Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3

Ligand

BDBM50563641

Substrate/Competitor

n/a

Meas. Tech.

ChEMBL_2083409 (CHEMBL4739200)

IC50

1585±n/a nM

Citation

Nissink, JWM; Bazzaz, S; Blackett, C; Clark, MA; Collingwood, O; Disch, JS; Gikunju, D; Goldberg, K; Guilinger, JP; Hardaker, E; Hennessy, EJ; Jetson, R; Keefe, AD; McCoull, W; McMurray, L; Olszewski, A; Overman, R; Pflug, A; Preston, M; Rawlins, PB; Rivers, E; Schimpl, M; Smith, P; Truman, C; Underwood, E; Warwicker, J; Winter-Holt, J; Woodcock, S; Zhang, Y Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy. J Med Chem64:3165-3184 (2021) [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

BDBM50563641

n/a

Name

BDBM50563641

Synonyms:

CHEMBL4744243

Type

Small organic molecule

Emp. Form.

C20H18ClF3N6O2S

Mol. Mass.

498.909

SMILES

CNC(=O)c1sc(nc1C(F)(F)F)N1CC2CC1(CNC(=O)c1c[nH]c3ncc(Cl)cc13)C2 |(43.22,-48.73,;41.68,-48.73,;40.91,-50.06,;41.68,-51.39,;39.37,-50.05,;38.47,-48.8,;37,-49.27,;37,-50.81,;38.46,-51.29,;38.92,-52.75,;40.46,-52.75,;39.69,-54.09,;37.9,-53.9,;35.75,-48.36,;35.76,-46.82,;34.3,-46.34,;33.39,-47.59,;34.29,-48.83,;33.81,-50.3,;32.3,-50.61,;31.28,-49.46,;31.76,-48,;29.77,-49.78,;29.14,-51.17,;27.61,-51.01,;27.3,-49.51,;25.96,-48.75,;25.96,-47.2,;27.29,-46.43,;27.29,-44.89,;28.63,-47.19,;28.63,-48.74,;34.69,-47.82,)|

Structure