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Assay Detail

CHEMBL5225666

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Binding
Agonist activity at human SST2 receptor expressed in CHO-K1 cells assessed as inhibition of NKH477-induced intracellular cAMP accumulation incubated for 20 mins by HTRF assay
ChEMBL ↗
60
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Discovery of Paltusotine (CRN00808), a Potent, Selective, and Orally Bioavailable Non-peptide SST2 Agonist.
Zhao J, Wang S, Markison S, Kim SH, Han S, Chen M, Kusnetzow AK, Rico-Bautista E, Johns M, Luo R, Struthers RS, Madan A, Zhu Y, Betz SF.
ACS Med Chem Lett (2023) 14 : 66 -74
PubMed 36655128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 60 8.18 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5286005 — — 2 9.92
CHEMBL5279239 — — 2 9.85
CHEMBL5279994 — — 2 9.80
CHEMBL5286879 — — 2 9.80
CHEMBL5283444 — — 2 9.80
CHEMBL5267842 PALTUSOTINE 3.0 2 9.60
CHEMBL5273084 — — 2 9.51
CHEMBL5276605 — — 2 9.50
CHEMBL5268837 — — 2 8.90
CHEMBL5289166 — — 2 8.72
CHEMBL5275725 — — 2 8.60
CHEMBL5286792 — — 2 8.50
CHEMBL5279790 — — 2 8.50
CHEMBL5278345 — — 2 8.33
CHEMBL5286495 — — 2 8.14
CHEMBL5286126 — — 2 8.04
CHEMBL5285564 — — 2 8.00
CHEMBL5270619 — — 2 7.60
CHEMBL5273476 — — 2 7.52
CHEMBL5273093 — — 2 7.52
CHEMBL5267035 — — 2 7.51
CHEMBL4760001 — — 2 7.44
CHEMBL4789268 — — 2 7.42
CHEMBL5288602 — — 2 7.30
CHEMBL5279978 — — 2 7.20
CHEMBL5270465 — — 2 6.90
CHEMBL5272881 — — 2 6.40
CHEMBL5290669 — — 2 6.24
CHEMBL5271468 — — 2 6.10
CHEMBL5266662 — — 2 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5286005 — EC50 = 0.12 nM 9.92
CHEMBL5286005 — EC50 = 0.1259 nM 9.90
CHEMBL5279239 — EC50 = 0.14 nM 9.85
CHEMBL5283444 — EC50 = 0.1585 nM 9.80
CHEMBL5279239 — EC50 = 0.1585 nM 9.80
CHEMBL5286879 — EC50 = 0.1585 nM 9.80
CHEMBL5279994 — EC50 = 0.1585 nM 9.80
CHEMBL5283444 — EC50 = 0.16 nM 9.80
CHEMBL5286879 — EC50 = 0.17 nM 9.77
CHEMBL5279994 — EC50 = 0.17 nM 9.77
CHEMBL5267842 PALTUSOTINE EC50 = 0.2512 nM 9.60
CHEMBL5267842 PALTUSOTINE EC50 = 0.25 nM 9.60
CHEMBL5273084 — EC50 = 0.31 nM 9.51
CHEMBL5273084 — EC50 = 0.3162 nM 9.50
CHEMBL5276605 — EC50 = 0.3162 nM 9.50
CHEMBL5276605 — EC50 = 0.34 nM 9.47
CHEMBL5268837 — EC50 = 1.259 nM 8.90
CHEMBL5268837 — EC50 = 1.4 nM 8.85
CHEMBL5289166 — EC50 = 1.9 nM 8.72
CHEMBL5289166 — EC50 = 1.995 nM 8.70
CHEMBL5275725 — EC50 = 2.512 nM 8.60
CHEMBL5275725 — EC50 = 2.5 nM 8.60
CHEMBL5286792 — EC50 = 3.162 nM 8.50
CHEMBL5279790 — EC50 = 3.162 nM 8.50
CHEMBL5279790 — EC50 = 3.4 nM 8.47
CHEMBL5286792 — EC50 = 3.5 nM 8.46
CHEMBL5278345 — EC50 = 4.7 nM 8.33
CHEMBL5278345 — EC50 = 5.012 nM 8.30
CHEMBL5286495 — EC50 = 7.3 nM 8.14
CHEMBL5286495 — EC50 = 7.943 nM 8.10
CHEMBL5286126 — EC50 = 9.2 nM 8.04
CHEMBL5285564 — EC50 = 10.0 nM 8.00
CHEMBL5286126 — EC50 = 10.0 nM 8.00
CHEMBL5285564 — EC50 = 10.0 nM 8.00
CHEMBL5270619 — EC50 = 25.12 nM 7.60
CHEMBL5270619 — EC50 = 26.0 nM 7.58
CHEMBL5273093 — EC50 = 30.0 nM 7.52
CHEMBL5273476 — EC50 = 30.0 nM 7.52
CHEMBL5267035 — EC50 = 31.0 nM 7.51
CHEMBL5267035 — EC50 = 31.62 nM 7.50
CHEMBL5273093 — EC50 = 31.62 nM 7.50
CHEMBL5273476 — EC50 = 31.62 nM 7.50
CHEMBL4760001 — EC50 = 36.0 nM 7.44
CHEMBL4789268 — EC50 = 38.0 nM 7.42
CHEMBL4789268 — EC50 = 39.81 nM 7.40
CHEMBL4760001 — EC50 = 39.81 nM 7.40
CHEMBL5288602 — EC50 = 50.12 nM 7.30
CHEMBL5288602 — EC50 = 50.0 nM 7.30
CHEMBL5279978 — EC50 = 63.1 nM 7.20
CHEMBL5279978 — EC50 = 63.0 nM 7.20