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Assay Detail

CHEMBL1120213

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Binding
Binding affinity to human CB2 receptor
ChEMBL ↗
44
Total Activities
31
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 2 (CHEMBL253) ↗
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 44 5.42 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
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 6.24
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 6.10
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 5.89
CHEMBL1084039 — — 1 5.89
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 5.75
CHEMBL1094521 — — 2 5.65
CHEMBL1084602 — — 1 5.64
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 5.61
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 5.61
CHEMBL1083000 — — 1 5.54
CHEMBL1084556 — — 1 5.52
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 5.50
CHEMBL1086012 — — 1 5.48
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 5.47
CHEMBL1086013 — — 1 5.47
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 5.46
CHEMBL1085259 — — 1 5.42
CHEMBL1086493 — — 1 5.41
CHEMBL1086271 — — 1 5.39
CHEMBL1084848 — — 1 5.38
CHEMBL1086494 — — 1 5.38
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 5.32
CHEMBL1085732 — — 1 5.30
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 5.29
CHEMBL1084471 — — 1 5.20
CHEMBL1085260 — — 1 5.11
CHEMBL1084558 — — 1 5.10
CHEMBL1084557 — — 1 5.08
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 4.99
CHEMBL1084555 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
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 = 570.0 nM 6.24
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 = 801.0 nM 6.10
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 = 1280.0 nM 5.89
CHEMBL1084039 — IC50 = 1300.0 nM 5.89
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 = 1800.0 nM 5.75
CHEMBL1094521 — IC50 = 2260.0 nM 5.65
CHEMBL1084602 — IC50 = 2300.0 nM 5.64
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 = 2330.0 nM 5.63
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 = 2480.0 nM 5.61
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 = 2460.0 nM 5.61
CHEMBL1083000 — IC50 = 2920.0 nM 5.54
CHEMBL1084556 — IC50 = 3000.0 nM 5.52
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 = 3200.0 nM 5.50
CHEMBL1086012 — IC50 = 3300.0 nM 5.48
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 = 3390.0 nM 5.47
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 = 3400.0 nM 5.47
CHEMBL1086013 — IC50 = 3400.0 nM 5.47
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 = 3450.0 nM 5.46
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 = 3600.0 nM 5.44
CHEMBL1085259 — IC50 = 3790.0 nM 5.42
CHEMBL1086493 — IC50 = 3900.0 nM 5.41
CHEMBL1086271 — IC50 = 4100.0 nM 5.39
CHEMBL1086494 — IC50 = 4200.0 nM 5.38
CHEMBL1084848 — IC50 = 4200.0 nM 5.38
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 = 4780.0 nM 5.32
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 = 4750.0 nM 5.32
CHEMBL1085732 — IC50 = 4950.0 nM 5.30
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 = 5150.0 nM 5.29
CHEMBL1094521 — IC50 = 5310.0 nM 5.28
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 = 5400.0 nM 5.27
CHEMBL1084471 — IC50 = 6300.0 nM 5.20
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 = 6610.0 nM 5.18
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 = 7450.0 nM 5.13
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 = 7600.0 nM 5.12
CHEMBL1085260 — IC50 = 7760.0 nM 5.11
CHEMBL1084558 — IC50 = 8000.0 nM 5.10
CHEMBL1084557 — IC50 = 8300.0 nM 5.08
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 = 10000.0 nM 5.00
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 = 10130.0 nM 4.99
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 = 12000.0 nM 4.92
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 > 2000.0 nM -
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 > 2000.0 nM -
CHEMBL1084555 — IC50 > 2000.0 nM -
CHEMBL1086492 — IC50 > 2000.0 nM -