Target
Tyrosine-protein kinase Tec
Ligand
BDBM291522
Substrate
n/a
Meas. Tech.
ChEMBL_1673717 (CHEMBL4023746)
IC50
38±n/a nM
Citation
 Crawford, JJJohnson, ARMisner, DLBelmont, LDCastanedo, GChoy, RCoraggio, MDong, LEigenbrot, CErickson, RGhilardi, NHau, JKatewa, AKohli, PBLee, WLubach, JWMcKenzie, BSOrtwine, DFSchutt, LTay, SWei, BReif, KLiu, LWong, HYoung, WB Discovery of GDC-0853: A Potent, Selective, and Noncovalent Bruton's Tyrosine Kinase Inhibitor in Early Clinical Development. J Med Chem 61:2227-2245 (2018) [PubMed]  Article 
Target
Name:
Tyrosine-protein kinase Tec
Synonyms:
PSCTK4 | TEC | TEC_HUMAN | Tyrosine-protein kinase TEC (TEC)
Type:
Protein
Mol. Mass.:
73597.00
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
631
Sequence:
MNFNTILEEILIKRSQQKKKTSPLNYKERLFVLTKSMLTYYEGRAEKKYRKGFIDVSKIKCVEIVKNDDGVIPCQNKYPFQVVHDANTLYIFAPSPQSRDLWVKKLKEEIKNNNNIMIKYHPKFWTDGSYQCCRQTEKLAPGCEKYNLFESSIRKALPPAPETKKRRPPPPIPLEEEDNSEEIVVAMYDFQAAEGHDLRLERGQEYLILEKNDVHWWRARDKYGNEGYIPSNYVTGKKSNNLDQYEWYCRNMNRSKAEQLLRSEDKEGGFMVRDSSQPGLYTVSLYTKFGGEGSSGFRHYHIKETTTSPKKYYLAEKHAFGSIPEIIEYHKHNAAGLVTRLRYPVSVKGKNAPTTAGFSYEKWEINPSELTFMRELGSGLFGVVRLGKWRAQYKVAIKAIREGAMCEEDFIEEAKVMMKLTHPKLVQLYGVCTQQKPIYIVTEFMERGCLLNFLRQRQGHFSRDVLLSMCQDVCEGMEYLERNSFIHRDLAARNCLVSEAGVVKVSDFGMARYVLDDQYTSSSGAKFPVKWCPPEVFNYSRFSSKSDVWSFGVLMWEVFTEGRMPFEKYTNYEVVTMVTRGHRLYQPKLASNYVYEVMLRCWQEKPEGRPSFEDLLRTIDELVECEETFGR
  
Inhibitor
Name:
BDBM291522
Synonyms:
1-(4-(((6-amino-5-(4-phenoxyphenyl)pyrimidin-4-yl)amino)methyl)piperidin-1-yl)prop-2-en-1-one | US10413562, Compound A250 | US9580449, Example A250 | US9580449, Example A39
Type:
Small organic molecule
Emp. Form.:
C25H27N5O2
Mol. Mass.:
429.5142
SMILES:
Nc1ncnc(NCC2CCN(CC2)C(=O)C=C)c1-c1ccc(Oc2ccccc2)cc1
Structure:
Search PDB for entries with ligand similarity: