Target
Receptor-interacting serine/threonine-protein kinase 1
Ligand
BDBM50233240
Substrate
n/a
Meas. Tech.
ChEMBL_1650162 (CHEMBL3999296)
IC50
0.630000±n/a nM
Citation
 Harris, PABerger, SBJeong, JUNagilla, RBandyopadhyay, DCampobasso, NCapriotti, CACox, JADare, LDong, XEidam, PMFinger, JNHoffman, SJKang, JKasparcova, VKing, BWLehr, RLan, YLeister, LKLich, JDMacDonald, TTMiller, NAOuellette, MTPao, CSRahman, AReilly, MARendina, ARRivera, EJSchaeffer, MCSehon, CASinghaus, RRSun, HHSwift, BATotoritis, RDVossenkämper, AWard, PWisnoski, DDZhang, DMarquis, RWGough, PJBertin, J Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem 60:1247-1261 (2017) [PubMed]  Article 
Target
Name:
Receptor-interacting serine/threonine-protein kinase 1
Synonyms:
Cell death protein RIP | RIP | RIP-1 | RIP1 | RIPK1 | RIPK1_HUMAN | Receptor-interacting protein 1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
75926.99
Organism:
Homo sapiens (Human)
Description:
Q13546
Residue:
671
Sequence:
MQPDMSLNVIKMKSSDFLESAELDSGGFGKVSLCFHRTQGLMIMKTVYKGPNCIEHNEALLEEAKMMNRLRHSRVVKLLGVIIEEGKYSLVMEYMEKGNLMHVLKAEMSTPLSVKGRIILEIIEGMCYLHGKGVIHKDLKPENILVDNDFHIKIADLGLASFKMWSKLNNEEHNELREVDGTAKKNGGTLYYMAPEHLNDVNAKPTEKSDVYSFAVVLWAIFANKEPYENAICEQQLIMCIKSGNRPDVDDITEYCPREIISLMKLCWEANPEARPTFPGIEEKFRPFYLSQLEESVEEDVKSLKKEYSNENAVVKRMQSLQLDCVAVPSSRSNSATEQPGSLHSSQGLGMGPVEESWFAPSLEHPQEENEPSLQSKLQDEANYHLYGSRMDRQTKQQPRQNVAYNREEERRRRVSHDPFAQQRPYENFQNTEGKGTAYSSAASHGNAVHQPSGLTSQPQVLYQNNGLYSSHGFGTRPLDPGTAGPRVWYRPIPSHMPSLHNIPVPETNYLGNTPTMPFSSLPPTDESIKYTIYNSTGIQIGAYNYMEIGGTSSSLLDSTNTNFKEEPAAKYQAIFDNTTSLTDKHLDPIRENLGKHWKNCARKLGFTQSQIDEIDHDYERDGLKEKVYQMLQKWVMREGIKGATVGKLAQALHQCSRIDLLSSLIYVSQN
  
Inhibitor
Name:
BDBM50233240
Synonyms:
CHEMBL4065561
Type:
Small organic molecule
Emp. Form.:
C20H19N5O3
Mol. Mass.:
377.3966
SMILES:
CN1c2ccccc2OC[C@H](NC(=O)c2ncn(Cc3ccccc3)n2)C1=O |r|
Structure:
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