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BAY-3153 | BAY-3153 : Antagonist of CCR1
RATINGS:
Cellular Use: (0 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
CCR1
    • IC50:3 nM
    Antagonist
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Selectivity within target family: Inactive on CCR3 (human); IC50 > 30 µM for human CCR2, CCR4, CCR5, ...

    Potency
    Cellular
    In Vitro

    CCR1

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    Other Reference: peer reviewed at SGC

    In Vivo Validations

    Rat
    Dose: 10 mg/Kg

    DOI Reference: 10.6019/CHEMBL4630906

    Negative Control Compounds

    BAY-173
    Notes: BAY-173 with 400-fold less in vitro potency (IC50 = 1200 nM (human), 8500 nM (mice); biochemical CCR1 assay); Shows weak activity in the GPCR scan: The closest off-target is SLC6A4 (SERT) (Ki = 1460.83 nM)

    Orthogonal Probes def

    BI 639667

    Chemical Information

    Molecular Formula C25H29Cl2N3O4
    SMILEs CCOc1cc(N2C3COCC2CN(C(=O)[C@H]2C[C@H](O)CN2c2ccc(Cl)cc2)C3)ccc1Cl
    InChI InChI=1S/C25H29Cl2N3O4/c1-2-34-24-9-18(7-8-22(24)27)30-19-11-28(12-20(30)15-33-14-19)25(32)23-10-21(31)13-29(23)17-5-3-16(26)4-6-17/h3-9,19-21,23,31H,2,10-15H2,1H3/t19?,20?,21-,23+/m0/s1
    Molecular weight 505.15 Da
    AlogP 0.0
    HBond acceptors 7
    HBond donors 1
    Atoms 63

    Expert Reviews

    No SERP comments found for BAY-3153

    Probe BAY-3153 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.