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: CHEMBL2018969 (GSK2239633A) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 |
---|---|---|---|---|---|---|---|---|
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 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]