ChEMBL ligand: CHEMBL63323 (Niflugel, Niflumic acid, NSC-758196, UP 83, UP-83)
COX-1 /Cyclooxygenase-1 in Human [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] There should be some charts here, you may need to enable JavaScript!
COX-2 /Cyclooxygenase-2 in Human [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] There should be some charts here, you may need to enable JavaScript!
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127] There should be some charts here, you may need to enable JavaScript!
GPR35/G-protein coupled receptor 35 in Human [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] There should be some charts here, you may need to enable JavaScript!
TEA domain transcription factor 4/Transcriptional enhancer factor TEF-3 in Human [ChEMBL: CHEMBL4295828] [GtoPdb: 3243] [UniProtKB: Q15561] There should be some charts here, you may need to enable JavaScript!
Transcription factor SOX-18 in Mouse [ChEMBL: CHEMBL4523228] [UniProtKB: P43680] There should be some charts here, you may need to enable JavaScript!
transthyretin/Transthyretin in Human [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766] There should be some charts here, you may need to enable JavaScript!
KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3] There should be some charts here, you may need to enable JavaScript!
TRPA1 in Rat [GtoPdb: 485] [UniProtKB: Q6RI86] There should be some charts here, you may need to enable JavaScript!
ClC-Ka in Human [GtoPdb: 700] [UniProtKB: P51800] There should be some charts here, you may need to enable JavaScript!
ClC-Kb in Human [GtoPdb: 701] [UniProtKB: P51801] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219]
ChEMBL	DRUGMATRIX: Cyclooxygenase COX-1 enzyme inhibition (substrate: Arachidonic acid)	B	5.97	pIC50	1064	nM	IC50	DrugMatrix in vitro pharmacology data
COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354]
ChEMBL	DRUGMATRIX: Cyclooxygenase COX-2 enzyme inhibition (substrate: Arachidonic acid)	B	6.04	pIC50	918	nM	IC50	DrugMatrix in vitro pharmacology data
dihydroorotate dehydrogenase (quinone)/Dihydroorotate dehydrogenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1966] [GtoPdb: 2604] [UniProtKB: Q02127]
ChEMBL	Inhibition of human recombinant DHODH	B	4.77	pIC50	17000	nM	IC50	ACS Med Chem Lett (2016) 7: 1112-1117 [PMID:27994748]
GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97]
ChEMBL	Displacement of [3H]PSB-13253 from human recombinant GPR35 exprssed in CHO cells by liquid scintillation counting analysis	B	5.44	pKi	3610	nM	Ki	J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL	Desensitization of GPR35 receptor in human HT-29 cells assessed as inhibition of zaprinast-induced dynamic mass redistribution after 10 mins	B	5.89	pIC50	1280	nM	IC50	ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
ChEMBL	Agonist activity at GPR35 receptor in human U2OS cells coexpressing Gal4-VP16-TEV assessed as beta arrestin translocation after 5 hrs by beta lactamase reporter gene assay	F	4.4	pEC50	40200	nM	EC50	ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
ChEMBL	Agonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay	B	4.51	pEC50	30800	nM	EC50	J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL	Agonist activity at human GPR35 expressed in HEK293T cells at 5 uM by EYPF-based beta-arrestin-2 luciferase reporter gene assay	B	4.82	pEC50	15000	nM	EC50	J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
ChEMBL	Agonist activity at GPR35 receptor in human HT-29 cells after 10 mins by dynamic mass redistribution assay	F	5.94	pEC50	1150	nM	EC50	ACS Med Chem Lett (2012) 3: 165-169 [PMID:24900447]
ChEMBL	Agonist activity at human GPR35 by DMR assay	B	5.95	pEC50	1110	nM	EC50	J Med Chem (2013) 56: 7084-7099 [PMID:23888932]
TEA domain transcription factor 4/Transcriptional enhancer factor TEF-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4295828] [GtoPdb: 3243] [UniProtKB: Q15561]
ChEMBL	Binding affinity to human His-tagged TEAD4 YBD (217 to 434 residues) expressed in Escherichia coli BL21(DE3) after 30 mins by ITC assay	B	4.55	pKd	28000	nM	Kd	J Med Chem (2018) 61: 5057-5072 [PMID:29251924]
ChEMBL	Binding affinity to N-terminal His6-tagged human TEAD4 YAP binding domain (217 to 434 residues) expressed in Escherichia coli C43 (DE3) cells by ITC method	B	4.55	pKd	28000	nM	Kd	J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
ChEMBL	Binding affinity to His-tagged TEAD4 YPD domain (217 to 434 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) by isothermal titration calorimetry	B	4.55	pKd	28000	nM	Kd	Eur J Med Chem (2021) 226: 113835-113835 [PMID:34509860]
ChEMBL	Inhibition of CPM binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by CPM addition and measured after 1 hr by fluorescence assay	B	4.38	pIC50	41900	nM	IC50	J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
ChEMBL	Inhibition of FITC-labeled palmitate tracer binding to N-terminal His6-tagged human TEAD4 (217 to 434 residues) expressed in Escherichia coli BL21-CodonPlus (DE3)-RIPL cells preincubated for 10 mins followed by FITC-labeled palmitate tracer addition and measured after 1 hr by fluorescence assay	B	5.23	pIC50	5900	nM	IC50	J Med Chem (2020) 63: 11972-11989 [PMID:32907324]
Transcription factor SOX-18 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523228] [UniProtKB: P43680]
ChEMBL	Inhibition of mouse SOX18 expressed in African green monkey COS7 cells assessed as reduction in SOX18 transcriptional activity by luciferase reporter gene assay	B	4.3	pIC50	50500	nM	IC50	WO-2018112545-A1. Inhibitors of sox18 protein activity for treating angiogenesis- and/or lymphangiogenesis-related diseases (null)
transthyretin/Transthyretin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3194] [GtoPdb: 2851] [UniProtKB: P02766]
ChEMBL	Binding affinity to TTR (unknown origin) by isothermal titration calorimetric analysis	B	6.59	pKd	260	nM	Kd	J Med Chem (2015) 58: 6507-6515 [PMID:26214366]
ChEMBL	FP Assay: The FP assay was then adapted for HTS and used to screen ~120,000 small molecule library for compounds that displaced probe 5 from the T4 binding of TTR. The FP assay was performed in 384-well plate using very low concentration of probe 5 (1.5 nM) and TTR (50 nM) in a 10 μL assay volume. A detergent (0.01% Triton-X100) was added to the assay buffer to avoid any false positive hits from promiscuous, aggregate-based inhibitors. The assay demonstrated robust performance, with a very good dynamic range (−70-230 mP) and a Z′ factor in the range of 0.57-0.78 (FIGS. 4A and 4B). "Hits" were defined as compounds that resulted in at least 50% decrease in fluorescence polarization and demonstrated relative fluorescence between 70 and 130%. Many fluorescence quenchers and enhancers having less than 70% and greater than 130% total fluorescence relative to a control, respectively, were excluded from the hit list. 200 compounds were designated as positive hits (0.167% hit rate).	B	6.54	pIC50	289	nM	IC50	US-8877795-B2. Identification of stabilizers of multimeric proteins (2014)
KNa1.2 in Human [GtoPdb: 386] [UniProtKB: Q6UVM3]
GtoPdb	-	-	8.68	pEC50	2.1	nM	EC50	J Gen Physiol (2010) 135: 275-95 [PMID:20176855]; Mol Pharmacol (2012) 82: 795-802 [PMID:22851714]
TRPA1 in Rat [GtoPdb: 485] [UniProtKB: Q6RI86]
GtoPdb	Two electrode voltage clamp	-	3.3	pEC50	-	-	-	Pflugers Arch (2010) 459: 579-92 [PMID:19888597]
ClC-Ka in Human [GtoPdb: 700] [UniProtKB: P51800]
GtoPdb	-	-	5	pEC50	10000	nM	EC50
ClC-Kb in Human [GtoPdb: 701] [UniProtKB: P51801]
GtoPdb	-	-	5	pEC50	10000	nM	EC50

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]