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

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ChEMBL ligand: CHEMBL2018969 (GSK2239633A)
  • ADGRF1/Adhesion G-protein coupled receptor F1 in Human [ChEMBL: CHEMBL4523872] [GtoPdb: 190] [UniProtKB: Q5T601]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
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  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
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  • CCR2/C-C chemokine receptor type 2 in Human [ChEMBL: CHEMBL4015] [GtoPdb: 59] [UniProtKB: P41597]
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  • CCR4/C-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2414] [GtoPdb: 61] [UniProtKB: P51679]
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
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  • CCR8/C-C chemokine receptor type 8 in Human [ChEMBL: CHEMBL4596] [GtoPdb: 65] [UniProtKB: P51685]
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  • CX3CR1/C-X3-C chemokine receptor 1 in Human [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238]
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  • CXCR3/C-X-C chemokine receptor type 3 in Human [ChEMBL: CHEMBL4441] [GtoPdb: 70] [UniProtKB: P49682]
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  • CXCR4/C-X-C chemokine receptor type 4 in Human [ChEMBL: CHEMBL2107] [GtoPdb: 71] [UniProtKB: P61073]
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  • GLP-1 receptor/Glucagon-like peptide 1 receptor in Human [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
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  • FFA4 receptor/G-protein coupled receptor 120 in Human [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
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  • CXCR1/Interleukin-8 receptor A in Human [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024]
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  • CXCR2/Interleukin-8 receptor B in Human [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025]
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  • OATP1B1/Solute carrier organic anion transporter family member 1B1 in Human [ChEMBL: CHEMBL1697668] [GtoPdb: 1220] [UniProtKB: Q9Y6L6]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ADGRF1/Adhesion G-protein coupled receptor F1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523872] [GtoPdb: 190] [UniProtKB: Q5T601]
ChEMBL GPCR PRESTO-Tango dose-response in agonist mode with target: ADGRF1 F 5 pEC50 >10000 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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]
CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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]
GLP-1 receptor/Glucagon-like peptide 1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1784] [GtoPdb: 249] [UniProtKB: P43220]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: GLP1R F 5 pIC50 >10000 nM IC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3]
ChEMBL GPCR PRESTO-Tango dose-response in antagonist mode with target: FFAR4 F 5.39 pEC50 4114.12 nM EC50 EUbOPEN Chemogenomics Library - GPCR Dose-Respose
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]