Target
Tyrosine-protein kinase ABL1 [201-500,Y253F]
Ligand
BDBM4814
Substrate
BDBM13531
Meas. Tech.
Kinase Assay and Binding Constant Measurement
Kd
700±n/a nM
Citation
 Carter, TAWodicka, LMShah, NPVelasco, AMFabian, MATreiber, DKMilanov, ZVAtteridge, CEBiggs, WHEdeen, PTFloyd, MFord, JMGrotzfeld, RMHerrgard, SInsko, DEMehta, SAPatel, HKPao, WSawyers, CLVarmus, HZarrinkar, PPLockhart, DJ Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases. Proc Natl Acad Sci U S A 102:11011-6 (2005) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase ABL1 [201-500,Y253F]
Synonyms:
ABL | ABL Mutant (Y253F) | ABL1 | ABL1_HUMAN | JTK7 | Proto-oncogene tyrosine-protein kinase ABL1 mutant Y253F | c-ABL | p150
Type:
Enzyme
Mol. Mass.:
34579.76
Organism:
Homo sapiens (Human)
Description:
P00519[201-500,Y253F]
Residue:
300
Sequence:
HHSTVADGLITTLHYPAPKRNKPTVYGVSPNYDKWEMERTDITMKHKLGGGQFGEVYEGVWKKYSLTVAVKTLKEDTMEVEEFLKEAAVMKEIKHPNLVQLLGVCTREPPFYIITEFMTYGNLLDYLRECNRQEVNAVVLLYMATQISSAMEYLEKKNFIHRDLAARNCLVGENHLVKVADFGLSRLMTGDTYTAHAGAKFPIKWTAPESLAYNKFSIKSDVWAFGVLLWEIATYGMSPYPGIDLSQVYELLEKDYRMERPEGCPEKVYELMRACWQWNPSDRPSFAEIHQAFETMFQES
  
Inhibitor
Name:
BDBM4814
Synonyms:
CHEMBL535 | N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1,2-dihydro-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide | N-[2-(diethylamino)ethyl]-5-{[(3Z)-5-fluoro-2-oxo-2,3-dihydro-1H-indol-3-ylidene]methyl}-2,4-dimethyl-1H-pyrrole-3-carboxamide | SU11248 | SUNITINIB | SUNITINIB MALATE | US10464902, Sunitinib | US9163010, Sunitinib | US9914707, SU11248
Type:
Small organic molecule
Emp. Form.:
C22H27FN4O2
Mol. Mass.:
398.4738
SMILES:
CCN(CC)CCNC(=O)c1c(C)[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c1C
Structure:
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Substrate
Name:
BDBM13531
Synonyms:
4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole | 4-[4-(4-Fluorophenyl)-5-(4-pyridinyl)-1H-imidazol-2-yl]phenol | 4-[4-(4-fluorophenyl)-5-(4-pyridyl)-4-imidazolin-2-ylidene]cyclohexa-2,5-dien-1-one | 4-[5-(4-fluorophenyl)-4-(pyridin-4-yl)-1H-imidazol-2-yl]phenol | SB-202190 | SB202190 | biotinylated SB202190
Type:
Small organic molecule
Emp. Form.:
C20H14FN3O
Mol. Mass.:
331.3431
SMILES:
Oc1ccc(cc1)-c1nc(c([nH]1)-c1ccc(F)cc1)-c1ccncc1
Structure:
Search PDB for entries with ligand similarity: