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Assay Detail

CHEMBL5115996

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Functional
Agonist activity at human SST5 expressed in CHO-K1 cells assessed as reduction in NKH477-induced intracellular cAMP level
ChEMBL ↗
86
Total Activities
43
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 5 (CHEMBL1792) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-(3-aminopyrrolidinyl)-3-aryl-5-(benzimidazol-2-yl)-pyridines as potent and selective SST5 agonists for the treatment of congenital hyperinsulinism.
Zhao J, Wang S, Hee Kim S, Han S, Rico-Bautista E, Sturchler E, Nguyen J, Tan H, Staley C, Karin Kusnetzow A, Betz SF, Johns M, Goulet L, Luo R, Fowler M, Athanacio J, Markison S, Scott Struthers R, Zhu Y.
Bioorg Med Chem Lett (2022) 71 : 128807 -128807
PubMed 35605837 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 86 8.57 10.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5208674 — — 2 10.33
CHEMBL5179782 — — 2 10.15
CHEMBL5178891 — — 2 10.11
CHEMBL5169724 — — 2 10.10
CHEMBL5180885 — — 2 9.70
CHEMBL5174433 — — 2 9.64
CHEMBL5176490 — — 2 9.60
CHEMBL5192315 — — 2 9.60
CHEMBL5186952 — — 2 9.50
CHEMBL5170249 — — 2 9.44
CHEMBL5195355 — — 2 9.43
CHEMBL5184249 — — 2 9.30
CHEMBL5202527 — — 2 9.30
CHEMBL5177934 — — 2 9.21
CHEMBL5200076 — — 2 9.20
CHEMBL5201920 — — 2 9.01
CHEMBL5198832 — — 2 9.00
CHEMBL5193208 — — 2 8.92
CHEMBL5180721 — — 2 8.80
CHEMBL5188855 — — 2 8.70
CHEMBL5204225 — — 2 8.70
CHEMBL5187920 — — 2 8.70
CHEMBL5181646 — — 2 8.64
CHEMBL5184298 — — 2 8.64
CHEMBL5182636 — — 2 8.60
CHEMBL5188516 — — 2 8.50
CHEMBL5208031 — — 2 8.40
CHEMBL5169928 — — 2 8.30
CHEMBL5177695 — — 2 8.30
CHEMBL5182561 — — 2 8.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5208674 — EC50 = 0.047 nM 10.33
CHEMBL5208674 — EC50 = 0.05012 nM 10.30
CHEMBL5179782 — EC50 = 0.071 nM 10.15
CHEMBL5178891 — EC50 = 0.077 nM 10.11
CHEMBL5169724 — EC50 = 0.07943 nM 10.10
CHEMBL5179782 — EC50 = 0.07943 nM 10.10
CHEMBL5178891 — EC50 = 0.07943 nM 10.10
CHEMBL5169724 — EC50 = 0.088 nM 10.06
CHEMBL5180885 — EC50 = 0.1995 nM 9.70
CHEMBL5180885 — EC50 = 0.2 nM 9.70
CHEMBL5174433 — EC50 = 0.23 nM 9.64
CHEMBL5176490 — EC50 = 0.2512 nM 9.60
CHEMBL5174433 — EC50 = 0.2512 nM 9.60
CHEMBL5192315 — EC50 = 0.2512 nM 9.60
CHEMBL5176490 — EC50 = 0.27 nM 9.57
CHEMBL5192315 — EC50 = 0.27 nM 9.57
CHEMBL5186952 — EC50 = 0.3162 nM 9.50
CHEMBL5186952 — EC50 = 0.32 nM 9.49
CHEMBL5170249 — EC50 = 0.36 nM 9.44
CHEMBL5195355 — EC50 = 0.37 nM 9.43
CHEMBL5195355 — EC50 = 0.3981 nM 9.40
CHEMBL5170249 — EC50 = 0.3981 nM 9.40
CHEMBL5184249 — EC50 = 0.5012 nM 9.30
CHEMBL5202527 — EC50 = 0.5012 nM 9.30
CHEMBL5202527 — EC50 = 0.55 nM 9.26
CHEMBL5184249 — EC50 = 0.56 nM 9.25
CHEMBL5177934 — EC50 = 0.62 nM 9.21
CHEMBL5200076 — EC50 = 0.631 nM 9.20
CHEMBL5177934 — EC50 = 0.631 nM 9.20
CHEMBL5200076 — EC50 = 0.65 nM 9.19
CHEMBL5201920 — EC50 = 0.97 nM 9.01
CHEMBL5201920 — EC50 = 1.0 nM 9.00
CHEMBL5198832 — EC50 = 1.0 nM 9.00
CHEMBL5198832 — EC50 = 1.0 nM 9.00
CHEMBL5193208 — EC50 = 1.2 nM 8.92
CHEMBL5193208 — EC50 = 1.259 nM 8.90
CHEMBL5180721 — EC50 = 1.585 nM 8.80
CHEMBL5180721 — EC50 = 1.7 nM 8.77
CHEMBL5188855 — EC50 = 1.995 nM 8.70
CHEMBL5187920 — EC50 = 1.995 nM 8.70
CHEMBL5204225 — EC50 = 1.995 nM 8.70
CHEMBL5204225 — EC50 = 2.1 nM 8.68
CHEMBL5188855 — EC50 = 2.2 nM 8.66
CHEMBL5181646 — EC50 = 2.3 nM 8.64
CHEMBL5184298 — EC50 = 2.3 nM 8.64
CHEMBL5184298 — EC50 = 2.512 nM 8.60
CHEMBL5181646 — EC50 = 2.512 nM 8.60
CHEMBL5182636 — EC50 = 2.512 nM 8.60
CHEMBL5182636 — EC50 = 2.6 nM 8.59
CHEMBL5187920 — EC50 = 2.9 nM 8.54