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TP-008 | TP-008 : Inhibitor of ACVR1B, TGFBR1
RATINGS:
Cellular Use: (1 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
ACVR1B
  • IC50:25 nM
  • IC50:300 nM
  • IC50:526 nM
TGFBR1
  • IC50:1000 nM
  • IC50:120 nM
  • IC50:245 nM
Inhibitor
1-10 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Clean KINOMEscan; off targets > 20 µM in NanoBRET. Selectivity outside target family: Closest off-ta ...

Potency
Cellular
In Vitro

ACVR1B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acschembio.0c00076

TGFBR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acschembio.0c00076

Negative Control Compounds

Al11
Notes: in vitro: > 10 µM (NanoBRET assay); Inactive in reporter gene assays, WB and kinome wide screen One off-target in GPCR scan: HTR2B ( Ki = 1591.74 nM)

Orthogonal Probes def

GW788388

Chemical Information

Molecular Formula C20H15ClFN5O2
SMILEs Cc1cnc(-c2cc(Cl)ccc2F)cc1-n1c(=O)n(CC(N)=O)c2cnccc21
InChI InChI=1S/C20H15ClFN5O2/c1-11-8-25-15(13-6-12(21)2-3-14(13)22)7-17(11)27-16-4-5-24-9-18(16)26(20(27)29)10-19(23)28/h2-9H,10H2,1H3,(H2,23,28)
Molecular weight 411.09 Da
AlogP 2.83542
HBond acceptors 7
HBond donors 2
Atoms 44

Vendors

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Expert Reviews

by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
The compound is very well characterised but potency varies significantly, between the different assays. The IC50 values determined in the radioactive kinase assay are high for a chemical probe (345 nM...
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