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BAY-474 | BAY-474 : Inhibitor of MET
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 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...
by SERP
(on 12 Apr 2026)
Cellular Use Rating
In Model Organisms
This is a highly potent and selective MET kinase inhibitor, the characterisation of which has been reported on the SGC website in a datasheet from Bayer. Biochemical activity against C-Met is < 1 nM with...
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