Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50453192
Substrate
n/a
Meas. Tech.
ChEMBL_1749251 (CHEMBL4183761)
IC50
4.0±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:
BDBM50453192
Synonyms:
CHEMBL4216043
Type:
Small organic molecule
Emp. Form.:
C27H36N8O
Mol. Mass.:
488.6277
SMILES:
N[C@H]1CC[C@@H](CC1)Nc1nc(Nc2ccc(cc2)N2CC3(COC3)C2)c2ncn(C3CCCC3)c2n1 |r,wU:4.7,wD:1.0,(16.44,-9.37,;17.21,-10.71,;16.44,-12.04,;17.21,-13.38,;18.75,-13.38,;19.52,-12.04,;18.75,-10.71,;19.52,-14.71,;18.75,-16.04,;19.52,-17.38,;18.75,-18.71,;19.52,-20.04,;21.06,-20.04,;21.83,-18.71,;23.37,-18.71,;24.14,-20.04,;23.37,-21.38,;21.83,-21.38,;25.68,-20.04,;26.77,-21.13,;27.86,-20.04,;28.95,-18.96,;30.04,-20.04,;28.95,-21.13,;26.77,-18.96,;17.21,-18.71,;16.18,-19.85,;14.78,-19.23,;14.94,-17.7,;13.79,-16.67,;12.29,-16.99,;11.52,-15.65,;12.55,-14.51,;13.95,-15.13,;16.44,-17.38,;17.21,-16.04,)|
Structure:
Search PDB for entries with ligand similarity: