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MRL-SYKi | MRL-SYKi : Inhibitor of SYK
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 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
SYK
  • IC50:0.9 nM
  • IC50:38 nM
  • IC50:287 nM
Inhibitor
100 nM

Selectivity

In Vitro Selectivity Assessment
ZAP70

Gene ID: P43403

Organism: Homo sapiens

Family: Tyr protein kinase family

Selectivity Assessment Description:
Selectivity within target family - Based on an internal assessment we found the closely related kina ...

Potency
Cellular
In Vitro

SYK

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.6019/CHEMBL4507285

In Vivo Validations

Rat
Dose: 1-30 mg/Kg
Route of delivery: Oral
Plasma half life: 2.2 h
Systemic clearance: 7-8 mL/min/kg
Fb : 94.7%
Bioavailability: 20%

DOI Reference: 10.6019/CHEMBL4507285

Dog
Dose: 1-30 mg/Kg
Route of delivery: Oral
Plasma half life: 3.6 h
Systemic clearance: 7-8 mL/min/kg
Fb : 90.9%
Bioavailability: 54%

DOI Reference: 10.6019/CHEMBL4507285

Negative Control Compounds

MRL-SYKi-NC
Notes: The negative control is 1000-fold less potent biochemically and shows no activity in cells @ 10µM; Note: Shows off-target activity in the GPCR scan: the closest hit is GABA/PBR (Ki = 774 nM)

Orthogonal Probes def

PRT-2607
ENTOSPLETINIB

Chemical Information

Molecular Formula C24H28N4O3S
SMILEs Cc1cc(Nc2nccc(C)n2)cc(-c2cnc([C@@]3(O)CC[C@H](C(=O)O)C(C)(C)C3)s2)c1
InChI InChI=1S/C24H28N4O3S/c1-14-9-16(11-17(10-14)28-22-25-8-6-15(2)27-22)19-12-26-21(32-19)24(31)7-5-18(20(29)30)23(3,4)13-24/h6,8-12,18,31H,5,7,13H2,1-4H3,(H,29,30)(H,25,27,28)/t18-,24-/m1/s1
Molecular weight 452.19 Da
AlogP 0.0
HBond acceptors 7
HBond donors 3
Atoms 60

Vendors

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Expert Reviews

by SERP
(on 3 Mar 2022 )
Cellular Use Rating
In Model Organisms
The additional activity of the molecule on ZAP70 (24 nM in vitro) needs to be considered when using the probe to interrogate SYK. The activity of the negative control on ZAP70 is not given.
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