SB-282241 [Ligand Id: 782] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL432713 (TCMDC-139245)
  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
There should be some charts here, you may need to enable JavaScript!
  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
There should be some charts here, you may need to enable JavaScript!
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
There should be some charts here, you may need to enable JavaScript!
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 28:

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]