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AZD3988 | Inhibitor of DGAT1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DGAT1
  • IC50:0.6 nM
  • IC50:0.5 nM
  • IC50:1.1 nM
  • IC50:0.5 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - ACAT1 86 nM, ACAT2 600 nM

Potency Assay Off-Target:
Enzymatic Activity
Selectivity Assessment Description:
no significant activity against DGAT-2, the hERG encoded potassium channel (>30 μM), and cytoc ...

Potency
Cellular
In Vitro

DGAT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2012.04.117

In Vivo Validations

Mouse, Rat, Dog
Dose: 0.5 (M), 2 (R), 1 (D) mg/kg IV, 1 (M), 5 (R), 1 (D) mg/kg PO, Reviewer suggest: 20 mg/Kg (M), 0.5-5 mg/Kg (R)
Route of delivery: Intravenous, Oral
Plasma half life: 4.9 (M), 3.4 (R), 1.8 (D) h (IV), 4.7 (M), 5.8 (R), 5.7 (D) h (PO)
Systemic clearance: 4.6 (M), 1.1 (R), 2.5 (D) mL/min/kg

DOI Reference: 10.1016/j.bmcl.2012.04.117

Orthogonal Probes def

GSK2973980A

Chemical Information

Molecular Formula C23H22F2N4O4
SMILEs O=C(O)C[C@H]1CC[C@H](c2ccc(NC(=O)c3nnc(Nc4ccc(F)c(F)c4)o3)cc2)CC1
InChI InChI=1S/C23H22F2N4O4/c24-18-10-9-17(12-19(18)25)27-23-29-28-22(33-23)21(32)26-16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-20(30)31/h5-10,12-14H,1-4,11H2,(H,26,32)(H,27,29)(H,30,31)/t13-,14-
Molecular weight 456.16 Da
AlogP 0.0
HBond acceptors 8
HBond donors 3
Atoms 55

Vendors

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Expert Reviews

by SERP
(on 18 Dec 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
by SERP
(on 7 Jan 2021)
Cellular Use Rating
In Model Organisms
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...
by SERP
(on 18 Feb 2021)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria