SB 225002 [Ligand Id: 833] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL239767 (SB-225002) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CXCR1/Interleukin-8 receptor A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4029] [GtoPdb: 68] [UniProtKB: P25024] | ||||||||
| ChEMBL | Binding affinity to CXCR1 | B | 5.52 | pIC50 | >3000 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ChEMBL | Antagonist activity at CXCR1 assessed as inhibition of CXCL8 binding by cell based assay | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| CXCR2/Interleukin-8 receptor B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2434] [GtoPdb: 69] [UniProtKB: P25025] | ||||||||
| ChEMBL | Antagonist activity against CXCR2 (unknown origin) by calcium flux assay | F | 6.7 | pIC50 | 197.5 | nM | IC50 | Eur J Med Chem (2021) 226: 113812-113812 [PMID:34536673] |
| ChEMBL | Antagonist activity at human CXCR2 expressed in HEK293 cells assessed as inhibition of CXCL8-induced intracellular Ca2+ release by fluorescence based calcium flux assay | F | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2014) 57: 8378-8397 [PMID:25254640] |
| ChEMBL | Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay | F | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2014) 57: 8378-8397 [PMID:25254640] |
| ChEMBL | Displacement of [125I]IL8 from human recombinant CXCR2 expressed in CHO cells | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 1713-1717 [PMID:17236763] |
| ChEMBL | Binding affinity to CXCR2 | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| GtoPdb | - | - | 7.7 | pIC50 | 19.9 | nM | IC50 | J Biol Chem (1998) 273: 10095-8 [PMID:9553055] |
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]
