SB-282241 [Ligand Id: 782] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL432713 (TCMDC-139245) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597] | ||||||||
| ChEMBL | Binding affinity of compound (10 uM) towards H121A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 5.6 | pKi | 2511.89 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards Y210A-292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 5.61 | pKi | 2454.71 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards H121A/T292A receptor variant (double mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 5.68 | pKi | 2089.3 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards T292A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.14 | pKi | 724.44 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards Y1210A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.25 | pKi | 562.34 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards D284A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.64 | pKi | 229.09 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards Q288A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.77 | pKi | 169.82 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards H121F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.78 | pKi | 165.96 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards T290A receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 6.89 | pKi | 128.82 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| GtoPdb | - | - | 7 | pKi | - | - | - | J Med Chem (2003) 46: 4070-86 [PMID:12954060] |
| ChEMBL | Binding affinity of compound (10 uM) towards WT receptor variant (mutant C-C chemokine receptor type 2) using radioligand [125I]MCP-1 in HEK 293 cells | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Antagonist activity at human CCR2 receptor | F | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1450-1456 [PMID:18226895] |
| ChEMBL | Binding displacement of [125I]MCP-1 (0.14 nM) was measured on CHO cell membranes expressing human CCR2 (C-C chemokine receptor type 2) | B | 7.3 | pKi | 50.12 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells | B | 7.3 | pKi | 50.12 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| ChEMBL | Inhibition of [125I]MCP-1 binding to the cloned C-C chemokine receptor type 2B expressed in CHO cells | B | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| ChEMBL | Binding affinity at C-C chemokine receptor type 2 was determined | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| ChEMBL | Antagonist activity against C-C chemokine receptor type 2 | F | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1803-1806 [PMID:10969972] |
| ChEMBL | Displacement of [125I]MCP1 from human CCR2 expressed in CHO cells | B | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 3735-3739 [PMID:16698264] |
| ChEMBL | Antagonist activity at human CCR2 receptor | F | 7.3 | pKi | 50 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 1450-1456 [PMID:18226895] |
| ChEMBL | Binding affinity of compound (10 uM) towards Y49F receptor variant (mutant CCR2 receptor) using radioligand [125I]MCP-1 in HEK 293 cells | B | 7.78 | pKi | 16.6 | nM | Ki | J Med Chem (2003) 46: 4070-4086 [PMID:12954060] |
| CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
| ChEMBL | Compound was evaluated for the antagonist activity against C-C chemokine receptor type 5 | F | 5.37 | pKi | 4260 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1803-1806 [PMID:10969972] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Binding affinity for Dopamine receptor D2 was determined | B | 7.8 | pKi | 15.85 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Binding affinity for Dopamine receptor D3 was determined | B | 8.1 | pKi | 7.94 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1A receptor was determined | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1B receptor was determined | B | 7.9 | pKi | 12.59 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1E receptor was determined | B | 8.2 | pKi | 6.31 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 1F receptor was determined | B | 8.5 | pKi | 3.16 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 2A receptor was determined | B | 7.7 | pKi | 19.95 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 2B receptor was determined | B | 7.6 | pKi | 25.12 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 2C receptor was determined | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 6 receptor was determined | B | 7.1 | pKi | 79.43 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Binding affinity for 5-hydroxytryptamine 7 receptor was determined | B | 7.2 | pKi | 63.1 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 2177-2180 [PMID:11514164] |
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]
