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BMS-986235 | BMS-986235 : Agonist of FPR2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (3 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
FPR2
    • EC50:0.41 nM
    • EC50:5.0 nM
    • EC50:5 nM to 13 nM; 260 nM and 855 nM
    Agonist
    100 nM to 1µM
    up to 100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Selective against FRP2 6800 fold

    Potency
    Cellular
    In Vitro

    FPR2

    Mode of Action: Agonist

    Structure-Activity-Relationship data available? No

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    In Vivo Validations

    Mouse
    Dose: 0.5 mg/Kg
    Route of delivery: Intravenous
    Systemic clearance: 90 mL/min/Kg
    Volume of Distribution at Steady-State: 3.5 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Dose: 1 mg/Kg
    Route of delivery: Oral
    Plasma half life: 0.68 h
    Cmax: 160 nM
    Area Under the Curve:: 120 nM*h
    Bioavailability: 24%

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Rat
    Dose: 1.0 mg/Kg
    Route of delivery: Intravenous
    Bioavailability: 49 mL/min/Kg
    Volume of Distribution at Steady-State: 3.0 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Dose: 1.0 mg/Kg
    Route of delivery: Oral
    Plasma half life: 3.8 h
    Cmax: 240 nM
    Area Under the Curve:: 640 nM*h
    Bioavailability: 67%

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Dog
    Dose: 1.0 mg/Kg
    Route of delivery: Intravenous
    Systemic clearance: 6.6 mL/min/Kg
    Volume of Distribution at Steady-State: 0.98 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Dose: 1.0 mg/Kg
    Route of delivery: Oral
    Plasma half life: 2.5 h
    Cmax: 820 nM
    Area Under the Curve:: 5700 nM*h
    Bioavailability: 50%

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Monkey (Cynomolgus)
    Dose: 1.0 mg/Kg
    Route of delivery: Intravenous
    Systemic clearance: 12 mL/min/Kg
    Volume of Distribution at Steady-State: 1.2 L/Kg

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Dose: 3.0 mg/Kg
    Route of delivery: Intravenous
    Plasma half life: 5.0 h
    Cmax: 800 nM
    Area Under the Curve:: 5800 nM*h
    Bioavailability: 49%

    DOI Reference: 10.1021/acs.jmedchem.9b02101

    Chemical Information

    Molecular Formula C18H17F2N3O3
    SMILEs COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1
    InChI InChI=1S/C18H17F2N3O3/c1-26-11-7-13(19)15(14(20)8-11)12-9-21-17(24)16(12)23-18(25)22-10-5-3-2-4-6-10/h2-8,12,16H,9H2,1H3,(H,21,24)(H2,22,23,25)/t12-,16-/m0/s1
    Molecular weight 361.12 Da
    AlogP 0.0
    HBond acceptors 6
    HBond donors 3
    Atoms 43

    References

    Publications

    Cross References

    canSARChEMBLBindingDB

    Vendors

    Note: This is not an exhaustive list and does not indicate endorsement by the portal.

    Expert Reviews

    by SERP
    (on 4 Mar 2024 )
    Cellular Use Rating
    In Model Organisms
    Based on the public information there is no outside family selectivity data. Therefore, the users might also want to consider this point in interpreting the experimental outcomes. The indicated doses are...
    by SERP
    (on 17 Mar 2024 )
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP+
    (on 14 Oct 2025 )
    Cellular Use Rating
    In Model Organisms
    This is a highly potent FPR2 agonist with good selectivity against FPR1. However, no wider selectivity profiling beyond FPR1 and 2 have been provided. For cAMP biased signaling a dose no higher than 50nM...
    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