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

CHEMBL3378642

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

Functional
Antagonist activity at mouse SSTR3 expressed in CHO cells assessed as cAMP level by fluorescence analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Somatostatin receptor type 3 (CHEMBL2238)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Investigation of Cardiovascular Effects of Tetrahydro-β-carboline sstr3 antagonists.
He S, Lai Z, Ye Z, Dobbelaar PH, Shah SK, Truong Q, Du W, Guo L, Liu J, Jian T, Qi H, Bakshi RK, Hong Q, Dellureficio J, Reibarkh M, Samuel K, Reddy VB, Mitelman S, Tong SX, Chicchi GG, Tsao KL, Trusca D, Wu M, Shao Q, Trujillo ME, Fernandez G, Nelson D, Bunting P, Kerr J, Fitzgerald P, Morissette P, Volksdorf S, Eiermann GJ, Li C, Zhang B, Howard AD, Zhou YP, Nargund RP, Hagmann WK.
ACS Med Chem Lett (2014) 5 : 748 -753
PubMed 25050159 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.24 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3323084 1 9.80
CHEMBL3323076 1 9.46
CHEMBL3323074 1 9.44
CHEMBL3323072 1 9.24
CHEMBL3323082 1 9.14
CHEMBL3323078 1 8.81
CHEMBL3323085 1 8.54
CHEMBL3323073 1 8.46
CHEMBL3323077 1 8.08
CHEMBL3323079 1 7.85
CHEMBL3323075 1 7.83
CHEMBL3323083 1 7.77
CHEMBL3323080 1 7.47
CHEMBL3323086 1 7.24
CHEMBL3323081 1 6.96
CHEMBL3323087 1 5.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3323084 IC50 = 0.16 nM 9.80
CHEMBL3323076 IC50 = 0.35 nM 9.46
CHEMBL3323074 IC50 = 0.36 nM 9.44
CHEMBL3323072 IC50 = 0.58 nM 9.24
CHEMBL3323082 IC50 = 0.73 nM 9.14
CHEMBL3323078 IC50 = 1.53 nM 8.81
CHEMBL3323085 IC50 = 2.9 nM 8.54
CHEMBL3323073 IC50 = 3.48 nM 8.46
CHEMBL3323077 IC50 = 8.37 nM 8.08
CHEMBL3323079 IC50 = 14.2 nM 7.85
CHEMBL3323075 IC50 = 14.7 nM 7.83
CHEMBL3323083 IC50 = 17.1 nM 7.77
CHEMBL3323080 IC50 = 34.0 nM 7.47
CHEMBL3323086 IC50 = 57.1 nM 7.24
CHEMBL3323081 IC50 = 111.0 nM 6.96
CHEMBL3323087 IC50 = 1863.0 nM 5.73