Reaction Details
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Receptor-interacting serine/threonine-protein kinase 1
Ligand
BDBM36371
Substrate
n/a
Meas. Tech.
ChEMBL_1644184 (CHEMBL3993113)
IC50
760±n/a nM
Citation
Ren, Y; Su, Y; Sun, L; He, S; Meng, L; Liao, D; Liu, X; Ma, Y; Liu, C; Li, S; Ruan, H; Lei, X; Wang, X; Zhang, Z Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome. J Med Chem 60:972-986 (2017) [PubMed] Article More Info.:
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:
BDBM36371
Synonyms:
5-(1H-indol-3-ylmethyl)-3-methyl-2-thioxo-4-Imidazolidinone, Nec-1 | CID2828334 | US10501473, Comparative Example 1
Type:
Small organic molecule
Emp. Form.:
C13H13N3OS
Mol. Mass.:
259.327
SMILES:
CN1C(=S)NC(Cc2c[nH]c3ccccc23)C1=O
Structure:
