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GSK2982772 | GSK2982772 : Inhibitor of RIPK1
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

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Targets Biochemical/Biophysical Potency Cellular Potency
RIPK1
  • IC50:16 nM
  • IC50:1 nM
  • IC50:2 nM
  • IC50:0.5 nM
up to 300 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases React ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
GSK2982772 demonstrated a clean profile against a range of nonkinase targets. No inhibitory poten ...

Potency
Cellular
In Vitro

RIPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b01751

In Vivo Validations

Rat, Monkey
Dose: 1.1 (R) - 1.2 (M) mg/Kg, 2.1 (R) - 1.9 (M) mg/Kg, Reviewer suggested 5-50 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 3.9 ± 0.7 (R), 6.5 ± 1.0 (M) h (IV)
Systemic clearance: 17 ± 5 (R), 10 ± 3(M) ml/min/Kg (IV)

DOI Reference: 10.1021/acs.jmedchem.6b01751

Orthogonal Probes def

R1-ICR-5

Chemical Information

Molecular Formula C20H19N5O3
SMILEs CN1C(=O)[C@@H](NC(=O)c2n[nH]c(Cc3ccccc3)n2)COc2ccccc21
InChI InChI=1S/C20H19N5O3/c1-25-15-9-5-6-10-16(15)28-12-14(20(25)27)21-19(26)18-22-17(23-24-18)11-13-7-3-2-4-8-13/h2-10,14H,11-12H2,1H3,(H,21,26)(H,22,23,24)/t14-/m0/s1
Molecular weight 377.15 Da
AlogP 1.5492999999999992
HBond acceptors 8
HBond donors 2
Atoms 47

Vendors

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Expert Reviews

by SERP
(on 2 Dec 2020)
Cellular Use Rating
In Model Organisms
The probe should be used in cellular system in combination with its enantiomer as negative control. Importantly, this probe shows significant species-differences as outlined by the authors in the J....
by SERP
(on 14 Dec 2020)
Cellular Use Rating
In Model Organisms
The enantiomer is very useful as a negative control probe. For orthogonal probe, e.g. in Cortellis Drug Discovery Intelligence there are 286 small molecules with Mw <750 g/mol that are used in either...
by SERP
(on 18 Dec 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
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