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SGC-AAK1-1 | SGC-AAK1-1 : Inhibitor of AAK1 and BMP2K
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 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
AAK1
  • Ki:9.1 nM
  • IC50:770 nM
BMP2K
  • Ki:17 nM
  • IC50:2800 nM
Inhibitor
up to 5 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Tested in KINOMEscan (DiscoverX) against 403 wildtype human protein kinases at 1 μM, it proved to be ...

Potency
Cellular
In Vitro

AAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.9b00399

BMP2K

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.9b00399

Negative Control Compounds

CANSAR3153834
Notes: SGC-AAK1-1N (cpd 16) IC50 18000 nM

Chemical Information

Molecular Formula C21H25N5O3S
SMILEs CCN(CC)S(=O)(=O)Nc1cccc(-c2ccc3c(NC(=O)C4CC4)n[nH]c3c2)c1
InChI InChI=1S/C21H25N5O3S/c1-3-26(4-2)30(28,29)25-17-7-5-6-15(12-17)16-10-11-18-19(13-16)23-24-20(18)22-21(27)14-8-9-14/h5-7,10-14,25H,3-4,8-9H2,1-2H3,(H2,22,23,24,27)
Molecular weight 427.17 Da
AlogP 3.576900000000001
HBond acceptors 8
HBond donors 3
Atoms 55

Vendors

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Expert Reviews

by SERP
(on 8 Feb 2023 )
Cellular Use Rating
SGC-AAK1-1 is a clean in vitro tool compound with decent biochemical potency, weak but selective cellular active. The upside of this compound is its kinome selectivity. The downside is its relatively modest...
by SERP+
(on 23 May 2024 )
Cellular Use Rating
Cell potency for AAK1 is less than 1 μM, but for BMP2K is 2.8 μM thus, it could be improved. Additional assays could be performed to gain more information regarding effect on endogenous protein. No cytotoxicity...
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