Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3

Ligand

BDBM50469371

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1804043 (CHEMBL4276335)

IC50

544±n/a nM

Citation

Zhao, J; Zhang, D; Zhang, W; Stashko, MA; DeRyckere, D; Vasileiadi, E; Parker, RE; Hunter, D; Liu, Q; Zhang, Y; Norris-Drouin, J; Li, B; Drewry, DH; Kireev, D; Graham, DK; Earp, HS; Frye, SV; Wang, X Highly Selective MERTK Inhibitors Achieved by a Single Methyl Group. J Med Chem61:10242-10254 (2018) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Receptor-type tyrosine-protein kinase FLT3

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:

MPALARDGGQLPLLVVFSAMIFGTITNQDLPVIKCVLINHKNNDSSVGKSSSYPMVSESP
EDLGCALRPQSSGTVYEAAAVEVDVSASITLQVLVDAPGNISCLWVFKHSSLNCQPHFDL
QNRGVVSMVILKMTETQAGEYLLFIQSEATNYTILFTVSIRNTLLYTLRRPYFRKMENQD
ALVCISESVPEPIVEWVLCDSQGESCKEESPAVVKKEEKVLHELFGTDIRCCARNELGRE
CTRLFTIDLNQTPQTTLPQLFLKVGEPLWIRCKAVHVNHGFGLTWELENKALEEGNYFEM
STYSTNRTMIRILFAFVSSVARNDTGYYTCSSSKHPSQSALVTIVEKGFINATNSSEDYE
IDQYEEFCFSVRFKAYPQIRCTWTFSRKSFPCEQKGLDNGYSISKFCNHKHQPGEYIFHA
ENDDAQFTKMFTLNIRRKPQVLAEASASQASCFSDGYPLPSWTWKKCSDKSPNCTEEITE
GVWNRKANRKVFGQWVSSSTLNMSEAIKGFLVKCCAYNSLGTSCETILLNSPGPFPFIQD
NISFYATIGVCLLFIVVLTLLICHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYD
LKWEFPRENLEFGKVLGSGAFGKVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMS
ELKMMTQLGSHENIVNLLGACTLSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKE
HNFSFYPTFQSHPNSSMPGSREVQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDL
NVLTFEDLLCFAYQVAKGMEFLEFKSCVHRDLAARNVLVTHGKVVKICDFGLARDIMSDS
NYVVRGNARLPVKWMAPESLFEGIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYK
LIQNGFKMDQPFYATEEIYIIMQSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDG
RVSECPHTYQNRRPFSREMDLGLLSPQAQVEDS

BDBM50469371

n/a

Name

BDBM50469371

Synonyms:

CHEMBL4288009

Type

Small organic molecule

Emp. Form.

C31H46N6O

Mol. Mass.

518.7365

SMILES

CCCCC[C@H](C)Nc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(CN2CCN(C)CC2)cc1 |r,wU:15.14,wD:18.18,5.5,(16.65,-22.53,;17.99,-21.76,;19.32,-22.53,;20.65,-21.76,;21.99,-22.53,;23.32,-21.76,;23.32,-20.22,;24.65,-22.54,;25.99,-21.77,;25.99,-20.22,;27.32,-19.45,;28.65,-20.22,;30.13,-19.74,;31.04,-20.99,;30.13,-22.24,;30.88,-23.59,;32.41,-23.61,;33.16,-24.97,;32.36,-26.28,;33.1,-27.63,;30.82,-26.25,;30.08,-24.91,;28.66,-21.77,;27.32,-22.54,;30.84,-18.37,;32.38,-18.31,;33.1,-16.95,;32.27,-15.65,;32.98,-14.28,;34.52,-14.21,;35.34,-15.52,;36.88,-15.46,;37.6,-14.1,;39.13,-14.04,;36.77,-12.79,;35.23,-12.85,;30.72,-15.72,;30.02,-17.08,)|

Structure