GSK2239633A [Ligand Id: 10416] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2018969 (GSK2239633A)
  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
  • This target only has 0 pki data point
1 CHEMBL2018969_lig_chart_1 C-C chemokine receptor type 1 Human
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  • CCR10/C-C chemokine receptor type 10 in Human [ChEMBL: CHEMBL2321628] [GtoPdb: 67] [UniProtKB: P46092]
  • This target only has 0 pki data point
2 CHEMBL2018969_lig_chart_2 C-C chemokine receptor type 10 Human
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
  • This target only has 0 pki data point
3 CHEMBL2018969_lig_chart_3 C-C chemokine receptor type 2 Human
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  • CCR4/C-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
  • This target only has 1 pki data point
4 CHEMBL2018969_lig_chart_4 C-C chemokine receptor type 4 Human
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
  • This target only has 0 pki data point
5 CHEMBL2018969_lig_chart_5 C-C chemokine receptor type 5 Human
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  • CCR8/C-C chemokine receptor type 8 in Human [ChEMBL: CHEMBL4596] [GtoPdb: 65] [UniProtKB: P51685]
  • This target only has 0 pki data point
6 CHEMBL2018969_lig_chart_6 C-C chemokine receptor type 8 Human
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  • CXCR3/C-X-C chemokine receptor type 3 in Human [ChEMBL: CHEMBL4441] [GtoPdb: 70] [UniProtKB: P49682]
  • This target only has 0 pki data point
7 CHEMBL2018969_lig_chart_7 C-X-C chemokine receptor type 3 Human
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  • CXCR4/C-X-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
  • This target only has 0 pki data point
8 CHEMBL2018969_lig_chart_8 C-X-C chemokine receptor type 4 Human
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  • CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
  • This target only has 0 pki data point
9 CHEMBL2018969_lig_chart_9 Interleukin-8 receptor A Human
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  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
  • This target only has 0 pki data point
10 CHEMBL2018969_lig_chart_10 Interleukin-8 receptor B Human
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
  • This target only has 0 pki data point
11 CHEMBL2018969_lig_chart_11 Solute carrier organic anion transporter family member 1B1 Human
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
ChEMBL Antagonist activity at CCR1 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CCR10/C-C chemokine receptor type 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321628] [GtoPdb: 67] [UniProtKB: P46092]
ChEMBL Antagonist activity at CCR10 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CCR2/C-C chemokine receptor type 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
ChEMBL Antagonist activity at CCR2 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CCR4/C-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
ChEMBL Antagonist activity at human CCR4 in human whole blood assessed as inhibition of TARC-induced CD4+ CCR4+lymphocyte chemotaxis measuring F-actin content F 6.2 pKd 630.96 nM Kd Bioorg. Med. Chem. Lett. (2012) 22: 2730-2733 [PMID:22437117]
ChEMBL Antagonist activity at CCR4 receptor in human whole blood assessed as F-actin polymerization after 30 mins by FACS-based flow cytometric analysis B 6.2 pKd 630.96 nM Kd J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
ChEMBL Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry B 6.2 pKd 630.96 nM Kd Eur. J. Med. Chem. (2016) 115: 14-25 [PMID:26991939]
ChEMBL Displacement of [125I]TARC from human CCR4 expressed in CHO membranes by SPA B 8 pKi 10 nM Ki Bioorg. Med. Chem. Lett. (2012) 22: 2730-2733 [PMID:22437117]
ChEMBL Antagonist activity at human recombinant CCR4 receptor expressed in CHO cell membranes by [35S]GTPgammaS binding assay F 7.4 pIC50 39.81 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
GtoPdb IC50 determined in a GTPγS binding assay using membranes from CHO cells expressing human recombinant CCR4 receptor. - 7.83 pIC50 14.8 nM IC50 J. Med. Chem. (2013) 56: 1946-60 [PMID:23409871]
ChEMBL Antagonist activity at human CCR4 expressed in CHO membranes assessed as inhibition of [35S]-GTPgammaS binding by scintillation counting F 7.83 pIC50 14.79 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 2730-2733 [PMID:22437117]
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
GtoPdb IC50 determined in a GTPγS binding assay using membranes from CHO cells expressing recombinant CCR5 receptor. - 5.2 pIC50 6310 nM IC50 J. Med. Chem. (2013) 56: 1946-60 [PMID:23409871]
ChEMBL Antagonist activity at CCR5 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5.2 pIC50 6309.57 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CCR8/C-C chemokine receptor type 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4596] [GtoPdb: 65] [UniProtKB: P51685]
ChEMBL Antagonist activity at CCR8 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CXCR3/C-X-C chemokine receptor type 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4441] [GtoPdb: 70] [UniProtKB: P49682]
ChEMBL Antagonist activity at CXCR3 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CXCR4/C-X-C chemokine receptor type 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
ChEMBL Antagonist activity at CXCR4 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
ChEMBL Antagonist activity at CXCR1 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
ChEMBL Antagonist activity at CXCR2 receptor (unknown origin) by [35S]GTPgammaS binding assay F 5 pIC50 >10000 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]
OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
ChEMBL Antagonist activity at OATP1B1 (unknown origin) by [35S]GTPgammaS binding assay F 6.4 pIC50 398.11 nM IC50 J. Med. Chem. (2013) 56: 1946-1960 [PMID:23409871]

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]