Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL895425

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

Binding
Binding affinity to human CB1 receptor
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 2: orally bioavailable compounds.
Kai H, Morioka Y, Tomida M, Takahashi T, Hattori M, Hanasaki K, Koike K, Chiba H, Shinohara S, Kanemasa T, Iwamoto Y, Takahashi K, Yamaguchi Y, Baba T, Yoshikawa T, Takenaka H.
Bioorg Med Chem Lett (2007) 17 : 3925 -3929
PubMed 17531479 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.72 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL231721 1 7.89
CHEMBL232116 1 7.82
CHEMBL465 DRONABINOL 4.0 1 7.77
CHEMBL232328 1 7.52
CHEMBL232336 1 7.36
CHEMBL233139 1 7.07
CHEMBL392842 1 7.02
CHEMBL231719 1 7.00
CHEMBL231932 1 6.97
CHEMBL232132 1 6.94
CHEMBL443842 1 6.91
CHEMBL393045 1 6.76
CHEMBL232538 1 6.61
CHEMBL234175 1 6.61
CHEMBL232130 1 6.45
CHEMBL232118 1 6.40
CHEMBL232131 1 6.38
CHEMBL231934 1 6.29
CHEMBL232929 1 6.27
CHEMBL231933 1 6.17
CHEMBL393188 1 6.15
CHEMBL398145 1 6.12
CHEMBL392841 1 5.90
CHEMBL232129 1 5.82
CHEMBL231935 1 5.76
CHEMBL391561 1 -
CHEMBL232730 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL231721 Ki = 13.0 nM 7.89
CHEMBL232116 Ki = 15.0 nM 7.82
CHEMBL465 DRONABINOL Ki = 17.0 nM 7.77
CHEMBL232328 Ki = 30.0 nM 7.52
CHEMBL232336 Ki = 44.0 nM 7.36
CHEMBL233139 Ki = 85.0 nM 7.07
CHEMBL392842 Ki = 95.0 nM 7.02
CHEMBL231719 Ki = 100.0 nM 7.00
CHEMBL231932 Ki = 108.0 nM 6.97
CHEMBL232132 Ki = 114.0 nM 6.94
CHEMBL443842 Ki = 122.0 nM 6.91
CHEMBL393045 Ki = 173.0 nM 6.76
CHEMBL232538 Ki = 246.0 nM 6.61
CHEMBL234175 Ki = 243.0 nM 6.61
CHEMBL232130 Ki = 358.0 nM 6.45
CHEMBL232118 Ki = 396.0 nM 6.40
CHEMBL232131 Ki = 418.0 nM 6.38
CHEMBL231934 Ki = 514.0 nM 6.29
CHEMBL232929 Ki = 541.0 nM 6.27
CHEMBL231933 Ki = 671.0 nM 6.17
CHEMBL393188 Ki = 711.0 nM 6.15
CHEMBL398145 Ki = 763.0 nM 6.12
CHEMBL392841 Ki = 1260.0 nM 5.90
CHEMBL232129 Ki = 1500.0 nM 5.82
CHEMBL231935 Ki = 1730.0 nM 5.76
CHEMBL391561 Ki > 5000.0 nM -
CHEMBL232730 Ki > 5000.0 nM -