SB 649915 [Ligand Id: 76] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL183460 (SB-649915)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
ChEMBL Binding affinity at adrenergic beta 1 receptor B 5.6 pKi 2511.89 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL Negative logarithm causing 50% receptor occupancy against beta-2 adrenergic receptor B 6.3 pKi <501.19 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL Displacement of [125I]iodosulpiride from human cloned D2 receptor expressed in CHO cells B 5.9 pKi 1258.93 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [125I]iodosulpiride from human cloned D3 receptor expressed in CHO cells B 6.2 pKi 630.96 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Displacement of [3H]WAY 100635 from human recombinant 5HT1A receptor expressed in CHO cells B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5214-5217 [PMID:17629698]
ChEMBL Displacement of [3H]WAY-100635 from human cloned 5HT1A receptor expressed in CHO cells B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
ChEMBL Displacement of [3H]WAY100635 from human recombinant 5HT1A receptor B 8.6 pKi 2.51 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Displacement of [3H]5HT from human cloned 5HT1A receptor expressed in CHO cells B 8.6 pKi 2.51 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5581-5585 [PMID:18829312]
ChEMBL Displacement of [3H]WAY-100635 from human 5-hydroxytryptamine 1A receptor expressed in CHO cells B 8.6 pKi 2.51 nM Ki J. Med. Chem. (2005) 48: 3478-3480 [PMID:15887956]
GtoPdb - - 8.6 pKi - - - J. Med. Chem. (2005) 48: 3478-80 [PMID:15887956]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor expressed in CHO cells B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5214-5217 [PMID:17629698]
ChEMBL Negative logarithm causing 50% receptor occupancy against 5-hydroxytryptamine 1A receptor B 9.5 pKi 0.32 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
ChEMBL Mean negative logarithim of binding affinity was measured for the human 5-hydroxytryptamine 1A receptor; n>/=3 B 9.5 pKi 0.32 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 737-741 [PMID:15664848]
ChEMBL Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor B 9.5 pKi 0.32 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
GtoPdb - - 8 pKi - - - J. Med. Chem. (2005) 48: 3478-80 [PMID:15887956]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1B receptor expressed in CHO cells B 8 pKi 10 nM Ki J. Med. Chem. (2005) 48: 3478-3480 [PMID:15887956]
ChEMBL Displacement of [3H]5-HT from human cloned 5HT1B receptor expressed in CHO cells B 8 pKi 10 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
ChEMBL Displacement of [3H]5-HT from human recombinant 5HT1B receptor expressed in CHO cells B 8 pKi 10 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5214-5217 [PMID:17629698]
ChEMBL Displacement of [3H]5HT from human recombinant 5HT1B receptor B 8 pKi 10 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Displacement of [3H]5HT from human cloned 5HT1B receptor expressed in CHO cells B 8 pKi 10 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5581-5585 [PMID:18829312]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki J. Med. Chem. (2005) 48: 3478-3480 [PMID:15887956]
ChEMBL Displacement of [3H]5-HT from human cloned 5HT1D receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
ChEMBL Displacement of [3H]5-HT from human recombinant 5HT1D receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5214-5217 [PMID:17629698]
ChEMBL Displacement of [3H]5HT from human recombinant 5HT1D receptor B 8.8 pKi 1.58 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Displacement of [3H]5HT from human cloned 5HT1D receptor expressed in CHO cells B 8.8 pKi 1.58 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5581-5585 [PMID:18829312]
GtoPdb - - 8.8 pKi - - - J. Med. Chem. (2005) 48: 3478-80 [PMID:15887956]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from human cloned 5HT2A receptor expressed in HEK293 cells B 5.5 pKi 3162.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL Displacement of [3H]5-HT from human cloned 5HT2B receptor expressed in HEK293 cells B 5.8 pKi 1584.89 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Displacement of [3H]mesulergine from human cloned 5HT2C receptor expressed in HEK293 cells B 5.1 pKi <7943.28 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HeLa cells B 5 pKi <10000 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL Displacement of [3H]5CT from human cloned 5HT7a receptor expressed in HEK293 cells B 6.7 pKi 199.53 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL Negative logarithm causing 50% receptor occupancy against serotonin transporter B 8.2 pKi 6.31 nM Ki J. Med. Chem. (2005) 48: 6523-6543 [PMID:16220969]
SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652]
ChEMBL Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes B 8 pKi 10 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 5214-5217 [PMID:17629698]
ChEMBL Inhibition of [3H]5HT uptake at SERT in rat cortical synaptosomes B 8 pKi 10 nM Ki J. Med. Chem. (2008) 51: 2887-2890 [PMID:18433113]
ChEMBL Inhibition of [3H]5-HT uptake at SERT in rat cortical synaptosomes B 8.1 pKi 7.94 nM Ki Bioorg. Med. Chem. Lett. (2007) 17: 1033-1036 [PMID:17129726]
ChEMBL Inhibition of [3H]5HT reuptake at SERT in rat cortical synaptosomes B 8.1 pKi 7.94 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 5581-5585 [PMID:18829312]
ChEMBL Mean negative logarithim of binding affinity was measured for the rat serotonin transporter; n>/=3 B 8.2 pKi 6.31 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 737-741 [PMID:15664848]
ChEMBL Inhibition of [3H]5-HT binding to serotonin transporter in rat cortical synaptosomes B 8.4 pKi 3.98 nM Ki J. Med. Chem. (2005) 48: 3478-3480 [PMID:15887956]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]