Reaction Details
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Tyrosine-protein kinase Mer
Ligand
BDBM50573129
Substrate
n/a
Meas. Tech.
ChEMBL_2119091 (CHEMBL4828157)
IC50
16±n/a nM
Citation
McCoull, W; Boyd, S; Brown, MR; Coen, M; Collingwood, O; Davies, NL; Doherty, A; Fairley, G; Goldberg, K; Hardaker, E; He, G; Hennessy, EJ; Hopcroft, P; Hodgson, G; Jackson, A; Jiang, X; Karmokar, A; Lainé, AL; Lindsay, N; Mao, Y; Markandu, R; McMurray, L; McLean, N; Mooney, L; Musgrove, H; Nissink, JWM; Pflug, A; Reddy, VP; Rawlins, PB; Rivers, E; Schimpl, M; Smith, GF; Tentarelli, S; Travers, J; Troup, RI; Walton, J; Wang, C; Wilkinson, S; Williamson, B; Winter-Holt, J; Yang, D; Zheng, Y; Zhu, Q; Smith, PD Optimization of an Imidazo[1,2- J Med Chem 64:13524-13539 (2021) [PubMed] Article More Info.:
Target
Name:
Tyrosine-protein kinase Mer
Synonyms:
MER | MER intracellular domain/EGFR extracellular domain chimera | MERTK | MERTK_HUMAN | Proto-oncogene c-Mer | Proto-oncogene tyrosine-protein kinase MER | Receptor tyrosine kinase MerTK | Tyrosine-protein kinase Mer
Type:
PROTEIN
Mol. Mass.:
110234.77
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1498723
Residue:
999
Sequence:
MGPAPLPLLLGLFLPALWRRAITEAREEAKPYPLFPGPFPGSLQTDHTPLLSLPHASGYQPALMFSPTQPGRPHTGNVAIPQVTSVESKPLPPLAFKHTVGHIILSEHKGVKFNCSISVPNIYQDTTISWWKDGKELLGAHHAITQFYPDDEVTAIIASFSITSVQRSDNGSYICKMKINNEEIVSDPIYIEVQGLPHFTKQPESMNVTRNTAFNLTCQAVGPPEPVNIFWVQNSSRVNEQPEKSPSVLTVPGLTEMAVFSCEAHNDKGLTVSKGVQINIKAIPSPPTEVSIRNSTAHSILISWVPGFDGYSPFRNCSIQVKEADPLSNGSVMIFNTSALPHLYQIKQLQALANYSIGVSCMNEIGWSAVSPWILASTTEGAPSVAPLNVTVFLNESSDNVDIRWMKPPTKQQDGELVGYRISHVWQSAGISKELLEEVGQNGSRARISVQVHNATCTVRIAAVTRGGVGPFSDPVKIFIPAHGWVDYAPSSTPAPGNADPVLIIFGCFCGFILIGLILYISLAIRKRVQETKFGNAFTEEDSELVVNYIAKKSFCRRAIELTLHSLGVSEELQNKLEDVVIDRNLLILGKILGEGEFGSVMEGNLKQEDGTSLKVAVKTMKLDNSSQREIEEFLSEAACMKDFSHPNVIRLLGVCIEMSSQGIPKPMVILPFMKYGDLHTYLLYSRLETGPKHIPLQTLLKFMVDIALGMEYLSNRNFLHRDLAARNCMLRDDMTVCVADFGLSKKIYSGDYYRQGRIAKMPVKWIAIESLADRVYTSKSDVWAFGVTMWEIATRGMTPYPGVQNHEMYDYLLHGHRLKQPEDCLDELYEIMYSCWRTDPLDRPTFSVLRLQLEKLLESLPDVRNQADVIYVNTQLLESSEGLAQGSTLAPLDLNIDPDSIIASCTPRAAISVVTAEVHDSKPHEGRYILNGGSEEWEDLTSAPSAAVTAEKNSVLPGERLVRNGVSWSHSSMLPLGSSLPDELLFADDSSEGSEVLM
Inhibitor
Name:
BDBM50573129
Synonyms:
CHEMBL4872116
Type:
Small organic molecule
Emp. Form.:
C24H25N7O2
Mol. Mass.:
443.501
SMILES:
COc1cc(ccc1-c1nnc(o1)N(C)Cc1ccc2nccn2c1)-c1c(C)nn(C)c1C
Structure:
