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BAY-474 | BAY-474 : Inhibitor of MET
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
MET
  • IC50:<1 nM
  • IC50:2.9 nM
Inhibitor
1-1000 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family: > 1000 fold vs all other kinases (Millipore panel (214 at 1 µM), I ...

Potency
Cellular
In Vitro

MET

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.7554/eLife.34311

In Vivo Validations

Mouse
Dose: 10 mg/Kg BID
Route of delivery: Oral
Plasma half life: 1.5 h
Systemic clearance: 0.90 (plasma), (blood) 0.60 L/(h•kg)
Cmax: 0.15 Kg/L
Area Under the Curve:: 1.46 kg•h/L
Bioavailability: 107%
Volume of Distribution at Steady-State: 1.2 L/Kg

DOI Reference: 10.7554/eLife.34311

Rat
Dose: 10 mg/Kg BID
Route of delivery: Oral
Plasma half life: 1.3 h
Systemic clearance: 1.5 (plasma), 1.0 (blood) L/(h•kg)
Cmax: 0.083 Kg/L
Area Under the Curve:: 0.30 kg•h/L
Bioavailability: 45%
Volume of Distribution at Steady-State: 1.7 L/Kg

DOI Reference: 10.7554/eLife.34311

Dog
Dose: 10 mg/Kg BID
Route of delivery: Oral
Plasma half life: 3.5 h
Systemic clearance: 0.13 (plasma), 0.093 (blood) L/(h•kg)
Cmax: 1.34 Kg/L
Area Under the Curve:: 5.6 kg•h/L
Bioavailability: 63%
Volume of Distribution at Steady-State: 0.53 L/Kg

DOI Reference: 10.7554/eLife.34311

Negative Control Compounds

BAY-827
Notes: BAY-827 with 4 orders of magnitude less in vitro potency (IC50 = 11 µM) Shows activity on HTR6 (pKi = 6.2) in the GPCR scan. For others check the GPCR scan data.

Orthogonal Probes def

CAPMATINIB
AMG-337

Chemical Information

Molecular Formula C17H15N5
SMILEs CC1=C(C#N)C(c2ccc3[nH]nc(C)c3c2)C(C#N)=C(C)N1
InChI InChI=1S/C17H15N5/c1-9-14(7-18)17(15(8-19)10(2)20-9)12-4-5-16-13(6-12)11(3)21-22-16/h4-6,17,20H,1-3H3,(H,21,22)
Molecular weight 289.13 Da
AlogP 3.1532800000000014
HBond acceptors 5
HBond donors 2
Atoms 37

Vendors

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Expert Reviews

by SERP
(on 5 Mar 2026 )
Cellular Use Rating
In Model Organisms
BAY474 is a MET inhibitor developed by Bayer and released subsequently as a chemical probe. It shows strong inhibition of MET in vitro and in vivo but also inhibits RSK family members and FLT1. In animals...
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