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Assay Detail

CHEMBL1212092

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

Functional
Agonist activity at human cannabinoid CB1 receptor expressed in CHO cells after 5 hrs by luciferase reporter gene assay
19
Total Activities
19
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

Cannabinoid receptor 1 (CHEMBL218)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.
Kiyoi T, York M, Francis S, Edwards D, Walker G, Houghton AK, Cottney JE, Baker J, Adam JM.
Bioorg Med Chem Lett (2010) 20 : 4918 -4921
PubMed 20634067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 7.36 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1209644 1 8.40
CHEMBL1209807 1 8.30
CHEMBL1209806 1 8.20
CHEMBL1209645 1 8.20
CHEMBL1209647 1 8.00
CHEMBL1209710 1 7.80
CHEMBL1209572 1 7.60
CHEMBL1209708 1 7.60
CHEMBL1209709 1 7.60
CHEMBL1209573 1 7.50
CHEMBL1209502 1 7.50
CHEMBL1209712 1 7.20
CHEMBL1209576 1 7.00
CHEMBL1209646 1 6.90
CHEMBL1209575 1 6.80
CHEMBL1209711 1 6.30
CHEMBL1209805 1 6.10
CHEMBL1209643 1 5.40
CHEMBL1209574 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1209644 EC50 = 3.981 nM 8.40
CHEMBL1209807 EC50 = 5.012 nM 8.30
CHEMBL1209806 EC50 = 6.31 nM 8.20
CHEMBL1209645 EC50 = 6.31 nM 8.20
CHEMBL1209647 EC50 = 10.0 nM 8.00
CHEMBL1209710 EC50 = 15.85 nM 7.80
CHEMBL1209572 EC50 = 25.12 nM 7.60
CHEMBL1209708 EC50 = 25.12 nM 7.60
CHEMBL1209709 EC50 = 25.12 nM 7.60
CHEMBL1209573 EC50 = 31.62 nM 7.50
CHEMBL1209502 EC50 = 31.62 nM 7.50
CHEMBL1209712 EC50 = 63.1 nM 7.20
CHEMBL1209576 EC50 = 100.0 nM 7.00
CHEMBL1209646 EC50 = 125.89 nM 6.90
CHEMBL1209575 EC50 = 158.49 nM 6.80
CHEMBL1209711 EC50 = 501.19 nM 6.30
CHEMBL1209805 EC50 = 794.33 nM 6.10
CHEMBL1209643 EC50 = 3981.07 nM 5.40
CHEMBL1209574 EC50 > 10000.0 nM -