SB 649915 [Ligand Id: 76] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL183460 (SB-649915) |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
