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Assay Detail

CHEMBL904754

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Functional
Agonist activity at human recombinant CB2 receptor expressed in Saccharomyces cerevisiae cells
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain.
Giblin GM, O'Shaughnessy CT, Naylor A, Mitchell WL, Eatherton AJ, Slingsby BP, Rawlings DA, Goldsmith P, Brown AJ, Haslam CP, Clayton NM, Wilson AW, Chessell IP, Wittington AR, Green R.
J Med Chem (2007) 50 : 2597 -2600
PubMed 17477516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 46 6.66 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307696 — — 1 8.52
CHEMBL225412 — — 1 7.48
CHEMBL227899 — — 1 7.40
CHEMBL389408 — — 1 7.31
CHEMBL226385 — — 1 7.30
CHEMBL375955 — — 1 7.22
CHEMBL389908 — — 1 7.20
CHEMBL225411 GW842166X 2.0 1 7.20
CHEMBL226067 — — 1 7.10
CHEMBL226386 — — 1 7.10
CHEMBL227947 — — 1 7.10
CHEMBL225357 — — 1 7.10
CHEMBL425126 — — 1 7.00
CHEMBL225413 — — 1 6.90
CHEMBL390526 — — 1 6.90
CHEMBL225464 — — 1 6.90
CHEMBL387620 — — 1 6.90
CHEMBL389281 — — 1 6.90
CHEMBL226419 — — 1 6.80
CHEMBL387654 — — 1 6.70
CHEMBL225465 — — 1 6.70
CHEMBL438836 — — 1 6.67
CHEMBL226018 — — 1 6.66
CHEMBL226260 — — 1 6.64
CHEMBL226154 — — 1 6.61
CHEMBL389280 — — 1 6.60
CHEMBL226209 — — 1 6.51
CHEMBL225466 — — 1 6.40
CHEMBL375703 — — 1 6.40
CHEMBL425128 — — 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307696 — EC50 = 3.0 nM 8.52
CHEMBL225412 — EC50 = 33.0 nM 7.48
CHEMBL227899 — EC50 = 40.0 nM 7.40
CHEMBL389408 — EC50 = 49.0 nM 7.31
CHEMBL226385 — EC50 = 50.0 nM 7.30
CHEMBL375955 — EC50 = 60.0 nM 7.22
CHEMBL389908 — EC50 = 63.0 nM 7.20
CHEMBL225411 GW842166X EC50 = 63.0 nM 7.20
CHEMBL226067 — EC50 = 80.0 nM 7.10
CHEMBL226386 — EC50 = 80.0 nM 7.10
CHEMBL227947 — EC50 = 80.0 nM 7.10
CHEMBL225357 — EC50 = 80.0 nM 7.10
CHEMBL425126 — EC50 = 100.0 nM 7.00
CHEMBL389281 — EC50 = 126.0 nM 6.90
CHEMBL390526 — EC50 = 125.0 nM 6.90
CHEMBL225464 — EC50 = 125.0 nM 6.90
CHEMBL225413 — EC50 = 125.0 nM 6.90
CHEMBL387620 — EC50 = 125.0 nM 6.90
CHEMBL226419 — EC50 = 158.0 nM 6.80
CHEMBL387654 — EC50 = 200.0 nM 6.70
CHEMBL225465 — EC50 = 200.0 nM 6.70
CHEMBL438836 — EC50 = 214.0 nM 6.67
CHEMBL226018 — EC50 = 220.0 nM 6.66
CHEMBL226260 — EC50 = 230.0 nM 6.64
CHEMBL226154 — EC50 = 245.0 nM 6.61
CHEMBL389280 — EC50 = 250.0 nM 6.60
CHEMBL226209 — EC50 = 310.0 nM 6.51
CHEMBL225466 — EC50 = 400.0 nM 6.40
CHEMBL375703 — EC50 = 400.0 nM 6.40
CHEMBL425128 — EC50 = 400.0 nM 6.40
CHEMBL226208 — EC50 = 400.0 nM 6.40
CHEMBL388118 — EC50 = 400.0 nM 6.40
CHEMBL226204 — EC50 = 455.0 nM 6.34
CHEMBL226316 — EC50 = 465.0 nM 6.33
CHEMBL226365 — EC50 = 630.0 nM 6.20
CHEMBL225518 — EC50 = 630.0 nM 6.20
CHEMBL389182 — EC50 = 630.0 nM 6.20
CHEMBL226366 — EC50 = 630.0 nM 6.20
CHEMBL427271 — EC50 = 1580.0 nM 5.80
CHEMBL226384 — EC50 = 5000.0 nM 5.30
CHEMBL376383 — EC50 = 10000.0 nM 5.00
CHEMBL388117 — EC50 = 25000.0 nM 4.60
CHEMBL226368 — EC50 > 25000.0 nM -
CHEMBL226367 — EC50 > 25000.0 nM -
CHEMBL226215 — EC50 > 25000.0 nM -
CHEMBL226317 — EC50 > 25000.0 nM -