Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50453205
Substrate
n/a
Meas. Tech.
ChEMBL_1749251 (CHEMBL4183761)
IC50
10.0±n/a nM
Citation
 Gucký, T?ezní?ková, ERado?ová Muchová, TJorda, RKlejová, ZMalínková, VBerka, KBazgier, VAjani, HLep?ík, MDivoký, VKry?tof, V Discovery of N J Med Chem 61:3855-3869 (2018) [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:
Human
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
  
Inhibitor
Name:
BDBM50453205
Synonyms:
CHEMBL4218371
Type:
Small organic molecule
Emp. Form.:
C20H26BrN7
Mol. Mass.:
444.371
SMILES:
CC(C)n1cnc2c(Nc3ccc(Br)cc3)nc(N[C@H]3CC[C@H](N)CC3)nc12 |r,wU:22.23,wD:19.19,(6.35,-5.98,;7.84,-5.58,;8.24,-4.09,;8.98,-6.61,;8.82,-8.14,;10.23,-8.77,;11.26,-7.62,;12.8,-7.62,;13.57,-8.96,;15.11,-8.96,;15.88,-7.62,;17.42,-7.62,;18.19,-8.96,;19.73,-8.96,;17.42,-10.29,;15.88,-10.29,;13.57,-6.29,;12.8,-4.96,;13.57,-3.62,;15.11,-3.62,;15.88,-4.96,;17.42,-4.96,;18.19,-3.62,;19.73,-3.62,;17.42,-2.29,;15.88,-2.29,;11.26,-4.96,;10.49,-6.29,)|
Structure:
Search PDB for entries with ligand similarity: