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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 |
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histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
ChEMBL | Determination of IC50 values for inhibition of enzymatic assay of human HDAC6 with custom peptide substrate | B | 6.21 | pIC50 | 612.5 | nM | IC50 | HDAC6 screening dataset using tau-based substrate in an enzymatic assay yields selective inhibitors and activators |
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] |
ChEMBL | Displacement of 125I-IL-8 from CXCR2 (unknown origin) expressed in CHO cell membrane incubated for 1 hr by liquid scintillation counter analysis | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2023) 250: 115175-115175 [PMID:36780833] |
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 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]