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Assay Detail

CHEMBL3383058

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

Binding
Displacement of [3H]CP-55,940 from human recombinant CB1R expressed in HEK-293 cells after 90 mins by liquid scintillation counting
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

CB2-selective cannabinoid receptor ligands: synthesis, pharmacological evaluation, and molecular modeling investigation of 1,8-Naphthyridin-2(1H)-one-3-carboxamides.
Lucchesi V, Hurst DP, Shore DM, Bertini S, Ehrmann BM, Allarà M, Lawrence L, Ligresti A, Minutolo F, Saccomanni G, Sharir H, Macchia M, Di Marzo V, Abood ME, Reggio PH, Manera C.
J Med Chem (2014) 57 : 8777 -8791
PubMed 25272206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 6.42 7.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3353437 1 7.65
CHEMBL3353452 1 7.49
CHEMBL3353438 1 7.45
CHEMBL3353454 1 7.28
CHEMBL3353453 1 7.18
CHEMBL3353439 1 7.02
CHEMBL3353441 1 6.92
CHEMBL3353440 1 6.78
CHEMBL466651 1 6.70
CHEMBL3353445 1 6.37
CHEMBL381689 SR-144528 1 6.36
CHEMBL3353446 1 6.33
CHEMBL371214 1 6.17
CHEMBL3353442 1 6.12
CHEMBL3353424 1 6.04
CHEMBL466223 1 6.00
CHEMBL3353436 1 6.00
CHEMBL3353423 1 5.64
CHEMBL3353443 1 5.49
CHEMBL3353444 1 5.48
CHEMBL3353448 1 5.46
CHEMBL3353450 1 5.39
CHEMBL3353449 1 -
CHEMBL3353425 1 -
CHEMBL3353426 1 -
CHEMBL3353427 1 -
CHEMBL3353428 1 -
CHEMBL3353429 1 -
CHEMBL3353430 1 -
CHEMBL3353431 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3353437 Ki = 22.59 nM 7.65
CHEMBL3353452 Ki = 32.7 nM 7.49
CHEMBL3353438 Ki = 35.67 nM 7.45
CHEMBL3353454 Ki = 52.9 nM 7.28
CHEMBL3353453 Ki = 66.7 nM 7.18
CHEMBL3353439 Ki = 96.1 nM 7.02
CHEMBL3353441 Ki = 121.0 nM 6.92
CHEMBL3353440 Ki = 166.0 nM 6.78
CHEMBL466651 Ki = 200.0 nM 6.70
CHEMBL3353445 Ki = 430.0 nM 6.37
CHEMBL381689 SR-144528 Ki = 437.0 nM 6.36
CHEMBL3353446 Ki = 472.0 nM 6.33
CHEMBL371214 Ki = 677.0 nM 6.17
CHEMBL3353442 Ki = 750.0 nM 6.12
CHEMBL3353424 Ki = 908.0 nM 6.04
CHEMBL466223 Ki = 1000.0 nM 6.00
CHEMBL3353436 Ki = 1011.0 nM 6.00
CHEMBL3353423 Ki = 2314.0 nM 5.64
CHEMBL3353443 Ki = 3262.0 nM 5.49
CHEMBL3353444 Ki = 3280.0 nM 5.48
CHEMBL3353448 Ki = 3444.0 nM 5.46
CHEMBL3353450 Ki = 4056.0 nM 5.39
CHEMBL3353447 Ki > 10000.0 nM -
CHEMBL3353451 Ki > 10000.0 nM -
CHEMBL3353435 Ki > 10000.0 nM -
CHEMBL3353434 Ki > 10000.0 nM -
CHEMBL3353433 Ki > 10000.0 nM -
CHEMBL3353432 Ki > 10000.0 nM -
CHEMBL3353431 Ki > 10000.0 nM -
CHEMBL3353430 Ki > 10000.0 nM -
CHEMBL3353429 Ki > 10000.0 nM -
CHEMBL3353428 Ki > 10000.0 nM -
CHEMBL3353427 Ki > 10000.0 nM -
CHEMBL3353426 Ki > 10000.0 nM -
CHEMBL3353425 Ki > 10000.0 nM -
CHEMBL3353449 Ki > 10000.0 nM -