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, Sulindaco)
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuAldose reductasepKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd RatpKi RatpIC50 RatpEC50 Rat02468Highcharts.com
  • 5-LOX/Arachidonate 5-lipoxygenase in Rat [ChEMBL: CHEMBL312] [GtoPdb: 1385] [UniProtKB: P12527]
Created with Highcharts 10.3.3ValuesChart context menuArachidonate 5-lipoxygenasepKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuBile salt export pumppKd RatpKi RatpIC50 RatpEC50 Rat012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuComplement C5pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclooxygenase-1pKd SheeppKi SheeppIC50 SheeppEC50 Sheep0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuCyclooxygenase-2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533]
Created with Highcharts 10.3.3ValuesChart context menuEpidermal growth factor receptor erbB1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • glycine receptor α1 subunit/Glycine receptor subunit alpha-1 in Human [ChEMBL: CHEMBL5845] [GtoPdb: 423] [UniProtKB: P23415]
Created with Highcharts 10.3.3ValuesChart context menuGlycine receptor subunit alpha-1pKd HumanpKi HumanpIC50 HumanpEC50 Human02468Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuGlyoxalase IpKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
Created with Highcharts 10.3.3ValuesChart context menuPeroxisome proliferator-activated receptor gammapKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuProstaglandin E synthasepKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • Retinoid X receptor-α/Retinoid X receptor alpha in Human [ChEMBL: CHEMBL2061] [GtoPdb: 610] [UniProtKB: P19793]
Created with Highcharts 10.3.3ValuesChart context menuRetinoid X receptor alphapKd HumanpKi HumanpIC50 HumanpEC50 Human012345Highcharts.com
  • COX-1 in Human [GtoPdb: 1375] [UniProtKB: P23219]
Created with Highcharts 10.3.3ValuesChart context menuCOX-1pKd HumanpKi HumanpIC50 HumanpEC50 Human01234567Highcharts.com
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 35:

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]