Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1211328

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at human recombinant NPS receptor expressed in CHOK1 cells assessed as inhibition of NPS-induced calcium mobilization by FLIPR assay
14
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuropeptide S receptor (CHEMBL5162)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of a new series of Neuropeptide S receptor antagonists.
Melamed JY, Zartman AE, Kett NR, Gotter AL, Uebele VN, Reiss DR, Condra CL, Fandozzi C, Lubbers LS, Rowe BA, McGaughey GB, Henault M, Stocco R, Renger JJ, Hartman GD, Bilodeau MT, Trotter BW.
Bioorg Med Chem Lett (2010) 20 : 4700 -4703
PubMed 20510609 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 7.10 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1210244 1 8.15
CHEMBL1210313 3 8.00
CHEMBL1210311 1 7.85
CHEMBL1210177 1 7.75
CHEMBL1210312 1 7.66
CHEMBL1210242 1 7.51
CHEMBL1210411 1 6.99
CHEMBL1210243 1 6.84
CHEMBL1210241 1 6.49
CHEMBL1210412 1 6.40
CHEMBL1210179 1 6.14
CHEMBL1210178 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1210244 IC50 = 7.0 nM 8.15
CHEMBL1210313 IC50 = 10.0 nM 8.00
CHEMBL1210311 IC50 = 14.0 nM 7.85
CHEMBL1210177 IC50 = 18.0 nM 7.75
CHEMBL1210312 IC50 = 22.0 nM 7.66
CHEMBL1210313 IC50 = 23.0 nM 7.64
CHEMBL1210242 IC50 = 31.0 nM 7.51
CHEMBL1210411 IC50 = 103.0 nM 6.99
CHEMBL1210243 IC50 = 144.0 nM 6.84
CHEMBL1210241 IC50 = 326.0 nM 6.49
CHEMBL1210412 IC50 = 398.0 nM 6.40
CHEMBL1210179 IC50 = 725.0 nM 6.14
CHEMBL1210313 IC50 = 785.0 nM 6.11
CHEMBL1210178 IC50 = 1577.0 nM 5.80