Chemical Probes logo
L-365260 | L-365260 : Antagonist of CCKBR
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CCKBR
  • Ki:2 nM
  • IC50:2 nM
Antagonist
up to 500 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Lack of activity (IC50 > 10 >uM) in various other radioligand binding assays including M1 and M2 ace ...

Potency
Cellular
In Vitro

CCKBR

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/jm00121a004

In Vivo Validations

Rat
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 35.7 ± 8.0 min
Systemic clearance: 56.8 ± 18.7 mL/min/Kg
Volume of Distribution at Steady-State: 1.80 ± 0.30 L/Kg

PMID Reference: 1355713

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 143.0 ± 78.0 min
Cmax: 0.061 ± 0.021 ug/mL
Tmax: 47.5 ± 48.6 min
Area Under the Curve:: 13.0 ± 7.2 ug*min/mL
Bioavailability: 13.6%

PMID Reference: 1355713

Dog
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 101.6 ± 34 min
Systemic clearance: 12.4 ± 0.8 mL/min/Kg
Volume of Distribution at Steady-State: 1.57 ± 0.30 L/Kg

PMID Reference: 1355713

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 109.0 ± 37.0 min
Cmax: 0.300 ± 0.099 ug/mL
Tmax: 109.0 ± 37.0 min
Area Under the Curve:: 35.9 ± 9.2 ug*min/mL
Bioavailability: 8.8 ± 1.9%

PMID Reference: 1355713

Monkey (Rheus)
Dose: 5 mg/Kg
Route of delivery: Intravenous
Plasma half life: 71.7 ± 7 min
Systemic clearance: 12.6 ± 3.3 mL/min/Kg
Volume of Distribution at Steady-State: 1.04 ± 0.12 L/Kg

PMID Reference: 1355713

Dose: 50 mg/Kg
Route of delivery: Oral
Plasma half life: 118.0 ± 37.0 min
Cmax: 0.538 ± 0.346 ug/mL
Tmax: 40.0 ± 16.0 min
Area Under the Curve:: 83.7 ± 59.9 ug*min/mL
Bioavailability: 1.8 ± 1.1%

PMID Reference: 1355713

Negative Control Compounds

CANSAR236284
Notes: S-Enantiomer IC50 = 151 nM in brain

Chemical Information

Molecular Formula C24H22N4O2
SMILEs Cc1cccc(NC(=O)N[C@@H]2N=C(c3ccccc3)c3ccccc3N(C)C2=O)c1
InChI InChI=1S/C24H22N4O2/c1-16-9-8-12-18(15-16)25-24(30)27-22-23(29)28(2)20-14-7-6-13-19(20)21(26-22)17-10-4-3-5-11-17/h3-15,22H,1-2H3,(H2,25,27,30)/t22-/m0/s1
Molecular weight 398.17 Da
AlogP 3.9566200000000027
HBond acceptors 6
HBond donors 2
Atoms 52

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 17 Aug 2022 )
Cellular Use Rating
In Model Organisms
This probe, having been disclosed in 1989, was shown to be a selective (~87-fold) antagonist of CCK-B relative to CCK-A. It was also shown to possess reasonable exposure (194 ug/mL at 2 hours) following...
by SERP+
(on 14 Oct 2025 )
Cellular Use Rating
In Model Organisms
The compound has been profiled in a smaller GPCR panel including muscarinic receptors, adrenal receptors and histamine receptors. Its in vivo use and doses used varies in different publications.
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