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Assay Detail

CHEMBL2156596

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

Binding
Displacement of 3[H]ligand from recombinant human CB1 receptor
44
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
Chorvat RJ, Berbaum J, Seriacki K, McElroy JF.
Bioorg Med Chem Lett (2012) 22 : 6173 -6180
PubMed 22959249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.74 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2153670 1 9.30
CHEMBL2153672 1 8.70
CHEMBL2153669 1 8.70
CHEMBL2153763 1 8.40
CHEMBL2153772 1 8.15
CHEMBL2153674 1 8.15
CHEMBL2153767 1 8.10
CHEMBL2153673 1 8.08
CHEMBL2153666 1 8.07
CHEMBL2153765 1 8.00
CHEMBL2153757 1 7.89
CHEMBL2153662 3 7.75
CHEMBL2153665 1 7.70
CHEMBL158784 RAC-IBIPINABANT 1 7.66
CHEMBL2153764 1 7.60
CHEMBL2153664 1 7.58
CHEMBL2153766 1 7.57
CHEMBL2153663 1 7.50
CHEMBL2153758 1 7.18
CHEMBL2153761 1 7.16
CHEMBL2153759 1 7.00
CHEMBL2153771 1 7.00
CHEMBL158138 1 7.00
CHEMBL2153648 1 7.00
CHEMBL2153655 1 6.52
CHEMBL2153654 1 -
CHEMBL2153649 1 -
CHEMBL2153770 1 -
CHEMBL2153769 1 -
CHEMBL2153768 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2153670 IC50 = 0.5 nM 9.30
CHEMBL2153672 IC50 = 2.0 nM 8.70
CHEMBL2153669 IC50 = 2.0 nM 8.70
CHEMBL2153763 IC50 = 4.0 nM 8.40
CHEMBL2153772 IC50 = 7.0 nM 8.15
CHEMBL2153674 IC50 = 7.0 nM 8.15
CHEMBL2153767 IC50 = 8.0 nM 8.10
CHEMBL2153673 IC50 = 8.3 nM 8.08
CHEMBL2153666 IC50 = 8.5 nM 8.07
CHEMBL2153765 IC50 = 10.0 nM 8.00
CHEMBL2153757 IC50 = 13.0 nM 7.89
CHEMBL2153662 IC50 = 18.0 nM 7.75
CHEMBL2153665 IC50 = 20.0 nM 7.70
CHEMBL158784 RAC-IBIPINABANT IC50 = 22.0 nM 7.66
CHEMBL2153764 IC50 = 25.0 nM 7.60
CHEMBL2153664 IC50 = 26.0 nM 7.58
CHEMBL2153766 IC50 = 27.0 nM 7.57
CHEMBL2153662 IC50 = 32.0 nM 7.50
CHEMBL2153663 IC50 = 32.0 nM 7.50
CHEMBL2153758 IC50 = 66.0 nM 7.18
CHEMBL2153761 IC50 = 70.0 nM 7.16
CHEMBL2153759 IC50 = 100.0 nM 7.00
CHEMBL2153648 IC50 = 100.0 nM 7.00
CHEMBL2153771 IC50 = 100.0 nM 7.00
CHEMBL158138 IC50 = 100.0 nM 7.00
CHEMBL2153655 IC50 = 300.0 nM 6.52
CHEMBL2153662 IC50 > 1000.0 nM -
CHEMBL2153661 IC50 > 1000.0 nM -
CHEMBL2153659 IC50 > 1000.0 nM -
CHEMBL2153667 IC50 > 100.0 nM -
CHEMBL2153651 IC50 > 5000.0 nM -
CHEMBL2153650 IC50 > 5000.0 nM -
CHEMBL2153671 IC50 > 1000.0 nM -
CHEMBL2153649 IC50 > 5000.0 nM -
CHEMBL2153657 IC50 > 1000.0 nM -
CHEMBL2153675 IC50 > 100.0 nM -
CHEMBL2153760 IC50 > 100.0 nM -
CHEMBL2153762 IC50 > 500.0 nM -
CHEMBL2153652 IC50 > 5000.0 nM -
CHEMBL2153654 IC50 > 1000.0 nM -
CHEMBL2153653 IC50 > 5000.0 nM -
CHEMBL2153768 IC50 > 100.0 nM -
CHEMBL2153769 IC50 > 100.0 nM -
CHEMBL2153770 IC50 > 100.0 nM -