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BI-6901 | BI-6901 : Antagonist of CCR10
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
CCR10
    • IC50:1 nM
    Antagonist
    100 nM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    No meaningful binding or activity was observed against 29 GPCR’s, including 6 chemokine receptors (s ...

    Potency
    Cellular
    In Vitro

    CCR10

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1016/j.bmcl.2016.09.047

    In Vivo Validations

    Mouse
    Dose: 100 mg/Kg
    Route of delivery: Intraperitoneal
    Plasma half life: <3 min
    Systemic clearance: >88% QH
    Fb : 99%

    DOI Reference: 10.1016/j.bmcl.2016.09.047

    Negative Control Compounds

    CANSAR3872900
    Notes: BI-6902 is the optical antipode of BI-6901 and inhibits the CCL27 dependent Ca2+ flux in CHO-K cells stably transfected with human CCR10 and aequorin with an pIC50 5.5. It was used as a negative control in in vivo pharmacology experiments

    Chemical Information

    Molecular Formula C23H27N5O3S
    SMILEs CC1CCN(C(=O)[C@@H](CCn2cccc2C#N)NS(=O)(=O)c2cccc3[nH]ccc23)CC1
    InChI InChI=1S/C23H27N5O3S/c1-17-8-13-28(14-9-17)23(29)21(10-15-27-12-3-4-18(27)16-24)26-32(30,31)22-6-2-5-20-19(22)7-11-25-20/h2-7,11-12,17,21,25-26H,8-10,13-15H2,1H3/t21-/m1/s1
    Molecular weight 453.18 Da
    AlogP 0.0
    HBond acceptors 8
    HBond donors 2
    Atoms 59

    Vendors

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    Expert Reviews

    No SERP comments found for BI-6901

    Probe BI-6901 is in the process of SERP review.

    Please continue to check back for new reviews and commentary.