Ki Summary

Reaction Details

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Target

Tyrosine-protein kinase ABL1 [201-500,M351T]

Ligand

BDBM13534

Substrate/Competitor

BDBM13531

Meas. Tech.

Kinase Assay and Binding Constant Measurement

8±n/a nM

Citation

Carter, TA; Wodicka, LM; Shah, NP; Velasco, AM; Fabian, MA; Treiber, DK; Milanov, ZV; Atteridge, CE; Biggs, WH; Edeen, PT; Floyd, M; Ford, JM; Grotzfeld, RM; Herrgard, S; Insko, DE; Mehta, SA; Patel, HK; Pao, W; Sawyers, CL; Varmus, H; Zarrinkar, PP; Lockhart, DJ Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A102:11011-6 (2005) [PubMed] Article

More Info.:

Get all data from this article, Solution Info, Assay Method

Tyrosine-protein kinase ABL1 [201-500,M351T]

Name:

Tyrosine-protein kinase ABL1 [201-500,M351T]

Synonyms:

ABL | ABL Mutant (M351T) | ABL1 | ABL1_HUMAN | JTK7 | Proto-oncogene tyrosine-protein kinase ABL1 mutant M351T | c-ABL | p150

Type:

Enzyme

Mol. Mass.:

34565.67

Organism:

Homo sapiens (Human)

Description:

P00519[201-500,M351T]

Residue:

300

Sequence:

HHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQYGEVYEGV
WKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTY
GNLLDYLRECNRQEVNAVVLLYMATQISSATEYLEKKNFIHRDLAARNCLVGENHLVKVA
DFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKSDVWAFGVLLWEIATYGMSPY
PGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNPSDRPSFAEIHQAFETMFQES

BDBM13534

BDBM13531

Name

BDBM13534

Synonyms:

CHEMBL572878 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide | N-[4-[[4-(4-methylpiperazino)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]thio]phenyl]cyclopropanecarboxamide | VX-680 | VX680 | cyclopropane carboxylic acid {4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2ylsulphanyl]-phenyl}-amide

Type

Small organic molecule

Emp. Form.

C23H28N8OS

Mol. Mass.

464.586

SMILES

CN1CCN(CC1)c1cc(Nc2cc(C)n[nH]2)nc(Sc2ccc(NC(=O)C3CC3)cc2)n1

Structure