Assay Detail

CHEMBL1120212

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Binding

Binding affinity to human CB1 receptor

ChEMBL ↗

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Target

Cannabinoid receptor 1 (CHEMBL218) ↗

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Cannabinoid receptor 1 (CHEMBL218) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Cannabinoid receptor 1

CHEMBL218

Anchored from Assay target.

Protein identity Cannabinoid receptor 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

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

Dihydro-pyrano[2,3-b]pyridines and tetrahydro-1,8-naphthyridines as CB1 receptor inverse agonists: synthesis, SAR and biological evaluation.

Madsen-Duggan CB, Debenham JS, Walsh TF, Yan L, Huo P, Wang J, Tong X, Lao J, Fong TM, Xiao JC, Huang CR, Shen CP, Stribling DS, Shearman LP, Strack AM, Goulet MT, Hale JJ.
Bioorg Med Chem Lett (2010) 20 : 3750 -3754
PubMed 20483606 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	47	7.93	9.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1083619	(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	2	9.70
CHEMBL220360	TARANABANT	3.0	1	9.52
CHEMBL1086494	—	—	1	9.52
CHEMBL1084820	(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	2	9.40
CHEMBL1085566	N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX)	—	2	9.15
CHEMBL1086493	—	—	1	8.89
CHEMBL1083025	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	2	8.77
CHEMBL1083014	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	—	2	8.77
CHEMBL1084555	—	—	1	8.77
CHEMBL1082650	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	—	2	8.74
CHEMBL1086013	—	—	1	8.72
CHEMBL1083016	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX)	—	2	8.68
CHEMBL1083646	(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	—	2	8.52
CHEMBL1086012	—	—	1	8.49
CHEMBL1082330	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	—	2	8.43
CHEMBL1084038	—	—	1	8.37
CHEMBL1094521	—	—	2	8.32
CHEMBL1084558	—	—	1	8.31
CHEMBL204232	NAPHTHYRIDINONE	—	1	8.12
CHEMBL1084557	—	—	1	8.09
CHEMBL1082321	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	—	2	7.85
CHEMBL1084848	—	—	1	7.82
CHEMBL1086271	—	—	1	7.82
CHEMBL1085259	—	—	1	7.72
CHEMBL1084471	—	—	1	7.68
CHEMBL1084556	—	—	1	7.64
CHEMBL1085261	N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	—	2	7.34
CHEMBL1084039	—	—	1	7.33
CHEMBL1083000	—	—	1	7.10
CHEMBL1082305	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	—	2	7.01

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1083619	(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	0.2	nM	9.70
CHEMBL220360	TARANABANT	IC50	=	0.3	nM	9.52
CHEMBL1086494	—	IC50	=	0.3	nM	9.52
CHEMBL1084820	(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	0.4	nM	9.40
CHEMBL1085566	N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	0.7	nM	9.15
CHEMBL1086493	—	IC50	=	1.3	nM	8.89
CHEMBL1083025	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	1.7	nM	8.77
CHEMBL1083014	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	IC50	=	1.7	nM	8.77
CHEMBL1084555	—	IC50	=	1.7	nM	8.77
CHEMBL1082650	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	1.8	nM	8.74
CHEMBL1086013	—	IC50	=	1.9	nM	8.72
CHEMBL1083619	(2R)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	2.0	nM	8.70
CHEMBL1083016	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	2.1	nM	8.68
CHEMBL1083646	(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	3.0	nM	8.52
CHEMBL1086012	—	IC50	=	3.2	nM	8.49
CHEMBL1082330	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	3.7	nM	8.43
CHEMBL1084038	—	IC50	=	4.3	nM	8.37
CHEMBL1094521	—	IC50	=	4.8	nM	8.32
CHEMBL1084558	—	IC50	=	4.9	nM	8.31
CHEMBL204232	NAPHTHYRIDINONE	IC50	=	7.5	nM	8.12
CHEMBL1084557	—	IC50	=	8.2	nM	8.09
CHEMBL1084820	(2S)-N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	13.0	nM	7.89
CHEMBL1082321	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	14.0	nM	7.85
CHEMBL1083025	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	14.0	nM	7.85
CHEMBL1084848	—	IC50	=	15.0	nM	7.82
CHEMBL1086271	—	IC50	=	15.0	nM	7.82
CHEMBL1083646	(2R)-N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	16.0	nM	7.80
CHEMBL1085566	N-(7'-(2-CHLOROPHENYL)-6'-(4-CHLOROPHENYL)-3',4'-DIHYDROSPIRO[CYCLOHEXANE-1,2'-PYRANO[2,3-B]PYRIDINE]-4'-YL)-2-HYDROXY-2-METHYLPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	18.0	nM	7.75
CHEMBL1085259	—	IC50	=	19.0	nM	7.72
CHEMBL1084471	—	IC50	=	21.0	nM	7.68
CHEMBL1084556	—	IC50	=	23.0	nM	7.64
CHEMBL1082650	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-((R)-1-HYDROXYETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	29.0	nM	7.54
CHEMBL1083016	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-3-HYDROXY-2,2-DIMETHYLPROPANAMIDE (ENANTIOMERIC MIX)	IC50	=	34.0	nM	7.47
CHEMBL1085261	N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	IC50	=	46.0	nM	7.34
CHEMBL1084039	—	IC50	=	47.0	nM	7.33
CHEMBL1082330	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	76.0	nM	7.12
CHEMBL1094521	—	IC50	=	78.0	nM	7.11
CHEMBL1083000	—	IC50	=	80.0	nM	7.10
CHEMBL1082305	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	97.0	nM	7.01
CHEMBL1085260	—	IC50	=	110.0	nM	6.96
CHEMBL1084602	—	IC50	=	120.0	nM	6.92
CHEMBL1085732	—	IC50	=	130.0	nM	6.89
CHEMBL1082321	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(1-HYDROXY-2-METHYLPROPAN-2-YL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	150.0	nM	6.82
CHEMBL1082305	6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX)	IC50	=	220.0	nM	6.66
CHEMBL1085261	N-(7-(2-CHLOROPHENYL)-6-(4-CHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	IC50	=	360.0	nM	6.44
CHEMBL1083014	N-(6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-2,2-DIMETHYL-3,4-DIHYDRO-2H-PYRANO[2,3-B]PYRIDIN-4-YL)-2-HYDROXYACETAMIDE (ENANTIOMERIC MIX)	IC50	=	670.0	nM	6.17
CHEMBL1086492	—	IC50	=	790.0	nM	6.10