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Assay Detail

CHEMBL3088892

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

Functional
Antagonist activity at neuropeptide S receptor (unknown origin) expressed in CHO cells assessed as cAMP level after 30 mins by phosphate-buffered saline assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationship of imidazopyridinium analogues as antagonists of neuropeptide s receptor.
Patnaik S, Marugan JJ, Liu K, Zheng W, Southall N, Dehdashti SJ, Thorsell A, Heilig M, Bell L, Zook M, Eskay B, Brimacombe KR, Austin CP.
J Med Chem (2013) 56 : 9045 -9056
PubMed 24171469 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.36 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1210313 1 8.92
CHEMBL469695 1 8.28
CHEMBL1474387 1 7.35
CHEMBL3086821 1 7.15
CHEMBL3086837 1 7.03
CHEMBL3086835 1 6.96
CHEMBL3086836 1 6.96
CHEMBL3086823 1 6.92
CHEMBL3086825 1 6.77
CHEMBL3086838 1 6.66
CHEMBL3086822 1 6.48
CHEMBL3086824 1 6.40
CHEMBL3086826 1 6.17
CHEMBL1472563 1 6.15
CHEMBL3086827 1 6.08
CHEMBL1553073 1 6.03
CHEMBL3086820 1 5.89
CHEMBL3086833 1 5.89
CHEMBL1598051 1 5.77
CHEMBL3086834 1 5.68
CHEMBL1315807 1 5.68
CHEMBL1514777 1 4.75
CHEMBL3086829 1 4.41
CHEMBL1393909 1 4.20
CHEMBL1314112 1 -
CHEMBL1701941 1 -
CHEMBL1474508 1 -
CHEMBL3086832 1 -
CHEMBL1589741 1 -
CHEMBL1474223 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1210313 IC50 = 1.2 nM 8.92
CHEMBL469695 IC50 = 5.3 nM 8.28
CHEMBL1474387 IC50 = 45.0 nM 7.35
CHEMBL3086821 IC50 = 71.0 nM 7.15
CHEMBL3086837 IC50 = 94.0 nM 7.03
CHEMBL3086835 IC50 = 110.0 nM 6.96
CHEMBL3086836 IC50 = 110.0 nM 6.96
CHEMBL3086823 IC50 = 120.0 nM 6.92
CHEMBL3086825 IC50 = 170.0 nM 6.77
CHEMBL3086838 IC50 = 220.0 nM 6.66
CHEMBL3086822 IC50 = 330.0 nM 6.48
CHEMBL3086824 IC50 = 400.0 nM 6.40
CHEMBL3086826 IC50 = 670.0 nM 6.17
CHEMBL1472563 IC50 = 710.0 nM 6.15
CHEMBL3086827 IC50 = 840.0 nM 6.08
CHEMBL1553073 IC50 = 940.0 nM 6.03
CHEMBL3086820 IC50 = 1300.0 nM 5.89
CHEMBL3086833 IC50 = 1300.0 nM 5.89
CHEMBL1598051 IC50 = 1700.0 nM 5.77
CHEMBL3086834 IC50 = 2100.0 nM 5.68
CHEMBL1315807 IC50 = 2100.0 nM 5.68
CHEMBL1514777 IC50 = 18000.0 nM 4.75
CHEMBL3086829 IC50 = 39000.0 nM 4.41
CHEMBL1393909 IC50 = 63000.0 nM 4.20
CHEMBL1314112 IC50 - -
CHEMBL1701941 IC50 - -
CHEMBL1474508 IC50 - -
CHEMBL3086832 IC50 - -
CHEMBL1589741 IC50 - -
CHEMBL1474223 IC50 - -
CHEMBL1394028 IC50 - -
CHEMBL1719577 IC50 - -
CHEMBL1358647 IC50 - -