ChEMBL ligand: CHEMBL2086421
coagulation factor II, thrombin/Prothrombin in Human [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734] There should be some charts here, you may need to enable JavaScript!
Serine protease hepsin in Human [ChEMBL: CHEMBL2079849] [UniProtKB: P05981] There should be some charts here, you may need to enable JavaScript!
ST14 transmembrane serine protease matriptase /Suppressor of tumorigenicity 14 protein in Human [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6] There should be some charts here, you may need to enable JavaScript!
transmembrane serine protease 11D/Transmembrane protease serine 11D in Human [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235] There should be some charts here, you may need to enable JavaScript!
transmembrane serine protease 6/Transmembrane protease serine 6 in Human [ChEMBL: CHEMBL1795139] [GtoPdb: 2422] [UniProtKB: Q8IU80] 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
coagulation factor II, thrombin/Prothrombin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL204] [GtoPdb: 2362] [UniProtKB: P00734]
ChEMBL	Mixed inhibition of human thrombin expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate by fluorimetric analysis	B	6.2	pKi	637	nM	Ki	ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505]
Serine protease hepsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2079849] [UniProtKB: P05981]
ChEMBL	Tight binding inhibition of human hepsin expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis	B	8.96	pKi	1.1	nM	Ki	ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505]
ST14 transmembrane serine protease matriptase /Suppressor of tumorigenicity 14 protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3018] [GtoPdb: 2418] [UniProtKB: Q9Y5Y6]
ChEMBL	Tight binding inhibition of human matriptase expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis	B	10.96	pKi	0.01	nM	Ki	ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505]
GtoPdb	-	-	10.96	pKi	0.01	nM	Ki	ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505]
transmembrane serine protease 11D/Transmembrane protease serine 11D in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795138] [GtoPdb: 2420] [UniProtKB: O60235]
ChEMBL	Tight binding inhibition of human TMPRSS11D expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis	B	8.08	pKi	8.4	nM	Ki	ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505]
GtoPdb	-	-	8.08	pKi	8.4	nM	Ki	ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505]
transmembrane serine protease 6/Transmembrane protease serine 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795139] [GtoPdb: 2422] [UniProtKB: Q8IU80]
GtoPdb	-	-	8.48	pKi	3.3	nM	Ki	ACS Med Chem Lett (2012) 3: 530-4 [PMID:24900505]
ChEMBL	Tight binding inhibition of human matriptase2 expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis	B	8.48	pKi	3.3	nM	Ki	ACS Med Chem Lett (2012) 3: 530-534 [PMID:24900505]
ChEMBL	Matriptase Inhibition: Enzymatic assays and Ki determination were performed at room temperature in an assay buffer containing 50 mM Tris-HCl, 150 mM NaCl and 500 μg/mL BSA at pH 7.4. To determine which method to use for the evaluation of inhibition, 0.25 nM protease was added to a reaction buffer containing 0 nM, 2.5 nM or 1 mM of inhibitors and 200 μM of a fluorogenic substrate (Boc-Gln-Ala-Arg-AMC). Proteolytic activity was monitored by measuring the release of fluorescence (excitation; 360 nm, emission; 441 nm) in a FLX800 TBE microplate reader (Bio-Tek Instruments, Winooski, Vt., USA).	B	10.96	pKi	0.01	nM	Ki	US-10988505-B2. Matriptase inhibitors and uses thereof (2021)

ChEMBL data shown on this page come from version 36:

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]