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Assay Detail

CHEMBL1767824

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

Functional
Agonist activity at human SST2 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP release after 40 mins by luminescence assay
18
Total Activities
18
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

Somatostatin receptor type 2 (CHEMBL1804)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and evaluation of novel 3,6-diaryl-4-aminoalkoxyquinolines as selective agonists of somatostatin receptor subtype 2.
Wolkenberg SE, Zhao Z, Thut C, Maxwell JW, McDonald TP, Kinose F, Reilly M, Lindsley CW, Hartman GD.
J Med Chem (2011) 54 : 2351 -2358
PubMed 21395312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 8.28 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1766090 1 9.54
CHEMBL1766102 1 9.42
CHEMBL1766096 1 9.42
CHEMBL1766099 1 9.41
CHEMBL1766097 1 8.96
CHEMBL1766094 1 8.33
CHEMBL1766103 1 8.32
CHEMBL1766100 1 8.32
CHEMBL1766110 1 8.12
CHEMBL1766104 1 8.08
CHEMBL1766089 1 8.08
CHEMBL1766093 1 7.96
CHEMBL1766105 1 7.96
CHEMBL1766098 1 7.89
CHEMBL1766095 1 7.70
CHEMBL1766091 1 7.47
CHEMBL1766092 1 7.30
CHEMBL1766101 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1766090 IC50 = 0.29 nM 9.54
CHEMBL1766102 IC50 = 0.38 nM 9.42
CHEMBL1766096 IC50 = 0.38 nM 9.42
CHEMBL1766099 IC50 = 0.39 nM 9.41
CHEMBL1766097 IC50 = 1.1 nM 8.96
CHEMBL1766094 IC50 = 4.7 nM 8.33
CHEMBL1766103 IC50 = 4.8 nM 8.32
CHEMBL1766100 IC50 = 4.8 nM 8.32
CHEMBL1766110 IC50 = 7.6 nM 8.12
CHEMBL1766104 IC50 = 8.3 nM 8.08
CHEMBL1766089 IC50 = 8.3 nM 8.08
CHEMBL1766093 IC50 = 11.0 nM 7.96
CHEMBL1766105 IC50 = 11.0 nM 7.96
CHEMBL1766098 IC50 = 13.0 nM 7.89
CHEMBL1766095 IC50 = 20.0 nM 7.70
CHEMBL1766091 IC50 = 34.0 nM 7.47
CHEMBL1766092 IC50 = 50.0 nM 7.30
CHEMBL1766101 IC50 = 145.0 nM 6.84