Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50453230
Substrate
n/a
Meas. Tech.
ChEMBL_1749251 (CHEMBL4183761)
IC50
6.0±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:
Homo sapiens (Human)
Description:
P36888
Residue:
993
Sequence:
MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESPEDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDLQNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQDALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRECTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEMSTYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYEIDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHAENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITEGVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQDNISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDSNYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS
  
Inhibitor
Name:
BDBM50453230
Synonyms:
CHEMBL4217517
Type:
Small organic molecule
Emp. Form.:
C33H43N9
Mol. Mass.:
565.7548
SMILES:
N[C@H]1CC[C@@H](CC1)Nc1nc(Nc2ccc(cc2)N2CCN(Cc3ccccc3)CC2)c2ncn(C3CCCC3)c2n1 |r,wU:4.7,wD:1.0,(20.4,-19.7,;21.73,-18.93,;23.06,-19.7,;24.4,-18.93,;24.4,-17.39,;23.06,-16.62,;21.73,-17.39,;25.73,-16.62,;25.73,-15.08,;24.4,-14.31,;24.4,-12.77,;23.06,-12,;21.73,-12.77,;21.73,-14.31,;20.4,-15.08,;19.06,-14.31,;19.06,-12.77,;20.4,-12,;17.73,-15.08,;17.73,-16.62,;16.39,-17.39,;15.06,-16.62,;13.73,-17.39,;12.39,-16.62,;11.06,-17.39,;9.73,-16.62,;9.73,-15.08,;11.06,-14.31,;12.39,-15.08,;15.06,-15.08,;16.39,-14.31,;25.73,-12,;26.05,-10.49,;27.58,-10.33,;28.21,-11.74,;29.71,-12.06,;30.86,-11.03,;32.19,-11.8,;31.87,-13.3,;30.34,-13.46,;27.06,-12.77,;27.06,-14.31,)|
Structure:
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