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ChEMBL ligand: CHEMBL15770 (Arthrocine, Artribid, Clinoril, MK-231, NSC-757344, Sulindac) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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aldo-keto reductase family 1 member B/Aldose reductase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121] | ||||||||
ChEMBL | Inhibition of Homo sapiens (human) aldose reductase | B | 6.43 | pIC50 | 374 | nM | IC50 | Med Chem Res (2013) 22: 3589-3605 |
aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943] | ||||||||
ChEMBL | DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) | B | 6.36 | pIC50 | 435 | nM | IC50 | DrugMatrix in vitro pharmacology data |
5-LOX/Arachidonate 5-lipoxygenase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527] | ||||||||
ChEMBL | Inhibition of 5-lipoxygenase in intact RBL-1 cell line | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (1990) 33: 2070-2072 [PMID:2115586] |
ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 4.06 | pIC50 | 87500 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
Complement C5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2364163] [UniProtKB: P01031] | ||||||||
ChEMBL | Binding affinity to human C5a assessed as dissociation constant after 1 hr by circular dichroism analysis | B | 6.24 | pKd | 570 | nM | Kd | Bioorg Med Chem (2019) 27: 115052-115052 [PMID:31447248] |
Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
ChEMBL | Inhibition of Ovine COX-1 preincubated for 15 mins by fluorescence analysis | B | 4.8 | pIC50 | 16000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
ChEMBL | Inhibition of recombinant human COX-2 preincubated for 15 mins by fluorescence analysis | B | 5.06 | pIC50 | 8800 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
GtoPdb | - | - | 5.47 | pIC50 | 3400 | nM | IC50 | Cancer Cell (2010) 17: 560-73 [PMID:20541701] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of EGFR (unknown origin) using tyrosine 4 as substrate by fluorescence analysis | B | 5 | pIC50 | >10000 | nM | IC50 | ACS Med Chem Lett (2015) 6: 1086-1090 [PMID:26487917] |
glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415] | ||||||||
ChEMBL | Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-electrode voltage clamp assay | B | 6.42 | pEC50 | 380 | nM | EC50 | J Med Chem (2015) 58: 2958-2966 [PMID:25790278] |
Glyoxalase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424] [UniProtKB: Q04760] | ||||||||
ChEMBL | Inhibition of glyoxalase 1 | B | 4.11 | pKi | 77900 | nM | Ki | Bioorg Med Chem (2011) 19: 1189-1196 [PMID:21237663] |
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
ChEMBL | Binding affinity to GAL4-DBD-fused PPARgamma ligand binding domain (unknown origin) expressed in HEK293T cells by spectra-fluorophotometry analysis | B | 4 | pKd | >100000 | nM | Kd | Eur J Med Chem (2021) 222: 113542-113542 [PMID:34118723] |
ChEMBL | Partial agonist activity at GAL4 DBD-fused PPARgamma LBD (unknown origin) expressed in pG5 luc and pBIND transfected HEK293T cells assessed as transcriptional activation incubated for 12 hrs by fluorescence based luciferase assay | B | 4.64 | pEC50 | 22650 | nM | EC50 | Eur J Med Chem (2021) 222: 113542-113542 [PMID:34118723] |
mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
ChEMBL | Inhibition of microsomal PGES | B | 4.1 | pIC50 | 80000 | nM | IC50 | Bioorg Med Chem (2011) 19: 6077-6086 [PMID:21920764] |
Retinoid X receptor-α/Retinoid X receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793] | ||||||||
ChEMBL | Displacement of [3H]-9-cis-RA from RXRalpha (unknown origin) by liquid scintillation counting | B | 4.08 | pIC50 | 82900 | nM | IC50 | Eur J Med Chem (2013) 62: 632-648 [PMID:23434637] |
GtoPdb | RXRα binding | - | 4.1 | pIC50 | 80000 | nM | IC50 | Cancer Cell (2010) 17: 560-73 [PMID:20541701] |
COX-1 in Human [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
GtoPdb | - | - | 5.92 | pIC50 | 1200 | nM | IC50 | Cancer Cell (2010) 17: 560-73 [PMID:20541701] |
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]