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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50603992
Substrate
n/a
Meas. Tech.
ChEMBL_2245832 (CHEMBL5160042)
Kd
100±n/a nM
Citation
 Taft, BR; Yokokawa, F; Kirrane, T; Mata, AC; Huang, R; Blaquiere, N; Waldron, G; Zou, B; Simon, O; Vankadara, S; Chan, WL; Ding, M; Sim, S; Straimer, J; Guiguemde, A; Lakshminarayana, SB; Jain, JP; Bodenreider, C; Thompson, C; Lanshoeft, C; Shu, W; Fang, E; Qumber, J; Chan, K; Pei, L; Chen, YL; Schulz, H; Lim, J; Abas, SN; Ang, X; Liu, Y; Angulo-Barturen, I; Jiménez-Díaz, MB; Gamo, FJ; Crespo-Fernandez, B; Rosenthal, PJ; Cooper, RA; Tumwebaze, P; Aguiar, ACC; Campo, B; Campbell, S; Wagner, J; Diagana, TT; Sarko, C Discovery and Preclinical Pharmacology of INE963, a Potent and Fast-Acting Blood-Stage Antimalarial with a High Barrier to Resistance and Potential for Single-Dose Cures in Uncomplicated Malaria. J Med Chem 65:3798-3813 (2022) [PubMed]  Article
Target
Name:
Receptor-type tyrosine-protein kinase FLT3
Synonyms:
CD135 | CD_antigen: CD135 | FL cytokine receptor | FLK-2 | FLK2 | FLT-3 | FLT3 | FLT3_HUMAN | Fetal liver kinase-2 | Fms-like tyrosine kinase 3 | Fms-like tyrosine kinase 3 (Flt-3) | Fms-related tyrosine kinase 3 | STK-1 | STK1 | Stem cell tyrosine kinase 1
Type:
Enzyme
Mol. Mass.:
112888.62
Organism:
Homo sapiens (Human)
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
  
Inhibitor
Name:
BDBM50603992
Synonyms:
CHEMBL5179988
Type:
Small organic molecule
Emp. Form.:
C14H15F2N5S
Mol. Mass.:
323.364
SMILES:
CC(C)(N)CNc1nn2c(cnc2s1)-c1ccc(F)cc1F
Structure:
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