Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM50453234
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:
BDBM50453234
Synonyms:
CHEMBL4213717
Type:
Small organic molecule
Emp. Form.:
C25H35N9O
Mol. Mass.:
477.6051
SMILES:
N[C@H]1CC[C@@H](CC1)Nc1nc(Nc2ccc(nc2)N2CCOCC2)c2ncn(C3CCCC3)c2n1 |r,wU:4.7,wD:1.0,(26.32,-12.34,;24.78,-12.34,;24.01,-11,;22.47,-11,;21.7,-12.34,;22.47,-13.67,;24.01,-13.67,;20.16,-12.34,;19.39,-13.67,;20.16,-15,;19.39,-16.34,;20.16,-17.67,;21.7,-17.67,;22.47,-16.34,;24.01,-16.34,;24.78,-17.67,;24.01,-19,;22.47,-19,;26.32,-17.67,;27.09,-16.34,;28.63,-16.34,;29.4,-17.67,;28.63,-19,;27.09,-19,;17.85,-16.34,;16.82,-17.48,;15.41,-16.85,;15.58,-15.32,;14.43,-14.29,;12.93,-14.61,;12.16,-13.28,;13.19,-12.13,;14.59,-12.76,;17.08,-15,;17.85,-13.67,)|
Structure:
Search PDB for entries with ligand similarity: