Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3

Ligand

BDBM50469376

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1804043 (CHEMBL4276335)

IC50

0.900000±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

BDBM50469376

n/a

Name

BDBM50469376

Synonyms:

CHEMBL4284541

Type

Small organic molecule

Emp. Form.

C30H42N6O

Mol. Mass.

502.6941

SMILES

CCCCNc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(cc1)C1(CC1)N1CCN(C)CC1 |r,wU:12.11,wD:15.15,(16.6,-19.72,;16.59,-21.26,;17.92,-22.04,;19.25,-21.27,;20.58,-22.04,;21.91,-21.27,;21.91,-19.73,;23.24,-18.96,;24.58,-19.72,;26.05,-19.24,;26.96,-20.49,;26.05,-21.75,;26.8,-23.09,;28.33,-23.11,;29.08,-24.47,;28.28,-25.78,;29.02,-27.13,;26.74,-25.75,;26,-24.41,;24.58,-21.27,;23.25,-22.04,;26.76,-17.88,;28.3,-17.82,;29.01,-16.45,;28.19,-15.15,;26.64,-15.22,;25.94,-16.59,;28.9,-13.79,;27.4,-13.38,;28.5,-12.29,;30.44,-13.72,;31.26,-15.03,;32.79,-14.97,;33.51,-13.6,;35.05,-13.54,;32.69,-12.3,;31.14,-12.36,)|

Structure