Chemical Probes logo
L-745870 | Antagonist of DRD4
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DRD4
    • Ki:0.43 nM
    Antagonist
    up to 1 uM

    Selectivity

    In Vitro Selectivity Assessment
    Selectivity Assessment Description:
    Within Target family: Selective against human D2 and D3 receptors with Ki 960 and 2300 nM respective ...

    Potency
    Cellular
    In Vitro

    DRD4

    Mode of Action: Antagonist

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/jm9600712

    In Vivo Validations

    Rat
    Dose: 3 mg/Kg
    Route of delivery: Intravenous, Oral
    Plasma half life: 2.1 h (plasma)
    Cmax: 360 ng/mL (plasma), 5.1 ug/mL (brain)
    Bioavailability: 66%
    Organ of interest (O): Brain
    Target engagement assay: Brain/Plasma ratio >10 ED50 3.0 mg/Kg in sigma assay

    PMID Reference: 9353380

    Dose: 1 mg/Kg
    Route of delivery: Intravenous, Oral
    Plasma half life: 2.8 h (plasma)
    Cmax: 35 ng/mL (plasma)
    Bioavailability: 20%

    PMID Reference: 9353380

    Chemical Information

    Molecular Formula C18H19ClN4
    SMILEs Clc1ccc(N2CCN(Cc3c[nH]c4ncccc34)CC2)cc1
    InChI InChI=1S/C18H19ClN4/c19-15-3-5-16(6-4-15)23-10-8-22(9-11-23)13-14-12-21-18-17(14)2-1-7-20-18/h1-7,12H,8-11,13H2,(H,20,21)
    Molecular weight 326.13 Da
    AlogP 3.5385000000000018
    HBond acceptors 4
    HBond donors 1
    Atoms 42

    References

    Publications

    Cross References

    Vendors

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

    Expert Reviews

    by SERP
    (on 25 Jul 2022 )
    Cellular Use Rating
    In Model Organisms
    Careful interpretation from in vivo study by means of this compound would be required because of the limited broader selectivity profiles against other targets. One mg/kg (in rats) could be used in lab...
    by SERP
    (on 2 Aug 2022 )
    In Model Organisms
    ( The reviewer did not leave any comments )
    by SERP+
    (on 14 Oct 2025 )
    Cellular Use Rating
    In Model Organisms
    L-745870 is a brain penetrant antagonist of dopamine D4 receptor, which demonstrates high potency (Ki = 0.4 nM) against D4 and 2000 and 5000 fold selectivity over D2 and D3 receptors, respectively. L-745870...
    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