Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3

Ligand

BDBM50469375

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_1804043 (CHEMBL4276335)

IC50

1.5±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

BDBM50469375

n/a

Name

BDBM50469375

Synonyms:

CHEMBL4283152

Type

Small organic molecule

Emp. Form.

C27H38N6O

Mol. Mass.

462.6302

SMILES

CCCCNc1ncc2c(cn([C@H]3CC[C@H](O)CC3)c2n1)-c1ccc(cc1)N1CCN(C)CC1 |r,wU:12.11,wD:15.15,(20.68,-20.42,;20.68,-21.96,;22.01,-22.74,;23.34,-21.97,;24.67,-22.74,;26,-21.97,;26,-20.42,;27.33,-19.65,;28.67,-20.42,;30.14,-19.94,;31.05,-21.19,;30.14,-22.45,;30.89,-23.79,;32.43,-23.81,;33.17,-25.17,;32.37,-26.48,;33.11,-27.83,;30.83,-26.45,;30.09,-25.11,;28.67,-21.97,;27.34,-22.74,;30.85,-18.57,;32.39,-18.52,;33.11,-17.15,;32.28,-15.85,;30.74,-15.92,;30.03,-17.28,;32.99,-14.48,;34.53,-14.42,;35.23,-13.06,;34.41,-11.76,;35.12,-10.39,;32.87,-11.83,;32.16,-13.19,)|

Structure