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Target
Serine/threonine-protein kinase ULK1
Ligand
BDBM379445
Substrate
n/a
Meas. Tech.
ChEMBL_2023820 (CHEMBL4677633)
IC50
31±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:
Homo sapiens (Human)
Description:
ChEMBL_1510275
Residue:
1050
Sequence:
MEPGRGGTETVGKFEFSRKDLIGHGAFAVVFKGRHREKHDLEVAVKCINKKNLAKSQTLLGKEIKILKELKHENIVALYDFQEMANSVYLVMEYCNGGDLADYLHAMRTLSEDTIRLFLQQIAGAMRLLHSKGIIHRDLKPQNILLSNPAGRRANPNSIRVKIADFGFARYLQSNMMAATLCGSPMYMAPEVIMSQHYDGKADLWSIGTIVYQCLTGKAPFQASSPQDLRLFYEKNKTLVPTIPRETSAPLRQLLLALLQRNHKDRMDFDEFFHHPFLDASPSVRKSPPVPVPSYPSSGSGSSSSSSSTSHLASPPSLGEMQQLQKTLASPADTAGFLHSSRDSGGSKDSSCDTDDFVMVPAQFPGDLVAEAPSAKPPPDSLMCSGSSLVASAGLESHGRTPSPSPPCSSSPSPSGRAGPFSSSRCGASVPIPVPTQVQNYQRIERNLQSPTQFQTPRSSAIRRSGSTSPLGFARASPSPPAHAEHGGVLARKMSLGGGRPYTPSPQVGTIPERPGWSGTPSPQGAEMRGGRSPRPGSSAPEHSPRTSGLGCRLHSAPNLSDLHVVRPKLPKPPTDPLGAVFSPPQASPPQPSHGLQSCRNLRGSPKLPDFLQRNPLPPILGSPTKAVPSFDFPKTPSSQNLLALLARQGVVMTPPRNRTLPDLSEVGPFHGQPLGPGLRPGEDPKGPFGRSFSTSRLTDLLLKAAFGTQAPDPGSTESLQEKPMEIAPSAGFGGSLHPGARAGGTSSPSPVVFTVGSPPSGSTPPQGPRTRMFSAGPTGSASSSARHLVPGPCSEAPAPELPAPGHGCSFADPITANLEGAVTFEAPDLPEETLMEQEHTEILRGLRFTLLFVQHVLEIAALKGSASEAAGGPEYQLQESVVADQISLLSREWGFAEQLVLYLKVAELLSSGLQSAIDQIRAGKLCLSSTVKQVVRRLNELYKASVVSCQGLSLRLQRFFLDKQRLLDRIHSITAERLIFSHAVQMVQSAALDEMFQHREGCVPRYHKALLLLEGLQHMLSDQADIENVTKCKLCIERRLSALLTGICA
Inhibitor
Name:
BDBM379445
Synonyms:
N4-cyclopropyl-N2-(4-ethyl-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-7-yl)-5-(trifluoromethyl)pyrimidine-2,4-diamine | US10266549, Example 344 | US10774092, Example 344
Type:
Small organic molecule
Emp. Form.:
C17H19F3N6O
Mol. Mass.:
380.3676
SMILES:
CCN1CCOc2cc(Nc3ncc(c(NC4CC4)n3)C(F)(F)F)cnc12