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JNJ-31020028 | JNJ-31020028 : Antagonist of NPY2R
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
NPY2R
  • IC50:10 nM
Antagonist
up to 1 uM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
>100-fold selective versus human Y1, Y4, and Y5 receptors in radioligand binding assays
In Vitro Selectivity Assessment
Potency Assay Off-Target:
The selectivity of JNJ-31020028 was evaluated in a large variety of ion channels, transporters, rece ...
Selectivity Assessment Description:
JNJ-31020028 was assayed by binding in a panel of 50 receptors, ion channels, and transporters assay ...

Potency
Cellular
In Vitro

NPY2R

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1007/s00213-009-1726-x

In Vivo Validations

Rat
Dose: 10 mg/Kg
Route of delivery: Oral
Plasma half life: 0.53 ± 0.19 h
Systemic clearance: 66.08 ± 56.85 L/h/Kg
Cmax: 0.41 ± 0.27 uM
Tmax: 0.5 ± 0 h
Area Under the Curve:: 0.44 ± 0.34 h*uM
Bioavailability: 6%
Volume of Distribution at Steady-State: 40.29 ± 19.66 L/Kg

DOI Reference: 10.1007/s00213-009-1726-x

Dose: 10 mg/Kg
Route of delivery: Subcutaneous
Plasma half life: 0.83 ± 0.10 h
Systemic clearance: 2.25 ± 0.21 L/h/Kg
Cmax: 4.35 ± 0.95 uM
Tmax: 0.5 ± 0.4 h
Area Under the Curve:: 7.91 ± 0.76 h*uM
Bioavailability: 100%
Volume of Distribution at Steady-State: 2.69 ± 0.25 L/Lg

DOI Reference: 10.1007/s00213-009-1726-x

Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.29 ± 0.02 h
Systemic clearance: 2.54 ± 0.37 L/h/Kg
Cmax: 3.33 ± 1.13 uM
Tmax: 0.03 ± 0 h
Area Under the Curve:: 0.71 ± 0.11 h*uM
Volume of Distribution at Steady-State: 1.07 ± 0.21 L/Kg

DOI Reference: 10.1007/s00213-009-1726-x

Orthogonal Probes def

BIIE0246
JNJ-5207787

Chemical Information

Molecular Formula C34H36FN5O2
SMILEs CCN(CC)C(=O)C(c1ccccc1)N1CCN(c2ccc(NC(=O)c3ccccc3-c3cccnc3)cc2F)CC1
InChI InChI=1S/C34H36FN5O2/c1-3-38(4-2)34(42)32(25-11-6-5-7-12-25)40-21-19-39(20-22-40)31-17-16-27(23-30(31)35)37-33(41)29-15-9-8-14-28(29)26-13-10-18-36-24-26/h5-18,23-24,32H,3-4,19-22H2,1-2H3,(H,37,41)
Molecular weight 565.29 Da
AlogP 5.871700000000006
HBond acceptors 7
HBond donors 1
Atoms 78
PAINS * Yes

* This is an automated alert only, and may not necessarily indicate an issue with this probe. ( Learn more about PAINS )

References

Publications

Cross References

canSARChEMBLBindingDB

Expert Reviews

by SERP
(on 8 Dec 2025 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 11 Dec 2025 )
Cellular Use Rating
In Model Organisms
JNJ 31020028 is a high quality, potent and selective antagonist of the NPYY2 receptor. Although it was found to be ineffective in a variety of anxiety models, receptor occupancy and pharmacodynamic marker...
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