 3H-5HT -251 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -251 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -251 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -251 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -251 67 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2435 10362 83 3H-5HT -1023 48 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-5HT -1023 48 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-5HT -1023 48 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-5HT -1023 48 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-5HT -1023 48 Rat 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
1150 10650 121 3H-5HT -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 10650 121 3H-5HT -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 10650 121 3H-5HT -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 10650 121 3H-5HT -7 25 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
2389 10104 118 3H-GR-125743 -93 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-GR-125743 -93 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-GR-125743 -93 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-GR-125743 -93 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-GR-125743 -93 66 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
3025067 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
65853 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
CHEMBL282614 106158 64 3H-5HT -2 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 220 1 1 4 0.9 c1cc2c(c(N3CCNCC3)c1)OCCO2 None
2470 10425 50 125I-CYP -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2470 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 125I-CYP -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 125I-CYP -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 125I-CYP -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 125I-CYP -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5HT -43651 58 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
115 10563 80 125I-ICYP 1 27 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-ICYP 1 27 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-ICYP 1 27 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
2337 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
50 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
5002 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
CHEMBL716 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
DB01224 10030 77 3H-5HT -575 62 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 None
18971832 9196 0 3H-5HT -85 13 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
21 9196 0 3H-5HT -85 13 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
CHEMBL3186179 9196 0 3H-5HT -85 13 Human 6.3 pKi = 6.3 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C None
3036780 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 3H-5HT -363 53 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
4106 9280 22 125I-ICYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-ICYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-ICYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-ICYP -102 33 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
132 8058 13 125I-CYP -54 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
155346 8058 13 125I-CYP -54 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
CHEMBL378501 8058 13 125I-CYP -54 15 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 None
2303 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 3H-5HT -1174 26 Human 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
165193 222724 0 125I-ICYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-ICYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-ICYP -154 30 Rat 7.3 pKi = 7.3 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
283 9904 57 125I-CYP -6606 12 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 9904 57 125I-CYP -6606 12 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 9904 57 125I-CYP -6606 12 Rat 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
165193 222724 0 125I-ICYP -154 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-ICYP -154 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-ICYP -154 30 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
5074 10105 80 125I-ICYP -4168 30 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
97 10105 80 125I-ICYP -4168 30 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
CHEMBL267777 10105 80 125I-ICYP -4168 30 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
DB12693 10105 80 125I-ICYP -4168 30 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 477 5 0 5 5.5 Fc1ccc(cc1)C(=C1CCN(CC1)CCc1c(C)nc2n(c1=O)ccs2)c1ccc(cc1)F None
5475158 73987 25 125I-CYP -1023 14 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 73987 25 125I-CYP -1023 14 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
2865 10915 73 3H-5CT -12 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 3H-5CT -12 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 3H-5CT -12 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 3H-5CT -12 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 3H-5CT -12 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
2176 9901 68 125I-ICYP -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-ICYP -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-ICYP -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-ICYP -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-ICYP -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2176 9901 68 125I-ICYP -741 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-ICYP -741 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-ICYP -741 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-ICYP -741 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-ICYP -741 27 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1809 6922 32 3H-GR-125743 -15 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 3H-GR-125743 -15 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 3H-GR-125743 -15 37 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
107780 8625 54 3H-GR-125743 -4 18 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 3H-GR-125743 -4 18 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 3H-GR-125743 -4 18 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
1212 8443 50 None -144 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -144 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -144 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -144 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -144 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
2351 10059 64 None -10 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
2820 10059 64 None -10 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
5035 10059 64 None -10 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
CHEMBL81 10059 64 None -10 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
DB00481 10059 64 None -10 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 473 7 2 6 6.1 Oc1ccc2c(c1)sc(c2C(=O)c1ccc(cc1)OCCN1CCCCC1)c1ccc(cc1)O None
213 10625 55 None -6 43 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
2717 10625 55 None -6 43 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
5533 10625 55 None -6 43 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
CHEMBL621 10625 55 None -6 43 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
DB00656 10625 55 None -6 43 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 None
242 7258 124 None -380 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 None -380 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 None -380 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 None -380 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 None -380 51 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
49831411 224525 0 None 1 15 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 659 19 0 6 8.7 CCCCCCCCCCCC(=O)OCN1C(=O)CCC2=CC=C(OCCCCN3CCN(CC3)C3=C(Cl)C(Cl)=CC=C3)C=C12 None
2247 7293 81 None -35 42 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
249 7293 81 None -35 42 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
2603 7293 81 None -35 42 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
CHEMBL296419 7293 81 None -35 42 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
DB00637 7293 81 None -35 42 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 None
135398737 7745 93 None -151 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 None -151 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 None -151 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 None -151 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 None -151 90 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
2181 9902 46 None -70 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
4830 9902 46 None -70 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
92 9902 46 None -70 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
CHEMBL440294 9902 46 None -70 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
DB09286 9902 46 None -70 34 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N None
2303 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 None -1174 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
2585 7590 103 None -100 22 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
522 7590 103 None -100 22 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
551 7590 103 None -100 22 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
CHEMBL723 7590 103 None -100 22 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
DB01136 7590 103 None -100 22 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O None
135398745 9688 112 None -199 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -199 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -199 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -199 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
37 7565 60 None -22 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
460 7565 60 None -22 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
54746 7565 60 None -22 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
CHEMBL1201087 7565 60 None -22 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
DB00248 7565 60 None -22 17 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C None
135398745 9688 112 None -162 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 None -162 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 None -162 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 None -162 65 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
1613 9127 53 None -13 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
205 9127 53 None -13 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
3964 9127 53 None -13 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
CHEMBL831 9127 53 None -13 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
DB00408 9127 53 None -13 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 None
1212 8443 50 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
204 8443 50 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3372 8443 50 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
CHEMBL726 8443 50 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
DB00623 8443 50 None -93 65 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 437 6 1 5 4.3 OCCN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F None
3389 224490 0 None -1 26 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 549 12 0 6 6.8 CCCCCCC(=O)OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(C=C3)C(F)(F)F)CC1 None
31101 7516 40 None -128 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 None -128 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 None -128 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 None -128 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 None -128 35 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
1353 8692 93 None -66 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 None -66 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 None -66 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 None -66 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 None -66 85 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
2601 10552 33 None -87 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
443951 10552 33 None -87 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
56 10552 33 None -87 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL73151 10552 33 None -87 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
DB13399 10552 33 None -87 21 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC None
1621 9207 17 3H-5HT -97 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
17 9207 17 3H-5HT -97 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
5761 9207 17 3H-5HT -97 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL263881 9207 17 3H-5HT -97 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB04829 9207 17 3H-5HT -97 44 Rat 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 323 3 1 2 2.9 CCN(C(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
26987 7736 33 None -138 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
6063 7736 33 None -138 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
671 7736 33 None -138 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
CHEMBL1626 7736 33 None -138 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
DB00283 7736 33 None -138 21 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 343 6 0 2 5.1 Clc1ccc(cc1)[C@@](c1ccccc1)(OCC[C@H]1CCCN1C)C None
212 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2639 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
941651 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
CHEMBL1201 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
DB01623 10578 47 None -6 25 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C None
2393 10107 82 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
5078 10107 82 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
51 10107 82 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
CHEMBL905 10107 82 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
DB00953 10107 82 None -1 5 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C None
130 10273 47 35S-GTPGammaS -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3378093 10273 47 35S-GTPGammaS -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL281350 10273 47 35S-GTPGammaS -1 13 Human 8.2 pKi = 8.2 Binding
NoneNone
PDSP KiDatabase 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
100 10577 58 None -13 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
2637 10577 58 None -13 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
5452 10577 58 None -13 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
CHEMBL479 10577 58 None -13 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
DB00679 10577 58 None -13 54 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 None
134 9292 24 None -251 67 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 None -251 67 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 None -251 67 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 None -251 67 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 None -251 67 Rat 8.2 pKi = 8.2 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
2435 10362 83 3H-Alniditan -128 48 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 3H-Alniditan -128 48 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 3H-Alniditan -128 48 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 3H-Alniditan -128 48 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 3H-Alniditan -128 48 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2543 10479 68 3H-GR-125743 -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-GR-125743 -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-GR-125743 -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-GR-125743 -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-GR-125743 -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115 10563 80 3H-5HT 1 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT 1 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT 1 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
182595 26709 14 3H-5HT -1000 4 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
CHEMBL130276 26709 14 3H-5HT -1000 4 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 350 4 0 4 3.3 c1ccc2c(c1)CC2CCN1CCN(c2cccc3c2OCCO3)CC1 None
1220 6975 55 125I-CYP -7413 44 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 125I-CYP -7413 44 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 125I-CYP -7413 44 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 125I-CYP -7413 44 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
3151 8244 97 125I-CYP -7762 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
945 8244 97 125I-CYP -7762 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
965 8244 97 125I-CYP -7762 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
CHEMBL219916 8244 97 125I-CYP -7762 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
DB01184 8244 97 125I-CYP -7762 26 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 None
2176 9901 68 3H-5HT -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-5HT -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-5HT -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-5HT -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-5HT -741 27 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2543 10479 68 3H-5HT -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1209 8439 75 3H-5HT -1148 32 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
203 8439 75 3H-5HT -1148 32 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
3386 8439 75 3H-5HT -1148 32 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
CHEMBL41 8439 75 3H-5HT -1148 32 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
DB00472 8439 75 3H-5HT -1148 32 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F None
None 222750 0 3H-8-OH-DPAT -1348 15 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 473 7 0 5 3.5 COC1=CC=CC=C1N2CCN(CC2)CCCCN3C(=O)C4=CC=CC=C4C3=O.Br None
135 9310 43 125I-CYP -851 56 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 125I-CYP -851 56 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 125I-CYP -851 56 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 125I-CYP -851 56 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 125I-CYP -851 56 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
21163 222709 0 125I-CYP -4 5 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 192 2 4 3 1.1 C1=C2C(=CC(=C1O)O)NC=C2CCN None
5475158 73987 25 3H-5HT -1023 14 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
CHEMBL18786 73987 25 3H-5HT -1023 14 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 340 8 1 3 4.4 CN(C)CCCSc1ccccc1NC(=O)/C=C/c1ccccc1 None
2176 9901 68 3H-5HT -199 27 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 3H-5HT -199 27 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 3H-5HT -199 27 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 3H-5HT -199 27 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 3H-5HT -199 27 Mouse 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
1220 6975 55 3H-5HT -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
206 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
2303 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 3H-5HT -1174 26 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
138107169 222731 0 125I-ICYP -19054 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 125I-ICYP -19054 23 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
None 222993 0 3H-5HT -562 14 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 438 5 1 4 4.8 C1CC(CCC1CCN2CCC3=C(C2)C=CC(=C3)C#N)NC(=O)C4=CC=NC5=CC=CC=C45 None
88747 211257 128 125I-CYP -4 5 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 164 1 1 4 -0.1 c1cnc(N2CCNCC2)nc1 None
CHEMBL724 211257 128 125I-CYP -4 5 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 164 1 1 4 -0.1 c1cnc(N2CCNCC2)nc1 None
115 10563 80 3H-5HT -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 3H-5HT -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 3H-5HT -2 27 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
71299720 222730 0 3H-GR-125743 -51 17 Guinea pig 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
127 9900 52 125I-CYP -95 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 9900 52 125I-CYP -95 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 9900 52 125I-CYP -95 15 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
206 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
68848 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
CHEMBL12314 9271 16 3H-5HT -549 25 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 362 3 1 4 1.3 CN1C[C@H](C[C@H]2[C@H]1Cc1cn(c3c1c2ccc3)C)NS(=O)(=O)N(C)C None
165193 222724 0 3H-5HT -1000 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5HT -1000 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5HT -1000 30 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
21830793 98610 10 3H-8-OH-DPAT -4265 46 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
CHEMBL2413154 98610 10 3H-8-OH-DPAT -4265 46 Bovine 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 373 7 0 8 0.6 COc1ccccc1N1CCN(CCCCn2ncc(=O)n(C)c2=O)CC1 None
135398737 7745 93 3H-Alniditan -151 90 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
38 7745 93 3H-Alniditan -151 90 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
722 7745 93 3H-Alniditan -151 90 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
CHEMBL42 7745 93 3H-Alniditan -151 90 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
DB00363 7745 93 3H-Alniditan -151 90 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 None
71299720 222730 0 3H-GR-125743 -44 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
135398745 9688 112 3H-Alniditan -199 65 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
47 9688 112 3H-Alniditan -199 65 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
CHEMBL715 9688 112 3H-Alniditan -199 65 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
DB00334 9688 112 3H-Alniditan -199 65 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C None
283 9904 57 3H-5HT -6606 12 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
4847 9904 57 3H-5HT -6606 12 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
CHEMBL18331 9904 57 3H-5HT -6606 12 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 393 5 0 5 3.3 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCc1c(C)nc2n(c1=O)cccc2 None
103 10925 61 3H-GR-125743 -48 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-GR-125743 -48 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-GR-125743 -48 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-GR-125743 -48 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-GR-125743 -48 53 Human 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
3036780 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 3H-5HT -363 53 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
None 222718 0 3H-5HT -218 6 Rat 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 370 6 2 7 2.1 CC(C1=CC=CC2=NC3=C(C=CC=C3N=C21)C(=O)O)OC(=O)C(CO)OC None
6917970 10463 61 3H-GR-125743 -1584 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
8370 10463 61 3H-GR-125743 -1584 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
CHEMBL487387 10463 61 3H-GR-125743 -1584 33 Human 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 327 2 2 5 2.8 COc1cc2CCN3[C@H](c2cc1O)Cc1c(C3)c(OC)c(cc1)O None
3294 8787 111 None -57 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 None -57 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 None -57 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 None -57 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 None -57 44 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2176 9901 68 None -741 27 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 None -741 27 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 None -741 27 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 None -741 27 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 None -741 27 Rat 8.2 pKi = 8.2 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
2176 9901 68 None -1737 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 None -1737 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 None -1737 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 None -1737 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 None -1737 27 Human 8.2 pKi = 8.2 Binding
NoneNone
Drug Central 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
133 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -23 43 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
103 10925 61 None -48 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 None -48 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 None -48 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 None -48 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 None -48 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
1809 6922 32 125I-ICYP -32 37 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
4 6922 32 125I-ICYP -32 37 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
CHEMBL18840 6922 32 125I-ICYP -32 37 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N None
2435 10362 83 None -128 48 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
60149 10362 83 None -128 48 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
98 10362 83 None -128 48 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
CHEMBL12713 10362 83 None -128 48 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
DB06144 10362 83 None -128 48 Human 8.1 pKi = 8.1 Binding
Ability to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptorAbility to displace [3H]5-CT (1.5 nM) from HeLa cells of human 5-hydroxytryptamine 1B receptor
Drug Central 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O None
2303 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 None -57 26 Rat 8.1 pKi = 8.1 Binding
Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.Inhibitory activity against 5-hydroxytryptamine 1B receptor of rat striatal membrane homogenate using [3H]5-HT as the radioligand.
Drug Central 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
3652 10869 79 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
57 10869 79 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
60809 10869 79 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
CHEMBL21536 10869 79 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
DB15357 10869 79 None -3 18 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C None
31101 7516 40 None -48 35 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
35 7516 40 None -48 35 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
403 7516 40 None -48 35 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
CHEMBL493 7516 40 None -48 35 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
DB01200 7516 40 None -48 35 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C None
2105 9828 37 None -6 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
47811 9828 37 None -6 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
48 9828 37 None -6 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
CHEMBL531 9828 37 None -6 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
DB01186 9828 37 None -6 32 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 None
1342 6824 49 3H-5HT -4 19 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
3 6824 49 3H-5HT -4 19 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
CHEMBL277120 6824 49 3H-5HT -4 19 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 None
71299720 222730 0 3H-5HT -44 17 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
71299720 222730 0 3H-5HT -44 17 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 450 3 2 6 3.0 CN1CCN(CC1)C2=NC3=C(C=CC(=C3)C(F)(F)F)N4C2=CC=C4.C(=CC(=O)O)C(=O)O None
4806 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
71768094 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
7351 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
9966051 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
CHEMBL2104993 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
DB09068 10780 88 None -2 13 Human 8.1 pKi = 8.1 Binding
partial agonistpartial agonist
Drug Central 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 None
2389 10104 118 None -93 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 None -93 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 None -93 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 None -93 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 None -93 66 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
11978813 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
5014 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
7672 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
CHEMBL2105760 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
DB09128 7508 79 None -9 24 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 433 7 1 5 4.7 O=c1ccc2c([nH]1)cc(cc2)OCCCCN1CCN(CC1)c1cccc2c1ccs2 None
135 9310 43 None -3 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -3 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -3 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -3 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -3 56 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
134 9292 24 3H-5HT -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 3H-5HT -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 3H-5HT -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 3H-5HT -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 3H-5HT -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
133 9274 52 None -40 43 Rat 8.1 pKi = 8.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 None -40 43 Rat 8.1 pKi = 8.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 None -40 43 Rat 8.1 pKi = 8.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 None -40 43 Rat 8.1 pKi = 8.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 None -40 43 Rat 8.1 pKi = 8.1 Binding
Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.Binding affinity (Ki) to rat cortical membranes at 5-HT1B binding site by using [125 I] ICYP as a radioligand.
Drug Central 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
134 9292 24 None -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
1775 9292 24 None -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
9681 9292 24 None -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
CHEMBL1065 9292 24 None -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
DB00247 9292 24 None -14 67 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO None
102 10899 48 None -64 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -64 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -64 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -64 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -64 49 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
5 6927 72 3H-5HT -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-5HT -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-5HT -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-5HT -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
2543 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 None -17 32 Rat 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1B receptor in rat striatum labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
115237 62359 119 None -93 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
CHEMBL1621 62359 119 None -93 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
DB01267 62359 119 None -93 54 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 426 4 1 7 3.1 Cc1nc2n(c(=O)c1CCN1CCC(c3noc4cc(F)ccc34)CC1)CCCC2O None
1588 9105 27 None -42 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 None -42 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 None -42 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 None -42 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 None -42 44 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
2869 10924 89 None -8 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60 10924 89 None -8 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
60857 10924 89 None -8 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
CHEMBL1185 10924 89 None -8 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
DB00315 10924 89 None -8 7 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C None
2543 10479 68 3H-5HT -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2477 7532 59 None -16 29 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
36 7532 59 None -16 29 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
437 7532 59 None -16 29 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
CHEMBL49 7532 59 None -16 29 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
DB00490 7532 59 None -16 29 Rat 8.1 pKi = 8.1 Binding
Inhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptorInhibition of [3H]5-HT binding to 5-hydroxytryptamine 1B receptor
Drug Central 385 6 0 6 2.1 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(CC1)c1ncccn1 None
3658 10879 53 None -4 8 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
517 10879 53 None -4 8 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5709 10879 53 None -4 8 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
CHEMBL312448 10879 53 None -4 8 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
DB06694 10879 53 None -4 8 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptorBinding affinity towards human 5-hydroxytryptamine 1B receptor
Drug Central 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C None
5 6927 72 35S-GTPGammaS -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 35S-GTPGammaS -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 35S-GTPGammaS -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 35S-GTPGammaS -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
107780 8625 54 35S-GTPGammaS 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
14 8625 54 35S-GTPGammaS 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL15928 8625 54 35S-GTPGammaS 1 18 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
28 10269 46 35S-GTPGammaS 13 10 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
3292447 10269 46 35S-GTPGammaS 13 10 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
CHEMBL20963 10269 46 35S-GTPGammaS 13 10 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C None
107715 207724 22 None -22 20 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL1255837 207724 22 None -22 20 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
CHEMBL601773 207724 22 None -22 20 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 611 5 3 6 2.7 CC(C)[C@@]1(NC(=O)[C@@H]2C[C@@H]3c4cccc5[nH]cc(c45)C[C@H]3N(C)C2)O[C@@]2(O)[C@@H]3CCCN3C(=O)[C@H](Cc3ccccc3)N2C1=O None
1251 8473 30 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
7191 8473 30 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
77992 8473 30 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
CHEMBL1279 8473 30 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
DB00998 8473 30 None -1 3 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O None
186 8588 52 3H-GR-125743 -11 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
71781 8588 52 3H-GR-125743 -11 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
CHEMBL18972 8588 52 3H-GR-125743 -11 17 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 295 5 1 2 3.7 OC(c1ccccc1)C1CCN(CC1)CCc1ccccc1 None
137 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
2119 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
563 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
66368 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
CHEMBL266195 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
DB00866 7158 52 125I-ICYP -154 12 Rat 7.2 pKi = 7.2 Binding
NoneNone
PDSP KiDatabase 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O None
1220 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
21138 105227 39 125I-ICYP -162 7 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
CHEMBL275742 105227 39 125I-ICYP -162 7 Rat 5.2 pKi = 5.2 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NC[C@@H](O)COc1cccc2ccccc12 None
1220 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-GR-125743 -208 44 Human 6.2 pKi = 6.2 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
2389 10104 118 3H-5CT -93 66 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-5CT -93 66 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-5CT -93 66 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-5CT -93 66 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-5CT -93 66 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
None 223018 0 3H-GR-125743 -4677 29 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 316 7 3 3 3.0 CC(CF)NCC(COC1=CC=CC2=C1C3=CC=CC=C3N2)O None
1220 6975 55 3H-5HT -7413 44 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
31 6975 55 3H-5HT -7413 44 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
7 6975 55 3H-5HT -7413 44 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
CHEMBL56 6975 55 3H-5HT -7413 44 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 247 5 1 2 3.4 CCCN(C1CCc2c(C1)c(O)ccc2)CCC None
145 6928 49 3H-5-CT -8 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
1832 6928 49 3H-5-CT -8 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL7257 6928 49 3H-5-CT -8 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB14010 6928 49 3H-5-CT -8 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 218 4 1 2 2.3 COc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
165193 222724 0 125I-ICYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-ICYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-ICYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
102 10899 48 125I-ICYP -2691 49 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 125I-ICYP -2691 49 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 125I-ICYP -2691 49 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 125I-ICYP -2691 49 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 125I-ICYP -2691 49 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
127 9900 52 3H-5HT -95 15 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
688095 9900 52 3H-5HT -95 15 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL117405 9900 52 3H-5HT -95 15 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C None
2303 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
4946 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
564 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
63 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
91536 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL27 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
CHEMBL452861 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
DB00571 9961 68 125I-ICYP -57 26 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 O[C@H](COc1cccc2c1cccc2)CNC(C)C None
24882193 195428 0 UNDEFINED -263 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
CHEMBL503468 195428 0 UNDEFINED -263 2 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 770 14 4 4 10.4 O=C(Nc1ccc2[nH]cc(C3CCN(CCCCCCCN4CCC(c5c[nH]c6ccc(NC(=O)c7ccc(F)cc7)cc56)CC4)CC3)c2c1)c1ccc(F)cc1 None
4209 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
4893 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
503 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
5385 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
CHEMBL2 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
DB00457 9937 75 125I-CYP -4073 33 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 None
123606 7140 70 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
128 7140 70 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
7110 7140 70 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
CHEMBL1505 7140 70 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
DB00918 7140 70 None -1 3 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 335 6 1 3 2.2 CN(CCc1c[nH]c2c1cc(cc2)CS(=O)(=O)N1CCCC1)C None
150 9287 21 None -6 16 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
1764 9287 21 None -6 16 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
8226 9287 21 None -6 16 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
CHEMBL1201356 9287 21 None -6 16 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
DB00353 9287 21 None -6 16 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO None
2543 10479 68 None -2 32 Western lowland gorilla 8.1 pKi = 8.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 None -2 32 Western lowland gorilla 8.1 pKi = 8.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 None -2 32 Western lowland gorilla 8.1 pKi = 8.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 None -2 32 Western lowland gorilla 8.1 pKi = 8.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 None -2 32 Western lowland gorilla 8.1 pKi = 8.1 Binding
The compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cellsThe compound was tested for CNS binding affinity towards 5-hydroxytryptamine 1B receptor from cloned gorilla membranes expressed in cultured HEK 293 cells
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
2543 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 None -3 32 Human 8.1 pKi = 8.1 Binding
Binding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HTBinding affinity was measured on 5-hydroxytryptamine 1D receptor beta in CHO cells transfected with human 5-HT1D beta gene labeled with [3H]5-HT
Drug Central 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
134551 7146 27 None -5 21 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
271 7146 27 None -5 21 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
885 7146 27 None -5 21 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
CHEMBL1403281 7146 27 None -5 21 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 575 5 3 6 2.4 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C(C)C)O)C None
1524 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
197 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
3822 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
88 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
CHEMBL51 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
DB12465 8962 96 None -4 51 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 None
135 9310 43 None -3 56 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
1796 9310 43 None -3 56 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
4184 9310 43 None -3 56 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
CHEMBL6437 9310 43 None -3 56 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
DB06148 9310 43 None -3 56 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 None
2470 10425 50 None -194 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 None -194 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 None -194 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 None -194 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 None -194 58 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
102 10899 48 None -186 49 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
3659 10899 48 None -186 49 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
8969 10899 48 None -186 49 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
CHEMBL15245 10899 48 None -186 49 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
DB01392 10899 48 None -186 49 Mouse 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 None
2865 10915 73 None -12 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
59 10915 73 None -12 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
60854 10915 73 None -12 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
CHEMBL708 10915 73 None -12 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
DB00246 10915 73 None -12 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 None
1588 9105 27 None -58 44 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
28864 9105 27 None -58 44 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
43 9105 27 None -58 44 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
CHEMBL157138 9105 27 None -58 44 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
DB00589 9105 27 None -58 44 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC None
3036780 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
46780481 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
9903970 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3187365 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL3544974 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
CHEMBL504548 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
DB06216 114308 20 None -32 53 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 None
1884 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
In vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptorIn vitro receptor binding affinity for cloned human 5-hydroxytryptamine 1B receptor
Drug Central 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
11954224 222732 0 None -32 59 Human 8.1 pKi = 8.1 Binding
Displacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation countingDisplacement of [3H]carboxytryptamine from recombinant human 5-HT1B receptor expressed in HEK cells by scintillation counting
Drug Central 581 4 3 6 2.0 CC1(C(=O)N2C(C(=O)N3CCCC3C2(O1)O)CC4=CC=CC=C4)NC(=O)C5CN(C6CC7=CNC8=CC=CC(=C78)C6=C5)C None
1042 8362 23 None -5 17 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
148 8362 23 None -5 17 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
443884 8362 23 None -5 17 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
CHEMBL119443 8362 23 None -5 17 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
DB01253 8362 23 None -5 17 Rat 8.1 pKi = 8.1 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 325 3 3 3 1.5 OC[C@@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)C None
151 9194 44 UNDEFINED -89 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
20 9194 44 UNDEFINED -89 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
5311258 9194 44 UNDEFINED -89 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
CHEMBL101690 9194 44 UNDEFINED -89 4 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 351 3 2 2 4.4 CN1CCC(CC1)c1c[nH]c2c1cc(cc2)NC(=O)c1ccc(cc1)F None
242 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
155 7515 25 3H-5HT -263 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
163 7515 25 3H-5HT -263 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
62065 7515 25 3H-5HT -263 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
CHEMBL6607 7515 25 3H-5HT -263 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
DB01484 7515 25 3H-5HT -263 13 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 273 4 1 3 2.4 COc1cc(Br)c(cc1CC(N)C)OC None
104911 222798 0 3H-8-OH-DPAT -38018 37 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 530 7 0 5 5.1 COC1=CC=CC=C1N2CCN(CC2)CCN(C3=CC=CC=N3)C(=O)C4CCCCC4.Cl.Cl.Cl None
119570 9933 96 3H-GR-125743 -398 39 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 3H-GR-125743 -398 39 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 3H-GR-125743 -398 39 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 3H-GR-125743 -398 39 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 3H-GR-125743 -398 39 Human 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
242 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
34 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
60795 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
CHEMBL1112 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
DB01238 7258 124 3H-GR-125743 -380 51 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl None
115 10563 80 125I-ICYP 1 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
4296 10563 80 125I-ICYP 1 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
CHEMBL274866 10563 80 125I-ICYP 1 27 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F None
180 7189 56 3H-5HT -389 40 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
200 7189 56 3H-5HT -389 40 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
2160 7189 56 3H-5HT -389 40 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
CHEMBL629 7189 56 3H-5HT -389 40 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
DB00321 7189 56 3H-5HT -389 40 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C None
277 8083 62 3H-5HT -501 50 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
2913 8083 62 3H-5HT -501 50 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
765 8083 62 3H-5HT -501 50 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
CHEMBL516 8083 62 3H-5HT -501 50 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
DB00434 8083 62 3H-5HT -501 50 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 None
62787 212967 21 3H-5HT -85 10 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
CHEMBL8642 212967 21 3H-5HT -85 10 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 195 4 1 3 1.6 COc1ccc(OC)c(CC(C)N)c1 None
165193 222724 0 3H-5-CT -1000 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 3H-5-CT -1000 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 3H-5-CT -1000 30 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
165193 222724 0 125I-CYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
62882 222724 0 125I-CYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
66366 222724 0 125I-CYP -154 30 Rat 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 259 6 2 3 2.6 CC(C)NCC(COC1=CC=CC2=CC=CC=C21)O None
1574 6869 60 3H-5HT -8 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 3H-5HT -8 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 3H-5HT -8 21 Human 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
1150 10650 121 3H-5HT -7 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
125 10650 121 3H-5HT -7 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
CHEMBL6640 10650 121 3H-5HT -7 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
DB08653 10650 121 3H-5HT -7 25 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 None
2142 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
4920903 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
502 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
5775 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
CHEMBL597 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
DB00692 9870 58 125I-ICYP -741 37 Rat 6.1 pKi = 6.1 Binding
NoneNone
PDSP KiDatabase 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 None
138107169 222731 0 125I-ICYP -19054 23 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
22831402 222731 0 125I-ICYP -19054 23 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 354 1 2 4 2.6 COC(=O)C1C(CCC2C1CC3C4=C(CCN3C2)C5=CC=CC=C5N4)O None
1353 8692 93 125I-CYP -5248 85 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3559 8692 93 125I-CYP -5248 85 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
86 8692 93 125I-CYP -5248 85 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
CHEMBL54 8692 93 125I-CYP -5248 85 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
DB00502 8692 93 125I-CYP -5248 85 Rat 5.1 pKi = 5.1 Binding
NoneNone
PDSP KiDatabase 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl None
3294 8787 111 3H-5HT -57 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-5HT -57 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-5HT -57 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-5HT -57 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-5HT -57 44 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
7153 104796 77 3H-5HT -11 33 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -11 33 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
5 6927 72 3H-GR-125743 -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5 6927 72 125I-ICYP -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 3H-GR-125743 -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
5202 6927 72 125I-ICYP -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 3H-GR-125743 -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
CHEMBL39 6927 72 125I-ICYP -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 3H-GR-125743 -11 53 Human 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
DB08839 6927 72 125I-ICYP -13 53 Rat 8.1 pKi = 8.1 Binding
NoneNone
PDSP KiDatabase 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 None
124 9755 47 None -2 32 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 None -2 32 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 None -2 32 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 None -2 32 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 None -2 32 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2543 10479 68 UNDEFINED -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 UNDEFINED -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 UNDEFINED -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 UNDEFINED -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 UNDEFINED -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
10531 8202 21 None -12 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 8202 21 None -12 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 8202 21 None -12 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 8202 21 None -12 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 8202 21 None -12 24 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
2543 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
5358 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
54 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
CHEMBL128 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
DB00669 10479 68 3H-5HT -3 32 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 None
133 9274 52 3H-GR-125743 -23 43 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1723 9274 52 3H-GR-125743 -23 43 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
28693 9274 52 3H-GR-125743 -23 43 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
CHEMBL19215 9274 52 3H-GR-125743 -23 43 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
DB13520 9274 52 3H-GR-125743 -23 43 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C None
1884 9512 58 3H-GR-125743 -3 5 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
4440 9512 58 3H-GR-125743 -3 5 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
45 9512 58 3H-GR-125743 -3 5 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
CHEMBL1278 9512 58 3H-GR-125743 -3 5 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
DB00952 9512 58 3H-GR-125743 -3 5 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C None
10531 8202 21 None -5 24 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
121 8202 21 None -5 24 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
888 8202 21 None -5 24 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
CHEMBL1732 8202 21 None -5 24 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
DB00320 8202 21 None -5 24 Rat 8.0 pKi = 8.0 Binding
DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)
Drug Central 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O None
124 9755 47 None 1 32 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2032 9755 47 None 1 32 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
4636 9755 47 None 1 32 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
CHEMBL762 9755 47 None 1 32 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
DB00935 9755 47 None 1 32 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligandBinding affinity towards human 5-hydroxytryptamine 1B receptor using [3H]5-HT trifluoroacetate as radioligand
Drug Central 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C None
2389 10104 118 3H-Alniditan -93 66 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
5073 10104 118 3H-Alniditan -93 66 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
96 10104 118 3H-Alniditan -93 66 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
CHEMBL85 10104 118 3H-Alniditan -93 66 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
DB00734 10104 118 3H-Alniditan -93 66 Human 8.0 pKi = 8.0 Binding
NoneNone
PDSP KiDatabase 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 None
7153 104796 77 3H-5HT -11 33 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 3H-5HT -11 33 Human 7.1 pKi = 7.1 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
10257 7525 31 125I-CYP -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
10257 7525 31 3H-5HT -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 7525 31 125I-CYP -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
144 7525 31 3H-5HT -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 7525 31 125I-CYP -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
CHEMBL416526 7525 31 3H-5HT -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 7525 31 125I-CYP -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
DB01445 7525 31 3H-5HT -141 19 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 204 3 2 2 2.0 CN(CCc1c[nH]c2c1cc(O)cc2)C None
None 222914 0 3H-GR-125743 -3162 23 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 772 16 4 10 5.5 CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.CN(C)CCONC(=CC=C1C=CC(=O)C=C1)C2=CC=CC=C2F.C(=CC(=O)O)C(=O)O None
1574 6869 60 3H-5HT -8 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
218 6869 60 3H-5HT -8 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
CHEMBL266591 6869 60 3H-5HT -8 21 Human 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O None
2176 9901 68 125I-CYP -741 27 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
4828 9901 68 125I-CYP -741 27 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
91 9901 68 125I-CYP -741 27 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
CHEMBL500 9901 68 125I-CYP -741 27 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
DB00960 9901 68 125I-CYP -741 27 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 248 6 3 3 1.9 OC(COc1cccc2c1cc[nH]2)CNC(C)C None
107992 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
3012003 222924 0 3H-5HT -371 12 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 311 5 0 3 3.8 CN1CCC(C(C1)COC2=CC=C(C=C2)OC)C3=CC=CC=C3 None
107992 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
165 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
CHEMBL269521 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
DB12111 9331 49 125I-CYP -12 10 Rat 5.0 pKi = 5.0 Binding
NoneNone
PDSP KiDatabase 198 1 1 4 0.5 Clc1cncc(n1)N1CCNCC1 None
103 10925 61 3H-5HT -776 53 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
2875 10925 61 3H-5HT -776 53 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
5736 10925 61 3H-5HT -776 53 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
CHEMBL285802 10925 61 3H-5HT -776 53 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
DB09225 10925 61 3H-5HT -776 53 Rat 6.0 pKi = 6.0 Binding
NoneNone
PDSP KiDatabase 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C None
4106 9280 22 125I-ICYP -102 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
5358812 9280 22 125I-ICYP -102 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
89 9280 22 125I-ICYP -102 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
CHEMBL93240 9280 22 125I-ICYP -102 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C None
7153 104796 77 125I-ICYP -10 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
CHEMBL272942 104796 77 125I-ICYP -10 33 Rat 7.0 pKi = 7.0 Binding
NoneNone
PDSP KiDatabase 214 3 1 2 2.5 Cc1cc(Cl)ccc1OC(C)C(=O)O None
3294 8787 111 3H-5CT -57 44 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
71360 8787 111 3H-5CT -57 44 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
87 8787 111 3H-5CT -57 44 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
CHEMBL14376 8787 111 3H-5CT -57 44 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
DB04946 8787 111 3H-5CT -57 44 Human 7.0 pKi = 7 Binding
NoneNone
PDSP KiDatabase 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C None
2470 10425 50 3H-5HT -95499 58 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
3300 10425 50 3H-5HT -95499 58 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
5265 10425 50 3H-5HT -95499 58 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
99 10425 50 3H-5HT -95499 58 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
CHEMBL267930 10425 50 3H-5HT -95499 58 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 None
2393 10107 82 None -1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
5078 10107 82 None -1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
51 10107 82 None -1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
CHEMBL905 10107 82 None -1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
DB00953 10107 82 None -1 5 Human 6.9 pKi = 6.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 269 5 1 4 1.9 CN(CCc1c[nH]c2c1cc(cc2)Cn1cncn1)C 10193663
2389 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
2389 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
2389 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
5073 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
5073 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
5073 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
96 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
96 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
96 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
CHEMBL85 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
CHEMBL85 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
CHEMBL85 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
DB00734 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 18308814
DB00734 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 8935801
DB00734 10104 118 None -93 66 Human 7.0 pKi = 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 9605573
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
2543 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
5358 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
54 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
CHEMBL128 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10193663
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10513577
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 10611634
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 11040052
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 1565658
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8863519
DB00669 10479 68 None -3 32 Human 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 295 6 2 3 1.3 CNS(=O)(=O)Cc1ccc2c(c1)c(CCN(C)C)c[nH]2 8967979
10446 7318 0 None -8 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
133081 7318 0 None -8 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
CHEMBL2110755 7318 0 None -8 4 Rat 7.4 pKi = 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
4806 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
71768094 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
7351 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
9966051 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
CHEMBL2104993 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
DB09068 10780 88 None -2 13 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 298 3 1 3 3.9 Cc1ccc(c(c1)C)Sc1ccccc1N1CCNCC1 21486038
113 8633 14 None 39 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
128018 8633 14 None 39 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
CHEMBL119264 8633 14 None 39 3 Human 7.5 pKi = 7.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 2 4 4.2 CN(CCCc1cc(ccc1O)C(=O)Nc1ccc(cc1)c1ccncc1)C 10513577
10446 7318 0 None -4 4 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
133081 7318 0 None -4 4 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
CHEMBL2110755 7318 0 None -4 4 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 458 9 2 7 1.8 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)CS(=O)(=O)NC 9050026
2869 10924 89 None -8 7 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
60 10924 89 None -8 7 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
60857 10924 89 None -8 7 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
CHEMBL1185 10924 89 None -8 7 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
DB00315 10924 89 None -8 7 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10193663
1251 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
7191 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
77992 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
CHEMBL1279 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
DB00998 8473 30 None -1 3 Human 8.0 pKi = 8.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 243 2 4 2 2.1 CN[C@H]1Cc2c(CC1)[nH]c1c2cc(cc1)C(=N)O 9986723
40 8329 58 None -2 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
77993 8329 58 None -2 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
995 8329 58 None -2 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
CHEMBL1510 8329 58 None -2 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
DB00216 8329 58 None -2 5 Human 8.0 pKi = 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 6 1 3 3.8 CN1CCC[C@@H]1Cc1c[nH]c2c1cc(cc2)CCS(=O)(=O)c1ccccc1 10193663
5 6927 72 None -41 53 Mouse 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
5202 6927 72 None -41 53 Mouse 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
CHEMBL39 6927 72 None -41 53 Mouse 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
DB08839 6927 72 None -41 53 Mouse 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1557407
1884 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
4440 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
45 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
CHEMBL1278 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
DB00952 9512 58 None -3 5 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 335 5 2 3 2.1 CNS(=O)(=O)CCc1ccc2c(c1)c(c[nH]2)C1CCN(CC1)C 10193663
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
5 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
5202 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
CHEMBL39 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 10431754
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 11040052
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 1565658
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 8957260
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9208142
DB08839 6927 72 None -11 53 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 176 2 3 2 1.4 NCCc1c[nH]c2c1cc(O)cc2 9776361
3231 10278 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
5311426 10278 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
CHEMBL1628625 10278 0 None - 1 Human 8.2 pKi = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 534 4 0 6 6.0 CCN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1nnc(o1)C 10443589
130 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
130 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
130 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
3378093 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
3378093 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
3378093 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
CHEMBL281350 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 11040052
CHEMBL281350 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
CHEMBL281350 10273 47 None -1 13 Human 8.4 pKi = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 520 3 0 6 5.6 CN1CCC2(CC1)COc1c2cc2c(c1)CCN2C(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
3221 7971 0 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
4029677 7971 0 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
CHEMBL1570196 7971 0 None - 1 Human 8.7 pKi = 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 257 4 2 3 2.7 CCCOc1ccc2c(n1)c(c[nH]2)C1=CCNCC1 None
132059 9016 57 None -1 3 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
15 9016 57 None -1 3 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
CHEMBL39317 9016 57 None -1 3 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 411 7 3 6 2.7 NCCc1c[nH]c2c1cc(cc2)c1onc(n1)Cc1ccc(cc1)NS(=O)(=O)C 10513577
202 8290 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
60835 8290 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
972 8290 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
CHEMBL1175 8290 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
DB00476 8290 77 None -1 33 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 None
119570 9933 96 None -398 39 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
2233 9933 96 None -398 39 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
953 9933 96 None -398 39 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
CHEMBL301265 9933 96 None -398 39 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
DB00413 9933 96 None -398 39 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N None
228 7233 28 None 1 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
33 7233 28 None 1 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
6005 7233 28 None 1 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
CHEMBL53 7233 28 None 1 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
DB00714 7233 28 None 1 23 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O None
3337 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
65801 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
66264 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
91452 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
CHEMBL87493 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
DB00574 213146 27 None -74 40 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 231 4 1 1 3.2 CCNC(C)Cc1cccc(C(F)(F)F)c1 None
179 7188 115 None -43 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2159 7188 115 None -43 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
963 7188 115 None -43 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
CHEMBL243712 7188 115 None -43 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
DB06288 7188 115 None -43 50 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 369 7 2 6 1.3 CCN1CCCC1CNC(=O)c1cc(c(cc1OC)N)S(=O)(=O)CC None
2995 211184 53 None -3 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL1696 211184 53 None -3 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
CHEMBL72 211184 53 None -3 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
DB01151 211184 53 None -3 23 Human 8.2 pKi None 8.2 Binding
NoneNone
Drug Central 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 None
29 7579 0 None -7943 9 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
9805719 7579 0 None -7943 9 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
CHEMBL2027925 7579 0 None -7943 9 Human 5.3 pKi None 5.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 456 5 1 8 3.4 Nc1c(Cl)cc(c2c1OCCO2)c1nn(c(=O)o1)C1CCN(CC1)CCc1ccccc1 12130738
126 10842 8 None -1258 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
6604840 10842 8 None -1258 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
CHEMBL38288 10842 8 None -1258 5 Human 5.8 pKi None 5.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.5 COc1ccccc1N1CCN(CC1)C[C@@H](C(=O)NC(C)(C)C)c1ccccc1 9208142
219050 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
219050 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
52 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
52 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
CHEMBL431367 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 10431754
CHEMBL431367 10146 25 None -7762 21 Human 5.9 pKi None 5.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 346 6 2 2 5.0 Oc1ccc2c(c1)c(CCCCN1CCC(=CC1)c1ccccc1)c[nH]2 12388666
1574 6869 60 None -8 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
218 6869 60 None -8 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
CHEMBL266591 6869 60 None -8 21 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 2 3 2 1.7 Cc1c(CCN)c2c([nH]1)ccc(c2)O 1565658
242 7258 124 None -380 51 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
34 7258 124 None -380 51 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
60795 7258 124 None -380 51 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
CHEMBL1112 7258 124 None -380 51 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
DB01238 7258 124 None -380 51 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 12784105
10 7510 28 None -63 9 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
3654103 7510 28 None -63 9 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
CHEMBL534232 7510 28 None -63 9 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 406 6 1 3 4.7 Clc1cccc(c1)N1CCN(CC1)CC(C(c1ccccc1)c1ccccc1)O 9303567
65 8851 0 None -2 2 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
9995893 8851 0 None -2 2 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
CHEMBL418834 8851 0 None -2 2 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
129 10213 10 None -2818 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
9868452 10213 10 None -2818 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
CHEMBL65280 10213 10 None -2818 8 Human 6.1 pKi None 6.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 7 1 4 4.8 N#Cc1ccc2c(c1)[C@H]1CN(C[C@@H]1CO2)CCCCNC(=O)c1ccc(cc1)c1ccccc1 10869410
135398737 7745 93 None -151 90 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
38 7745 93 None -151 90 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
722 7745 93 None -151 90 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
CHEMBL42 7745 93 None -151 90 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
DB00363 7745 93 None -151 90 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 8935801
2181 9902 46 None -70 34 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
4830 9902 46 None -70 34 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
92 9902 46 None -70 34 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
CHEMBL440294 9902 46 None -70 34 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
DB09286 9902 46 None -70 34 Human 6.2 pKi None 6.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 8935801
37 7565 60 None -22 17 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
460 7565 60 None -22 17 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
54746 7565 60 None -22 17 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
CHEMBL1201087 7565 60 None -22 17 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
DB00248 7565 60 None -22 17 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 12388666
18971832 9196 0 None -85 13 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
21 9196 0 None -85 13 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
CHEMBL3186179 9196 0 None -85 13 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 351 3 2 2 4.0 CN(C1CCc2c(C1)c1cc(ccc1[nH]2)NC(=O)c1ccc(cc1)F)C 9395253
135398745 9688 112 None -199 65 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
47 9688 112 None -199 65 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
CHEMBL715 9688 112 None -199 65 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
DB00334 9688 112 None -199 65 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 8935801
1150 10650 121 None -7 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
125 10650 121 None -7 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
CHEMBL6640 10650 121 None -7 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
DB08653 10650 121 None -7 25 Human 6.3 pKi None 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 160 2 2 1 1.7 NCCc1c[nH]c2c1cccc2 1565658
31101 7516 40 None -128 35 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
35 7516 40 None -128 35 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
403 7516 40 None -128 35 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
CHEMBL493 7516 40 None -128 35 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
DB01200 7516 40 None -128 35 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 12388666
10358392 8865 0 None -10 2 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
66 8865 0 None -10 2 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
CHEMBL326418 8865 0 None -10 2 Human 6.5 pKi None 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 316 7 3 3 3.0 FCC(NC[C@@H](COc1cccc2c1c1ccccc1[nH]2)O)C 11512051
115 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
115 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
4296 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
4296 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
CHEMBL274866 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 1565658
CHEMBL274866 10563 80 None -2 27 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 230 1 1 2 2.1 FC(c1cccc(c1)N1CCNCC1)(F)F 8863519
114 9034 14 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
6426760 9034 14 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
CHEMBL292779 9034 14 None - 1 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 432 8 1 5 3.7 Fc1cccc(c1)CCN1CCN(CC1)CCCc1c[nH]c2c1cc(cc2)n1cnnc1 11040052
2105 9828 37 None -100 32 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
47811 9828 37 None -100 32 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
48 9828 37 None -100 32 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
CHEMBL531 9828 37 None -100 32 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
DB01186 9828 37 None -100 32 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 12388666
2601 10552 33 None -87 21 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
443951 10552 33 None -87 21 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
56 10552 33 None -87 21 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL73151 10552 33 None -87 21 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB13399 10552 33 None -87 21 Human 6.6 pKi None 6.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
10287730 10309 40 None -251 12 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
77 10309 40 None -251 12 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
CHEMBL425190 10309 40 None -251 12 Human 6.7 pKi None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 6 0 5 4.3 Cc1ccc2c(n1)cccc2OCCN1CCN(CC1)Cc1cccc2c1nccc2 15887956
475100 6977 0 None -158 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
67 6977 0 None -158 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
CHEMBL3542429 6977 0 None -158 6 Human 6.8 pKi None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 426 4 1 7 2.6 OC1CCc2n(C1)c(=O)c(c(n2)C)CCN1CCC(CC1)c1noc2c1ccc(c2)F 8935801
136 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
136 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
223 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
223 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
643606 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
643606 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
CHEMBL10347 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
CHEMBL10347 10065 32 None -177 16 Human 7.0 pKi None 7.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@@H]1[C@@H](O)CC[C@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 8863519
2435 10362 83 None -128 48 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
60149 10362 83 None -128 48 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
98 10362 83 None -128 48 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
CHEMBL12713 10362 83 None -128 48 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
DB06144 10362 83 None -128 48 Human 7.0 pKi None 7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 8935801
134 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
134 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
1775 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
1775 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
9681 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
9681 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
CHEMBL1065 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
CHEMBL1065 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
DB00247 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 1565658
DB00247 9292 24 None -14 67 Human 7.1 pKi None 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 8863519
102 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
102 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
3659 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
3659 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
8969 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
8969 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
CHEMBL15245 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
CHEMBL15245 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
DB01392 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10611634
DB01392 10899 48 None -64 49 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1565658
133 9274 52 None -23 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
1723 9274 52 None -23 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
28693 9274 52 None -23 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
CHEMBL19215 9274 52 None -23 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
DB13520 9274 52 None -23 43 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 8863519
103 10925 61 None -48 53 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
2875 10925 61 None -48 53 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
5736 10925 61 None -48 53 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
CHEMBL285802 10925 61 None -48 53 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
DB09225 10925 61 None -48 53 Human 7.2 pKi None 7.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 8935801
3652 10869 79 None -3 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
57 10869 79 None -3 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
60809 10869 79 None -3 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
CHEMBL21536 10869 79 None -3 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
DB15357 10869 79 None -3 18 Human 7.3 pKi None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 9884068
107 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
107 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
1833 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
1833 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
CHEMBL8165 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 1565658
CHEMBL8165 6929 121 None -16 31 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 190 3 2 2 1.7 NCCc1c[nH]c2c1cc(OC)cc2 8863519
122 8219 9 None -5 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
156314 8219 9 None -5 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
CHEMBL1332062 8219 9 None -5 11 Human 7.4 pKi None 7.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 8 2 2 2.9 CCCN(CCC)CCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
1588 9105 27 None -42 44 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
28864 9105 27 None -42 44 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
43 9105 27 None -42 44 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
CHEMBL157138 9105 27 None -42 44 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
DB00589 9105 27 None -42 44 Human 7.7 pKi None 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 12388666
4106 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
4106 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
4106 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
4106 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
5358812 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
5358812 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
5358812 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
5358812 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
89 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
89 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
89 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
89 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
CHEMBL93240 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 10513577
CHEMBL93240 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 11040052
CHEMBL93240 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8863519
CHEMBL93240 9280 22 None -11 33 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 356 2 0 4 4.4 CSc1ccc2c(c1)C(Cc1c(S2)cccc1)N1CCN(CC1)C 8957260
1342 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
1342 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
1342 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
3 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
3 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
3 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
CHEMBL277120 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 1565658
CHEMBL277120 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 8863519
CHEMBL277120 6824 49 None -4 19 Human 7.8 pKi None 7.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 212 1 1 2 2.2 N1CCN(CC1)c1cccc2c1cccc2 9397179
108 7456 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 5 2.9 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(F)cc2 11040052
177836 7456 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 369 6 1 5 2.9 COc1cncnc1N1CCN(CC1)CCCc1c[nH]c2c1cc(F)cc2 11040052
10296414 10304 15 None -7 9 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
76 10304 15 None -7 9 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
CHEMBL183460 10304 15 None -7 9 Human 8.0 pKi None 8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 431 6 1 5 4.2 O=C1COc2c(N1)cc(cc2)CC1CCN(CC1)CCOc1cccc2c1ccc(n2)C 15887956
1809 6922 32 None -97 37 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
4 6922 32 None -97 37 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
CHEMBL18840 6922 32 None -97 37 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1557407
163091 7282 34 None -131 10 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
22 7282 34 None -131 10 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
CHEMBL504548 7282 34 None -131 10 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
DB06216 7282 34 None -131 10 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 285 0 0 2 4.3 Clc1ccc2c(c1)[C@H]1CN(C[C@@H]1c1c(O2)cccc1)C 8935801
132 8058 13 None -125 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
155346 8058 13 None -125 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
CHEMBL378501 8058 13 None -125 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 287 5 3 4 2.2 N#Cc1[nH]c2c(c1)c(OCC(CNC(C)(C)C)O)ccc2 1557407
127 9900 52 None -18 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
688095 9900 52 None -18 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
CHEMBL117405 9900 52 None -18 15 Mouse 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 248 6 3 3 1.9 O[C@H](COc1cccc2c1cc[nH]2)CNC(C)C 1557407
108029 10187 57 None -7 13 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
23 10187 57 None -7 13 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
CHEMBL18785 10187 57 None -7 13 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 228 2 2 2 2.6 COc1ccc2c(c1)c(c[nH]2)C1=CCNCC1 1557407
75 10287 7 None -3 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
9870500 10287 7 None -3 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
CHEMBL191971 10287 7 None -3 3 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 3 1 4 5.9 CN1CCN(CC1)c1cc2c(cc1Cl)CCN2C(=O)Nc1ccc(c2c1cccc2)c1ccncc1 11454652
123 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
123 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
14987 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
14987 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
CHEMBL39947 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 1565658
CHEMBL39947 9208 41 None -10 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 254 1 2 2 2.0 OC[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3 8863519
106 6936 26 None 4 6 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
1797 6936 26 None 4 6 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
CHEMBL97450 6936 26 None 4 6 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 11 2 2 4.8 CCCCCCCCCOc1ccc2c(c1)c(CCN)c[nH]2 10513577
1809 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
1809 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
4 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
4 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
CHEMBL18840 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 1565658
CHEMBL18840 6922 32 None -15 37 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 203 3 3 2 0.8 NCCc1c[nH]c2c1cc(cc2)C(=O)N 8863519
1524 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
197 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
3822 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
88 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
CHEMBL51 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
DB12465 8962 96 None -4 51 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 1557407
135 9310 43 None -3 56 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
1796 9310 43 None -3 56 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
4184 9310 43 None -3 56 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
CHEMBL6437 9310 43 None -3 56 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
DB06148 9310 43 None -3 56 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 1557407
2470 10425 50 None -194 58 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
3300 10425 50 None -194 58 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
5265 10425 50 None -194 58 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
99 10425 50 None -194 58 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
CHEMBL267930 10425 50 None -194 58 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 1557407
102 10899 48 None -186 49 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
3659 10899 48 None -186 49 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
8969 10899 48 None -186 49 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
CHEMBL15245 10899 48 None -186 49 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
DB01392 10899 48 None -186 49 Mouse 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 1557407
2865 10915 73 None -12 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
59 10915 73 None -12 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
60854 10915 73 None -12 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
CHEMBL708 10915 73 None -12 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
DB00246 10915 73 None -12 53 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 8935801
109 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
109 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
2689 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
2689 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
CHEMBL27403 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 10513577
CHEMBL27403 7689 31 None -1 7 Human 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 334 1 0 4 3.3 CN1CCN(CC1)c1nc2cc(ccc2n2c1ccc2)C(F)(F)F 1565658
128 6937 11 None -2 7 Mouse 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
172267 6937 11 None -2 7 Mouse 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
CHEMBL273273 6937 11 None -2 7 Mouse 8.4 pKi None 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 247 5 1 2 3.4 CCCN(C1CCc2c(C1)cccc2O)CCC 1557407
10531 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8863519
10531 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8967979
121 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8863519
121 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8967979
888 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8863519
888 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8967979
CHEMBL1732 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8863519
CHEMBL1732 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8967979
DB00320 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8863519
DB00320 8202 21 None -12 24 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 8967979
14533720 6970 0 None -3 3 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 2.2 O=C(OCC1OC1)NCC[Si]([Si](C)(C)C)(C)C 9397179
6 6970 0 None -3 3 Human 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 2.2 O=C(OCC1OC1)NCC[Si]([Si](C)(C)C)(C)C 9397179
117 7141 19 None -1 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
120 7141 19 None -1 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
66004 7141 19 None -1 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
CHEMBL88240 7141 19 None -1 2 Human 8.9 pKi None 8.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 6 3 5 1.3 C(NC[C@H]1CCc2c(O1)cccc2)CCNC1=NCCCN1 8967979
28 10269 46 None 13 10 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
3292447 10269 46 None 13 10 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL20963 10269 46 None 13 10 Human 9.0 pKi None 9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 486 9 1 7 5.2 COc1ccc(cc1OCCN(C)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
107780 8625 54 None 1 18 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
14 8625 54 None 1 18 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
CHEMBL15928 8625 54 None 1 18 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 10513577
107780 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
107780 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
107780 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
107780 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
107780 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
14 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
14 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
14 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
14 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
14 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
CHEMBL15928 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 8957260
CHEMBL15928 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9303567
CHEMBL15928 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9397179
CHEMBL15928 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9548813
CHEMBL15928 8625 54 None 1 18 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 497 6 1 7 5.0 COc1ccc(cc1N1CCN(CC1)C)NC(=O)c1ccc(cc1)c1ccc(cc1C)c1noc(n1)C 9776361
197706 8246 0 None -1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 8246 0 None -1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 8246 0 None -1 10 Human 9.4 pKi None 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
124 9755 47 None 1 32 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
2032 9755 47 None 1 32 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
4636 9755 47 None 1 32 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
CHEMBL762 9755 47 None 1 32 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
DB00935 9755 47 None 1 32 Human 9.5 pKi None 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 9632357
197706 8246 0 None 1 10 Rat 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
39 8246 0 None 1 10 Rat 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763
CHEMBL1742428 8246 0 None 1 10 Rat 9.7 pKi None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 403 6 2 5 2.3 NCCc1c[nH]c2c1cc(OCC(=O)N1CCN(CC1)c1ccc(cc1)C#N)cc2 10381763