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Target
Serine/threonine-protein kinase ULK1
Ligand
BDBM379413
Substrate
n/a
Meas. Tech.
ChEMBL_2023820 (CHEMBL4677633)
IC50
30±n/a nM
Citation
Ren, H; Bakas, NA; Vamos, M; Chaikuad, A; Limpert, AS; Wimer, CD; Brun, SN; Lambert, LJ; Tautz, L; Celeridad, M; Sheffler, DJ; Knapp, S; Shaw, RJ; Cosford, 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
More Info.:
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:
Human
Description:
ChEMBL_1510275
Residue:
1050
Sequence:
MEPGRGGTETVGKFEFSRKDLIGHGAFAVVFKGRHREKHDLEVAVKCINKKNLAKSQTLLGKEIKILKELKHENIVALYDFQEMANSVYLVMEYCNGGDLADYLHAMRTLSEDTIRLFLQQIAGAMRLLHSKGIIHRDLKPQNILLSNPAGRRANPNSIRVKIADFGFARYLQSNMMAATLCGSPMYMAPEVIMSQHYDGKADLWSIGTIVYQCLTGKAPFQASSPQDLRLFYEKNKTLVPTIPRETSAPLRQLLLALLQRNHKDRMDFDEFFHHPFLDASPSVRKSPPVPVPSYPSSGSGSSSSSSSTSHLASPPSLGEMQQLQKTLASPADTAGFLHSSRDSGGSKDSSCDTDDFVMVPAQFPGDLVAEAPSAKPPPDSLMCSGSSLVASAGLESHGRTPSPSPPCSSSPSPSGRAGPFSSSRCGASVPIPVPTQVQNYQRIERNLQSPTQFQTPRSSAIRRSGSTSPLGFARASPSPPAHAEHGGVLARKMSLGGGRPYTPSPQVGTIPERPGWSGTPSPQGAEMRGGRSPRPGSSAPEHSPRTSGLGCRLHSAPNLSDLHVVRPKLPKPPTDPLGAVFSPPQASPPQPSHGLQSCRNLRGSPKLPDFLQRNPLPPILGSPTKAVPSFDFPKTPSSQNLLALLARQGVVMTPPRNRTLPDLSEVGPFHGQPLGPGLRPGEDPKGPFGRSFSTSRLTDLLLKAAFGTQAPDPGSTESLQEKPMEIAPSAGFGGSLHPGARAGGTSSPSPVVFTVGSPPSGSTPPQGPRTRMFSAGPTGSASSSARHLVPGPCSEAPAPELPAPGHGCSFADPITANLEGAVTFEAPDLPEETLMEQEHTEILRGLRFTLLFVQHVLEIAALKGSASEAAGGPEYQLQESVVADQISLLSREWGFAEQLVLYLKVAELLSSGLQSAIDQIRAGKLCLSSTVKQVVRRLNELYKASVVSCQGLSLRLQRFFLDKQRLLDRIHSITAERLIFSHAVQMVQSAALDEMFQHREGCVPRYHKALLLLEGLQHMLSDQADIENVTKCKLCIERRLSALLTGICA
Inhibitor
Name:
BDBM379413
Synonyms:
N-(cyclopropanecarbonyl)-N-(4-((4-(cyclopropylamino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)phenyl)cyclopropanecarboxamide | US10266549, Example 311 | US10774092, Example 311
Type:
Small organic molecule
Emp. Form.:
C22H22F3N5O2
Mol. Mass.:
445.4376
SMILES:
FC(F)(F)c1cnc(Nc2ccc(cc2)N(C(=O)C2CC2)C(=O)C2CC2)nc1NC1CC1