Target
Serine/threonine-protein kinase ULK1
Ligand
BDBM379414
Substrate
n/a
Meas. Tech.
ChEMBL_2023820 (CHEMBL4677633)
IC50
13±n/a nM
Citation
 Ren, HBakas, NAVamos, MChaikuad, ALimpert, ASWimer, CDBrun, SNLambert, LJTautz, LCeleridad, MSheffler, DJKnapp, SShaw, RJCosford, NDP Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. J Med Chem 63:14609-14625 (2020) [PubMed]  Article 
Target
Name:
Serine/threonine-protein kinase ULK1
Synonyms:
ATG1 | Autophagy-related protein 1 homolog | KIAA0722 | ULK1 | ULK1_HUMAN | Unc-51-like kinase 1 | hATG1
Type:
PROTEIN
Mol. Mass.:
112661.80
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1510275
Residue:
1050
Sequence:
MEPGRGGTETVGKFEFSRKDLIGHGAFAVVFKGRHREKHDLEVAVKCINKKNLAKSQTLLGKEIKILKELKHENIVALYDFQEMANSVYLVMEYCNGGDLADYLHAMRTLSEDTIRLFLQQIAGAMRLLHSKGIIHRDLKPQNILLSNPAGRRANPNSIRVKIADFGFARYLQSNMMAATLCGSPMYMAPEVIMSQHYDGKADLWSIGTIVYQCLTGKAPFQASSPQDLRLFYEKNKTLVPTIPRETSAPLRQLLLALLQRNHKDRMDFDEFFHHPFLDASPSVRKSPPVPVPSYPSSGSGSSSSSSSTSHLASPPSLGEMQQLQKTLASPADTAGFLHSSRDSGGSKDSSCDTDDFVMVPAQFPGDLVAEAPSAKPPPDSLMCSGSSLVASAGLESHGRTPSPSPPCSSSPSPSGRAGPFSSSRCGASVPIPVPTQVQNYQRIERNLQSPTQFQTPRSSAIRRSGSTSPLGFARASPSPPAHAEHGGVLARKMSLGGGRPYTPSPQVGTIPERPGWSGTPSPQGAEMRGGRSPRPGSSAPEHSPRTSGLGCRLHSAPNLSDLHVVRPKLPKPPTDPLGAVFSPPQASPPQPSHGLQSCRNLRGSPKLPDFLQRNPLPPILGSPTKAVPSFDFPKTPSSQNLLALLARQGVVMTPPRNRTLPDLSEVGPFHGQPLGPGLRPGEDPKGPFGRSFSTSRLTDLLLKAAFGTQAPDPGSTESLQEKPMEIAPSAGFGGSLHPGARAGGTSSPSPVVFTVGSPPSGSTPPQGPRTRMFSAGPTGSASSSARHLVPGPCSEAPAPELPAPGHGCSFADPITANLEGAVTFEAPDLPEETLMEQEHTEILRGLRFTLLFVQHVLEIAALKGSASEAAGGPEYQLQESVVADQISLLSREWGFAEQLVLYLKVAELLSSGLQSAIDQIRAGKLCLSSTVKQVVRRLNELYKASVVSCQGLSLRLQRFFLDKQRLLDRIHSITAERLIFSHAVQMVQSAALDEMFQHREGCVPRYHKALLLLEGLQHMLSDQADIENVTKCKLCIERRLSALLTGICA
  
Inhibitor
Name:
BDBM379414
Synonyms:
N-(4-((4-(cyclopropylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)phenyl)cyclopropanecarboxamide | US10266549, Example 312 | US10774092, Example 312
Type:
Small organic molecule
Emp. Form.:
C18H18F3N5O
Mol. Mass.:
377.3636
SMILES:
FC(F)(F)c1cnc(Nc2ccc(NC(=O)C3CC3)cc2)nc1NC1CC1
Structure:
Search PDB for entries with ligand similarity: