ChEMBL ligand: CHEMBL4439972
large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835] 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
large tumor suppressor kinase 1/Serine/threonine-protein kinase LATS1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6167] [GtoPdb: 1515] [UniProtKB: O95835]
GtoPdb	Inhibition of human LATS1 kinase domain determined in a biochemical fluorescence-based assay	-	9.15	pIC50	0.7	nM	IC50	WO2018198077A2. 6-6 fused bicyclic heteroaryl compounds and their use as lats inhibitors (2018)
ChEMBL	Inhibition of human LATS1 kinase domain (589 to 1130 amino acids) incubated for 1 hr in presence of Fluo-SGKtide substrate by fluorescence detection based biochemical caliper assay	B	9.15	pIC50	0.7	nM	IC50	US-20180344738-A1. 6-6 Fused Bicyclic Heteroaryl Compounds and their Use as LATS Inhibitors (2018)
ChEMBL	LATS1 Biochemical Caliper Assay: The LATS1 biochemical Caliper assay was performed as following.Human LATS1 kinase domain protein was purchased from Carnabio (catalogue number 01-123; lot 15CBS-0098D). Human LATS1, catalytic domain [589-1130(end) amino acids of accession number NP_004681.1] was co-expressed as N-terminal GST-fusion protein (90 kDa) with human His-tagged MOBKL1A [1-216(end) amino acids of accession number NP_775739.1] using baculovirus expression system. GST-LATS1 was purified by using glutathione sepharose chromatography. The substrate (Fluo-SGKtide; Peptide for LATS1; lot BS-41067) has the following sequence: 5-Fluo-Nva-KKRNRRLSVA-amide (SEQ ID NO: 27) x TFA and was purchased from Biosyntan.The reaction is performed in reaction buffer containing 50 mM Hepes pH 7,5; 0.02% Tween20; 0.02% BSA; 1 mM DTT; 10 uM Na3VO4 and 10 mM beta-Glycerolphosphat and fresh added 1 mM MgCl2 and qsp H2O.The substrate solution (2× conc.) in Reaction Buffer contains 300 μM ATP and 4 μM Fluo-SGKtide.The kinase solution (2× conc.) in Reaction Buffer contains 20 nM LATS1 kinase. 4.5 μL of 2× conc. Kinase solution, 50 nL of 1.8 mM compounds and 4.5 μL of substrate solution were added into 384-well plates black small volume from Greiner and incubated at 32° C. for 1 hour. 15 μL of stop buffer containing 100 mM Hepes pH 7,5; 5% DMSO; 0.1% Coating reagent; 10 mM EDTA and 0.02% Brij35 and qsp H2O to each well to terminate the reaction.Substrates and products were electrophoretically separated using the microfluidic-based Caliper EZ Reader System (Caliper Life Sciences) using a 12 sipper chip (cat 760404). The separation takes place in Coating Buffer (idem Stop buffer) and containing 0.1% Coating reagent CR3 and 0.5% coating reagent CR8 (Perkin Elmer).Plates were read using a LED with an excitation at 488 nm and a detection at 520 nm to 5 quantify the fluorescence intensity. The IC50 is measured when the effect of the compound reduces the product fluorescence signal by 50%.	B	9.15	pIC50	0.7	nM	IC50	US-11458138-B2. 6-6 fused bicyclic heteroaryl compounds and their use as LATS inhibitors (2022)

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]
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