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Assay Detail

CHEMBL1014610

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Functional
Agonist activity at human CB2 receptor expressed in yeast cells assessed as degradation of FDGlu to fluorescein after 24 hrs
ChEMBL ↗
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cannabinoid receptor 2 (CHEMBL253) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
Mitchell WL, Giblin GM, Naylor A, Eatherton AJ, Slingsby BP, Rawlings AD, Jandu KS, Haslam CP, Brown AJ, Goldsmith P, Clayton NM, Wilson AW, Chessell IP, Green RH, Whittington AR, Wall ID.
Bioorg Med Chem Lett (2009) 19 : 259 -263
PubMed 19010671 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 41 6.75 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307696 — — 1 8.60
CHEMBL465470 — — 1 7.90
CHEMBL465274 — — 1 7.50
CHEMBL464915 — — 1 7.40
CHEMBL465113 — — 1 7.40
CHEMBL520916 — — 1 7.30
CHEMBL464916 — — 1 7.30
CHEMBL466191 — — 1 7.30
CHEMBL481586 — — 1 7.20
CHEMBL464914 — — 1 7.20
CHEMBL467016 — — 1 7.20
CHEMBL513651 — — 1 7.10
CHEMBL517646 — — 1 7.10
CHEMBL464069 — — 1 7.10
CHEMBL512583 — — 1 7.00
CHEMBL464062 — — 1 7.00
CHEMBL450462 — — 1 6.90
CHEMBL465638 — — 1 6.80
CHEMBL465460 — — 1 6.80
CHEMBL482186 — — 1 6.80
CHEMBL480398 — — 1 6.70
CHEMBL480399 — — 1 6.70
CHEMBL465247 — — 1 6.70
CHEMBL465246 — — 1 6.60
CHEMBL463860 — — 1 6.60
CHEMBL512060 — — 1 6.60
CHEMBL520413 — — 1 6.60
CHEMBL467018 — — 1 6.40
CHEMBL506790 — — 1 6.40
CHEMBL465459 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307696 — EC50 = 2.512 nM 8.60
CHEMBL465470 — EC50 = 12.59 nM 7.90
CHEMBL465274 — EC50 = 31.62 nM 7.50
CHEMBL464915 — EC50 = 39.81 nM 7.40
CHEMBL465113 — EC50 = 39.81 nM 7.40
CHEMBL520916 — EC50 = 50.12 nM 7.30
CHEMBL464916 — EC50 = 50.12 nM 7.30
CHEMBL466191 — EC50 = 50.12 nM 7.30
CHEMBL481586 — EC50 = 63.1 nM 7.20
CHEMBL464914 — EC50 = 63.1 nM 7.20
CHEMBL467016 — EC50 = 63.1 nM 7.20
CHEMBL513651 — EC50 = 79.43 nM 7.10
CHEMBL464069 — EC50 = 79.43 nM 7.10
CHEMBL517646 — EC50 = 79.43 nM 7.10
CHEMBL464062 — EC50 = 100.0 nM 7.00
CHEMBL512583 — EC50 = 100.0 nM 7.00
CHEMBL450462 — EC50 = 125.89 nM 6.90
CHEMBL465638 — EC50 = 158.49 nM 6.80
CHEMBL465460 — EC50 = 158.49 nM 6.80
CHEMBL482186 — EC50 = 158.49 nM 6.80
CHEMBL480398 — EC50 = 199.53 nM 6.70
CHEMBL465247 — EC50 = 199.53 nM 6.70
CHEMBL480399 — EC50 = 199.53 nM 6.70
CHEMBL465246 — EC50 = 251.19 nM 6.60
CHEMBL463860 — EC50 = 251.19 nM 6.60
CHEMBL512060 — EC50 = 251.19 nM 6.60
CHEMBL520413 — EC50 = 251.19 nM 6.60
CHEMBL479628 — EC50 = 398.11 nM 6.40
CHEMBL518251 — EC50 = 398.11 nM 6.40
CHEMBL465459 — EC50 = 398.11 nM 6.40
CHEMBL506790 — EC50 = 398.11 nM 6.40
CHEMBL467018 — EC50 = 398.11 nM 6.40
CHEMBL464231 — EC50 = 501.19 nM 6.30
CHEMBL467017 — EC50 = 501.19 nM 6.30
CHEMBL480212 — EC50 = 794.33 nM 6.10
CHEMBL465245 — EC50 = 1000.0 nM 6.00
CHEMBL481398 — EC50 = 1258.93 nM 5.90
CHEMBL464070 — EC50 = 1584.89 nM 5.80
CHEMBL480214 — EC50 = 1584.89 nM 5.80
CHEMBL480213 — EC50 = 1995.26 nM 5.70
CHEMBL518619 — EC50 = 2511.89 nM 5.60