AZD3988

Inhibitor of DGAT1

Structure

Information

Protein target names: DGAT1

Mechanism of action: Inhibitor

Recommended in-cell concentration:
up to 100 nM

In Vitro Validations

Uniprot ID: O75907
Target Class: Other
Target SubClass: Diacylglycerol O-acyltransferase
Potency: IC50
Potency Value: 0.6 nM
Potency Assay: Enzymatic activity for human homolog
PDB ID for probe-target interaction (3D structure): --
Structure-activity relationship: yes
Target aliases:
Diacylglycerol O-acyltransferase 1, DGAT, AGRP1, D ...

DOI Reference: 10.1016/j.bmcl.2012.04.117

Uniprot ID: O75907
Target Class: Other
Target SubClass: Diacylglycerol O-acyltransferase
Potency: IC50
Potency Value: 0.5 nM
Potency Assay: Enzymatic activity for rat homolog
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Diacylglycerol O-acyltransferase 1, DGAT, AGRP1, D ...

DOI Reference: 10.1016/j.bmcl.2012.04.117

Uniprot ID: O75907
Target Class: Other
Target SubClass: Diacylglycerol O-acyltransferase
Potency: IC50
Potency Value: 1.1 nM
Potency Assay: Enzymatic activity for mouse homolog
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Diacylglycerol O-acyltransferase 1, DGAT, AGRP1, D ...

DOI Reference: 10.1016/j.bmcl.2012.04.117

In Cell Validations

In Vivo Data

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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 18 Dec 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

Overall, AZD3988 has very favourable probe properties to study DGAT-1. The probe shows a clear mechanism of action and engages with the target at low nanomolar concentrations, exhibits selectivity for DGAT-1 over DGAT-2 in vitro in cellulo, and in vivo, and there are no common off-target liabilities observed (hERG, P450s). Additionally, the physicochemical properties are fairly drug-like for a probe molecule: 3 H-bond donors, 8 H-bond acceptors, molecular weight of 456.45 Da, logD = 3.0, 7 rotatable bonds, and a calculated tPSA of 112.38 Å2.

(last updated: 7 Jan 2021 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 18 Feb 2021 )