Co-Target(s) Information
Target General Information | Top | ||||
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Target ID | T05409 | Target Info | |||
Target Name | Neutral endopeptidase (MME) | ||||
Synonyms |
Skin fibroblast elastase; SFE; Neutral endopeptidase 24.11; Neprilysin; NEP protein; Enkephalinase; EPN; Common acute lymphocytic leukemia antigen; CD10; CALLA; Atriopeptidase
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Target Type | Clinical trial Target | ||||
Gene Name | MME | ||||
Biochemical Class | Peptidase | ||||
UniProt ID |
Co-Targets of This Target | Top | |||||
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Co-Target Name | Voltage-gated L-type calcium channel (L-CaC) | Successful Target | ||||
UniProt ID | CAC1C_HUMAN; CAC1D_HUMAN; CAC1F_HUMAN; CAC1S_HUMAN | |||||
Gene Name | NO-GeName | |||||
Synonyms |
L-type voltage-dependent Ca(2+) channel; L-type Ca2+ channel; L-type Ca(2+) channel
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Representative Drug(s) | Gallopamil | Drug Info | Ki = 5.4 nM | [1] | ||
Co-Target Name | Angiotensin-converting enzyme (ACE) | Successful Target | ||||
UniProt ID | ACE_HUMAN | |||||
Gene Name | SLC33A1 | |||||
Synonyms |
Kininase II; Dipeptidyl carboxypeptidase I; DCP1; DCP; CD143 antigen; CD143; ACE
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Representative Drug(s) | Sampatrilat | Drug Info | Ki = 13.8 nM | [2] | ||
Co-Target Name | Voltage-gated calcium channel alpha Cav1.2 (CACNA1C) | Successful Target | ||||
UniProt ID | CAC1C_HUMAN | |||||
Gene Name | CACNA1C | |||||
Synonyms |
Voltage-gated calcium channel subunit alpha Cav1.2; Voltage-dependent L-type calcium channel subunit alpha-1C; Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle; CCHL1A1; CACNL1A1; CACN2; CACH2
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Representative Drug(s) | Gallopamil | Drug Info | IC50 = 17 nM | [3] | ||
Co-Target Name | Natriuretic peptides A (NPPA) | Co-Target | ||||
UniProt ID | ANF_HUMAN | |||||
Gene Name | NPPA | |||||
Synonyms |
Atrial natriuretic factor prohormone; proANF; Atrial natriuretic peptide prohormone; preproANP; proANP; Atriopeptigen; Cardiodilatin; CDD; preproCDD-ANF
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Representative Drug(s) | Sampatrilat | Drug Info | IC50 = 3.4 nM | [4] |
References | Top | ||||
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REF 1 | Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds. Eur J Med Chem. 2013 May;63:85-94. | ||||
REF 2 | Molecular Basis for Omapatrilat and Sampatrilat Binding to Neprilysin-Implications for Dual Inhibitor Design with Angiotensin-Converting Enzyme. J Med Chem. 2020 May 28;63(10):5488-5500. | ||||
REF 3 | Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment. J Appl Toxicol. 2012 Oct;32(10):858-66. | ||||
REF 4 | Synthesis and evaluation of heteroarylalanine diacids as potent and selective neutral endopeptidase inhibitors. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3404-6. |
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