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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