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Assay Detail

CHEMBL4841562

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Functional
Agonist activity at human SSTR2 expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by GloSensor cAMP Assay
25
Total Activities
25
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

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

Publication

Design, synthesis, and biological evaluation of novel somatostatin receptor subtype-2 agonists: Optimization for potency and risk mitigation of hERG and phospholipidosis.
Ishida A, Okabe Y, Matsushita T, Sekiguchi T, Nishio T, Komagata T, Iwaki M, Miyata H, Katagi J, Naganawa A, Maruyama T, Imagawa A.
Bioorg Med Chem (2021) 49 : 116424 -116424
PubMed 34626901 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 25 10.14 10.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4866325 1 10.89
CHEMBL4872591 1 10.89
CHEMBL4861425 1 10.89
CHEMBL4849848 1 10.85
CHEMBL4860633 1 10.82
CHEMBL4873269 1 10.77
CHEMBL4853282 1 10.72
CHEMBL4858892 1 10.57
CHEMBL1680 OCTREOTIDE 4.0 1 10.52
CHEMBL4863880 1 10.52
CHEMBL4845867 1 10.40
CHEMBL4870834 1 10.39
CHEMBL4862195 1 10.32
CHEMBL4876263 1 10.11
CHEMBL4851978 1 10.10
CHEMBL4878917 1 10.09
CHEMBL4854548 1 10.00
CHEMBL4862497 1 9.92
CHEMBL4862717 1 9.85
CHEMBL4854239 1 9.68
CHEMBL4856293 1 9.33
CHEMBL4856084 1 9.23
CHEMBL4878248 1 9.10
CHEMBL4868777 1 9.00
CHEMBL4845931 1 8.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4866325 EC50 = 0.013 nM 10.89
CHEMBL4872591 EC50 = 0.013 nM 10.89
CHEMBL4861425 EC50 = 0.013 nM 10.89
CHEMBL4849848 EC50 = 0.014 nM 10.85
CHEMBL4860633 EC50 = 0.015 nM 10.82
CHEMBL4873269 EC50 = 0.017 nM 10.77
CHEMBL4853282 EC50 = 0.019 nM 10.72
CHEMBL4858892 EC50 = 0.027 nM 10.57
CHEMBL1680 OCTREOTIDE EC50 = 0.03 nM 10.52
CHEMBL4863880 EC50 = 0.03 nM 10.52
CHEMBL4845867 EC50 = 0.04 nM 10.40
CHEMBL4870834 EC50 = 0.041 nM 10.39
CHEMBL4862195 EC50 = 0.048 nM 10.32
CHEMBL4876263 EC50 = 0.078 nM 10.11
CHEMBL4851978 EC50 = 0.08 nM 10.10
CHEMBL4878917 EC50 = 0.081 nM 10.09
CHEMBL4854548 EC50 = 0.1 nM 10.00
CHEMBL4862497 EC50 = 0.12 nM 9.92
CHEMBL4862717 EC50 = 0.14 nM 9.85
CHEMBL4854239 EC50 = 0.21 nM 9.68
CHEMBL4856293 EC50 = 0.47 nM 9.33
CHEMBL4856084 EC50 = 0.59 nM 9.23
CHEMBL4878248 EC50 = 0.8 nM 9.10
CHEMBL4868777 EC50 = 1.0 nM 9.00
CHEMBL4845931 EC50 = 3.7 nM 8.43