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Assay Detail

CHEMBL1070562

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Functional
Agonist activity at human CB2 receptor
36
Total Activities
36
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

Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.
Gleave RJ, Beswick PJ, Brown AJ, Giblin GM, Goldsmith P, Haslam CP, Mitchell WL, Nicholson NH, Page LW, Patel S, Roomans S, Slingsby BP, Swarbrick ME.
Bioorg Med Chem Lett (2010) 20 : 465 -468
PubMed 20005703 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 6.88 9.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL594530 1 9.20
CHEMBL594529 1 8.90
CHEMBL594281 1 8.20
CHEMBL611620 1 8.00
CHEMBL594837 1 7.80
CHEMBL595238 1 7.60
CHEMBL608403 1 7.40
CHEMBL594055 1 7.40
CHEMBL610914 1 7.40
CHEMBL595221 1 7.30
CHEMBL608992 1 7.30
CHEMBL577347 1 7.10
CHEMBL593582 1 7.10
CHEMBL594977 1 7.10
CHEMBL594056 1 7.00
CHEMBL608702 1 6.80
CHEMBL610489 1 6.80
CHEMBL593581 1 6.70
CHEMBL594835 1 6.70
CHEMBL594531 1 6.70
CHEMBL595244 1 6.60
CHEMBL596569 1 6.40
CHEMBL608700 1 6.20
CHEMBL608698 1 6.20
CHEMBL611321 1 6.00
CHEMBL593130 1 5.90
CHEMBL593131 1 5.90
CHEMBL593835 1 5.80
CHEMBL596355 1 5.70
CHEMBL596590 1 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL594530 EC50 = 0.631 nM 9.20
CHEMBL594529 EC50 = 1.259 nM 8.90
CHEMBL594281 EC50 = 6.31 nM 8.20
CHEMBL611620 EC50 = 10.0 nM 8.00
CHEMBL594837 EC50 = 15.85 nM 7.80
CHEMBL595238 EC50 = 25.12 nM 7.60
CHEMBL608403 EC50 = 39.81 nM 7.40
CHEMBL594055 EC50 = 39.81 nM 7.40
CHEMBL610914 EC50 = 39.81 nM 7.40
CHEMBL608992 EC50 = 50.12 nM 7.30
CHEMBL595221 EC50 = 50.12 nM 7.30
CHEMBL577347 EC50 = 79.43 nM 7.10
CHEMBL593582 EC50 = 79.43 nM 7.10
CHEMBL594977 EC50 = 79.43 nM 7.10
CHEMBL594056 EC50 = 100.0 nM 7.00
CHEMBL608702 EC50 = 158.49 nM 6.80
CHEMBL610489 EC50 = 158.49 nM 6.80
CHEMBL594531 EC50 = 199.53 nM 6.70
CHEMBL594835 EC50 = 199.53 nM 6.70
CHEMBL593581 EC50 = 199.53 nM 6.70
CHEMBL595244 EC50 = 251.19 nM 6.60
CHEMBL596569 EC50 = 398.11 nM 6.40
CHEMBL608700 EC50 = 630.96 nM 6.20
CHEMBL608698 EC50 = 630.96 nM 6.20
CHEMBL611321 EC50 = 1000.0 nM 6.00
CHEMBL593130 EC50 = 1258.93 nM 5.90
CHEMBL593131 EC50 = 1258.93 nM 5.90
CHEMBL593835 EC50 = 1584.89 nM 5.80
CHEMBL596355 EC50 = 1995.26 nM 5.70
CHEMBL596590 EC50 = 7943.28 nM 5.10
CHEMBL611612 EC50 = 12589.25 nM 4.90
CHEMBL595450 EC50 > 31622.78 nM -
CHEMBL596155 EC50 > 31622.78 nM -
CHEMBL595008 EC50 > 31622.78 nM -
CHEMBL595243 EC50 > 31622.78 nM -
CHEMBL593834 EC50 > 31622.78 nM -