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Target
Receptor-type tyrosine-protein kinase FLT3
Ligand
BDBM497229
Substrate
n/a
Meas. Tech.
ChEMBL_2129276 (CHEMBL4838705)
IC50
1650±n/a nM
Citation
 Zheng, H; Zhao, J; Li, B; Zhang, W; Stashko, MA; Minson, KA; Huey, MG; Zhou, Y; Earp, HS; Kireev, D; Graham, DK; DeRyckere, D; Frye, SV; Wang, X UNC5293, a potent, orally available and highly MERTK-selective inhibitor. Eur J Med Chem 220:0 (2021) [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:
BDBM497229
Synonyms:
(1S,4R)-4-(2-(((S)-pentan- 2-yl)amino)-5-(1- ((tetrahydro-2H-pyran-4- yl)sulfonyl)piperidin-4-yl)- 7H-pyrrolo[2,3- d]pyrimidin-7- yl)cyclohexan-1-ol | US11001586, Example 2
Type:
Small organic molecule
Emp. Form.:
C27H43N5O4S
Mol. Mass.:
533.726
SMILES:
CCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)C1CCN(CC1)S(=O)(=O)C1CCOCC1 |r,wU:13.12,wD:3.3,16.16,(-8.58,-2.31,;-7.25,-1.54,;-5.92,-2.31,;-4.58,-1.54,;-4.58,,;-3.25,-2.31,;-1.91,-1.54,;-1.91,,;-.58,.77,;.75,,;2.22,.48,;3.12,-.77,;2.22,-2.02,;2.69,-3.48,;4.2,-3.8,;4.68,-5.27,;3.64,-6.41,;4.12,-7.87,;2.14,-6.09,;1.66,-4.63,;.75,-1.54,;-.58,-2.31,;2.69,1.94,;4.2,2.26,;4.68,3.73,;3.64,4.87,;2.14,4.55,;1.66,3.09,;4.12,6.33,;4.12,7.87,;2.63,6.73,;5.61,5.94,;6.01,4.45,;7.49,4.05,;8.58,5.14,;8.18,6.63,;6.7,7.02,)|
Structure:
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