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Assay Detail

CHEMBL4669860

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Functional
Agonist activity at human SST2 expressed in CHOK1 cells assessed as inhibition of NKH477-stimulated intracellular cAMP levels
ChEMBL ↗
73
Total Activities
37
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

Discovery of substituted 3H-pyrido[2,3-d]pyrimidin-4-ones as potent, biased, and orally bioavailable sst2 agonist.
Zhao J,Chen Z,Kusnetzow AK,Nguyen J,Rico-Bautista E,Tan H,Betz SF,Struthers RS,Zhu Y
Bioorg Med Chem Lett (2020) 30 : 127496 -127496
PubMed 32805408 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 73 7.65 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741372 — — 2 9.40
CHEMBL4778342 — — 1 9.30
CHEMBL4750168 — — 2 8.92
CHEMBL4754720 — — 2 8.92
CHEMBL4747697 — — 2 8.80
CHEMBL4756956 — — 2 8.50
CHEMBL4760476 — — 2 8.50
CHEMBL4745767 — — 2 8.42
CHEMBL4778857 — — 2 8.32
CHEMBL4742147 — — 2 8.21
CHEMBL4740611 — — 2 8.13
CHEMBL4741139 — — 2 8.00
CHEMBL4800376 — — 2 7.90
CHEMBL4748425 — — 2 7.82
CHEMBL4800534 — — 2 7.60
CHEMBL4782501 — — 2 7.51
CHEMBL4760001 — — 2 7.44
CHEMBL4799254 — — 2 7.40
CHEMBL4749169 — — 2 7.40
CHEMBL4758610 — — 2 7.30
CHEMBL4752814 — — 2 7.20
CHEMBL4784765 — — 2 7.00
CHEMBL4777739 — — 2 7.00
CHEMBL4744310 — — 2 6.96
CHEMBL4752223 — — 2 6.92
CHEMBL4754672 — — 2 6.80
CHEMBL4776516 — — 2 6.70
CHEMBL4792889 — — 2 6.60
CHEMBL4761276 — — 2 6.60
CHEMBL4749667 — — 2 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741372 — EC50 = 0.4 nM 9.40
CHEMBL4741372 — EC50 = 0.3981 nM 9.40
CHEMBL4778342 — EC50 = 0.5012 nM 9.30
CHEMBL4754720 — EC50 = 1.2 nM 8.92
CHEMBL4750168 — EC50 = 1.2 nM 8.92
CHEMBL4750168 — EC50 = 1.259 nM 8.90
CHEMBL4754720 — EC50 = 1.259 nM 8.90
CHEMBL4747697 — EC50 = 1.585 nM 8.80
CHEMBL4747697 — EC50 = 1.8 nM 8.74
CHEMBL4760476 — EC50 = 3.162 nM 8.50
CHEMBL4756956 — EC50 = 3.162 nM 8.50
CHEMBL4760476 — EC50 = 3.2 nM 8.49
CHEMBL4756956 — EC50 = 3.4 nM 8.47
CHEMBL4745767 — EC50 = 3.8 nM 8.42
CHEMBL4745767 — EC50 = 3.981 nM 8.40
CHEMBL4778857 — EC50 = 4.8 nM 8.32
CHEMBL4742147 — EC50 = 6.1 nM 8.21
CHEMBL4742147 — EC50 = 6.31 nM 8.20
CHEMBL4778857 — EC50 = 6.31 nM 8.20
CHEMBL4740611 — EC50 = 7.4 nM 8.13
CHEMBL4740611 — EC50 = 7.943 nM 8.10
CHEMBL4741139 — EC50 = 10.0 nM 8.00
CHEMBL4741139 — EC50 = 11.0 nM 7.96
CHEMBL4800376 — EC50 = 12.59 nM 7.90
CHEMBL4800376 — EC50 = 14.0 nM 7.85
CHEMBL4748425 — EC50 = 15.0 nM 7.82
CHEMBL4748425 — EC50 = 15.85 nM 7.80
CHEMBL4800534 — EC50 = 25.12 nM 7.60
CHEMBL4800534 — EC50 = 27.0 nM 7.57
CHEMBL4782501 — EC50 = 31.0 nM 7.51
CHEMBL4782501 — EC50 = 31.62 nM 7.50
CHEMBL4760001 — EC50 = 36.0 nM 7.44
CHEMBL4760001 — EC50 = 39.81 nM 7.40
CHEMBL4799254 — EC50 = 39.81 nM 7.40
CHEMBL4749169 — EC50 = 39.81 nM 7.40
CHEMBL4799254 — EC50 = 42.0 nM 7.38
CHEMBL4749169 — EC50 = 42.0 nM 7.38
CHEMBL4758610 — EC50 = 50.0 nM 7.30
CHEMBL4758610 — EC50 = 50.12 nM 7.30
CHEMBL4752814 — EC50 = 63.1 nM 7.20
CHEMBL4752814 — EC50 = 71.0 nM 7.15
CHEMBL4784765 — EC50 = 100.0 nM 7.00
CHEMBL4784765 — EC50 = 100.0 nM 7.00
CHEMBL4777739 — EC50 = 100.0 nM 7.00
CHEMBL4744310 — EC50 = 110.0 nM 6.96
CHEMBL4777739 — EC50 = 120.0 nM 6.92
CHEMBL4752223 — EC50 = 119.0 nM 6.92
CHEMBL4744310 — EC50 = 125.89 nM 6.90
CHEMBL4754672 — EC50 = 158.49 nM 6.80
CHEMBL4752223 — EC50 = 158.49 nM 6.80