sulindac [Ligand Id: 5425] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL15770 (Arthrocine, Artribid, Clinoril, MK-231, NSC-757344, Sulindac)
  • aldo-keto reductase family 1 member B/Aldose reductase in Human [ChEMBL: CHEMBL1900] [GtoPdb: 2768] [UniProtKB: P15121]
  • aldo-keto reductase family 1 member B/Aldose reductase in Rat [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943]
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  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
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  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
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  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
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  • COX-1 in Human [GtoPdb: 1375] [UniProtKB: P23219]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 32:

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]