Ki Summary

Reaction Details

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Target

Receptor-type tyrosine-protein kinase FLT3

Ligand

BDBM50563644

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

BDBM50563644

n/a

Name

BDBM50563644

Synonyms:

CHEMBL4782810

Type

Small organic molecule

Emp. Form.

C21H21F3N6O2S

Mol. Mass.

478.491

SMILES

CNC(=O)c1sc(nc1C(F)(F)F)N1CC2CC1(CNC(=O)c1c[nH]c3ncc(C)cc13)C2 |(45.05,-5.8,;43.51,-5.8,;42.74,-7.13,;43.5,-8.46,;41.2,-7.12,;40.3,-5.87,;38.82,-6.34,;38.82,-7.88,;40.29,-8.36,;40.75,-9.82,;42.29,-9.82,;41.52,-11.16,;39.72,-10.97,;37.58,-5.43,;37.59,-3.89,;36.13,-3.41,;35.22,-4.66,;36.12,-5.9,;35.64,-7.37,;34.13,-7.68,;33.1,-6.53,;33.58,-5.07,;31.6,-6.85,;30.97,-8.24,;29.44,-8.08,;29.13,-6.58,;27.79,-5.81,;27.79,-4.27,;29.12,-3.5,;29.11,-1.96,;30.45,-4.26,;30.46,-5.81,;36.52,-4.89,)|

Structure