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Target
Neprilysin
Ligand
BDBM50034842
Substrate
n/a
Meas. Tech.
ChEMBL_1839011 (CHEMBL4339144)
IC50
6.0±n/a nM
Citation
Kawanami, T; Karki, RG; Cody, E; Liu, Q; Liang, G; Ksander, GM; Rigel, DF; Schiering, N; Gong, Y; Coppola, GM; Iwaki, Y; Sun, R; Neubert, A; Fan, L; Ingles, S; D'Arcy, A; Villard, F; Ramage, P; Jeng, AY; Leung-Chu, J; Liu, J; Beil, M; Fu, F; Chen, W; Cumin, F; Wiesmann, C; Mogi, M Structure-Guided Design of Substituted Biphenyl Butanoic Acid Derivatives as Neprilysin Inhibitors. ACS Med Chem Lett 11:188-194 (2020) [PubMed] Article
More Info.:
Target
Name:
Neprilysin
Synonyms:
Atriopeptidase | CALLA | CD_antigen=CD10 | Common acute lymphocytic leukemia antigen | EPN | Enkephalinase | MME | NEP | NEP_HUMAN | Neutral Endopeptidase (NEP) | Neutral endopeptidase | Neutral endopeptidase 24.11
Type:
Enzyme
Mol. Mass.:
85505.38
Organism:
Homo sapiens (Human)
Description:
P08473
Residue:
750
Sequence:
MGKSESQMDITDINTPKPKKKQRWTPLEISLSVLVLLLTIIAVTMIALYATYDDGICKSSDCIKSAARLIQNMDATTEPCTDFFKYACGGWLKRNVIPETSSRYGNFDILRDELEVVLKDVLQEPKTEDIVAVQKAKALYRSCINESAIDSRGGEPLLKLLPDIYGWPVATENWEQKYGASWTAEKAIAQLNSKYGKKVLINLFVGTDDKNSVNHVIHIDQPRLGLPSRDYYECTGIYKEACTAYVDFMISVARLIRQEERLPIDENQLALEMNKVMELEKEIANATAKPEDRNDPMLLYNKMTLAQIQNNFSLEINGKPFSWLNFTNEIMSTVNISITNEEDVVVYAPEYLTKLKPILTKYSARDLQNLMSWRFIMDLVSSLSRTYKESRNAFRKALYGTTSETATWRRCANYVNGNMENAVGRLYVEAAFAGESKHVVEDLIAQIREVFIQTLDDLTWMDAETKKRAEEKALAIKERIGYPDDIVSNDNKLNNEYLELNYKEDEYFENIIQNLKFSQSKQLKKLREKVDKDEWISGAAVVNAFYSSGRNQIVFPAGILQPPFFSAQQSNSLNYGGIGMVIGHEITHGFDDNGRNFNKDGDLVDWWTQQSASNFKEQSQCMVYQYGNFSWDLAGGQHLNGINTLGENIADNGGLGQAYRAYQNYIKKNGEEKLLPGLDLNHKQLFFLNFAQVWCGTYRPEYAVNSIKTDVHSPGNFRIIGTLQNSAEFSEAFHCRKNSYMNPEKKCRVW
Inhibitor
Name:
BDBM50034842
Synonyms:
(2R,4S)-5-Biphenyl-4-yl-4-(3-carboxy-propionylamino)-2-methyl-pentanoic acid | CHEMBL417007 | US10123984, Compound 21a(R,S) | US11547687, Comparative Compound B | US20230285340, Comparative Compound B
Type:
Small organic molecule
Emp. Form.:
C22H25NO5
Mol. Mass.:
383.4376
SMILES:
C[C@H](C[C@@H](Cc1ccc(cc1)-c1ccccc1)NC(=O)CCC(O)=O)C(O)=O