Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3 [563-993,D835Y]

Ligand

BDBM225230

Substrate/Competitor

n/a

Meas. Tech.

HMT Assay

IC50

>1.0e+4±n/a nM

Citation

Qi, W; Zhao, K; Gu, J; Huang, Y; Wang, Y; Zhang, H; Zhang, M; Zhang, J; Yu, Z; Li, L; Teng, L; Chuai, S; Zhang, C; Zhao, M; Chan, H; Chen, Z; Fang, D; Fei, Q; Feng, L; Feng, L; Gao, Y; Ge, H; Ge, X; Li, G; Lingel, A; Lin, Y; Liu, Y; Luo, F; Shi, M; Wang, L; Wang, Z; Yu, Y; Zeng, J; Zeng, C; Zhang, L; Zhang, Q; Zhou, S; Oyang, C; Atadja, P; Li, E An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED. Nat Chem Biol13:381-388 (2017) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Receptor-type tyrosine-protein kinase FLT3 [563-993,D835Y]

Name:

Receptor-type tyrosine-protein kinase FLT3 [563-993,D835Y]

Synonyms:

CD135 | FLK2 | FLT3 | FLT3_HUMAN | Receptor-type tyrosine-protein kinase FLT3 (FLT3) | STK1

Type:

Enzyme

Mol. Mass.:

49836.34

Organism:

Homo sapiens (Human)

Description:

Human FLT3 truncation (563-993 aa) with D835Y mutation

Residue:

431

Sequence:

CHKYKKQFRYESQLQMVQVTGSSDNEYFYVDFREYEYDLKWEFPRENLEFGKVLGSGAFG
KVMNATAYGISKTGVSIQVAVKMLKEKADSSEREALMSELKMMTQLGSHENIVNLLGACT
LSGPIYLIFEYCCYGDLLNYLRSKREKFHRTWTEIFKEHNFSFYPTFQSHPNSSMPGSRE
VQIHPDSDQISGLHGNSFHSEDEIEYENQKRLEEEEDLNVLTFEDLLCFAYQVAKGMEFL
EFKSCVHRDLAARNVLVTHGKVVKICDFGLARYIMSDSNYVVRGNARLPVKWMAPESLFE
GIYTIKSDVWSYGILLWEIFSLGVNPYPGIPVDANFYKLIQNGFKMDQPFYATEEIYIIM
QSCWAFDSRKRPSFPNLTSFLGCQLADAEEAMYQNVDGRVSECPHTYQNRRPFSREMDLG
LLSPQAQVEDS

BDBM225230

n/a

Name

BDBM225230

Synonyms:

EED226 | US11013745, Compound EED226

Type

Small organic molecule

Emp. Form.

C17H15N5O3S

Mol. Mass.

369.398

SMILES

CS(=O)(=O)c1ccc(cc1)-c1cnc(NCc2ccco2)n2cnnc12

Structure