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Assay Detail

CHEMBL1837632

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

Binding
Displacement of [3H]-WIN 55,212-2 from human CB2 receptor expressed in human HEK293 cells after 90 mins by radioligand assay
ChEMBL ↗
57
Total Activities
50
Compounds Tested
2
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 2 (CHEMBL253) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Homology modeling in tandem with 3D-QSAR analyses: a computational approach to depict the agonist binding site of the human CB2 receptor.
Cichero E, Ligresti A, Allarà M, di Marzo V, Lazzati Z, D'Ursi P, Marabotti A, Milanesi L, Spallarossa A, Ranise A, Fossa P.
Eur J Med Chem (2011) 46 : 4489 -4505
PubMed 21835510 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 8.00 9.90
IC50 3 5.96 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411631 — — 1 9.90
CHEMBL271839 — — 1 9.83
CHEMBL411244 — — 1 9.39
CHEMBL269851 — — 1 9.29
CHEMBL271838 — — 1 9.19
CHEMBL270125 — — 1 9.16
CHEMBL270546 — — 1 9.05
CHEMBL1836186 — — 1 8.99
CHEMBL272876 — — 1 8.90
CHEMBL271810 — — 1 8.86
CHEMBL410677 — — 1 8.80
CHEMBL409265 — — 1 8.80
CHEMBL270987 — — 1 8.75
CHEMBL270955 — — 1 8.72
CHEMBL411674 — — 1 8.60
CHEMBL411937 — — 1 8.53
CHEMBL271527 — — 1 8.53
CHEMBL271565 — — 1 8.52
CHEMBL410676 — — 1 8.52
CHEMBL270082 — — 1 8.50
CHEMBL408964 — — 1 8.48
CHEMBL410441 — — 1 8.46
CHEMBL259253 — — 1 8.41
CHEMBL262865 — — 1 8.36
CHEMBL272882 — — 1 8.34
CHEMBL409669 — — 1 8.31
CHEMBL410655 — — 1 8.30
CHEMBL259463 — — 1 8.18
CHEMBL1836187 — — 2 8.12
CHEMBL409491 — — 1 8.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411631 — Ki = 0.1259 nM 9.90
CHEMBL271839 — Ki = 0.1479 nM 9.83
CHEMBL411244 — Ki = 0.4074 nM 9.39
CHEMBL269851 — Ki = 0.5129 nM 9.29
CHEMBL271838 — Ki = 0.6457 nM 9.19
CHEMBL270125 — Ki = 0.6918 nM 9.16
CHEMBL270546 — Ki = 0.8913 nM 9.05
CHEMBL1836186 — Ki = 1.023 nM 8.99
CHEMBL272876 — Ki = 1.259 nM 8.90
CHEMBL271810 — Ki = 1.38 nM 8.86
CHEMBL410677 — Ki = 1.585 nM 8.80
CHEMBL409265 — Ki = 1.585 nM 8.80
CHEMBL270987 — Ki = 1.778 nM 8.75
CHEMBL270955 — Ki = 1.905 nM 8.72
CHEMBL411674 — Ki = 2.512 nM 8.60
CHEMBL411937 — Ki = 2.951 nM 8.53
CHEMBL271527 — Ki = 2.951 nM 8.53
CHEMBL410676 — Ki = 3.02 nM 8.52
CHEMBL271565 — Ki = 3.02 nM 8.52
CHEMBL270082 — Ki = 3.162 nM 8.50
CHEMBL408964 — Ki = 3.311 nM 8.48
CHEMBL410441 — Ki = 3.467 nM 8.46
CHEMBL259253 — Ki = 3.89 nM 8.41
CHEMBL262865 — Ki = 4.365 nM 8.36
CHEMBL272882 — Ki = 4.571 nM 8.34
CHEMBL409669 — Ki = 4.898 nM 8.31
CHEMBL410655 — Ki = 5.012 nM 8.30
CHEMBL259463 — Ki = 6.607 nM 8.18
CHEMBL1836187 — Ki = 7.5 nM 8.12
CHEMBL1836187 — Ki = 7.586 nM 8.12
CHEMBL409491 — Ki = 8.511 nM 8.07
CHEMBL259462 — Ki = 9.333 nM 8.03
CHEMBL410842 — Ki = 9.333 nM 8.03
CHEMBL1836189 — Ki = 10.2 nM 7.99
CHEMBL1836189 — Ki = 10.23 nM 7.99
CHEMBL272176 — Ki = 21.38 nM 7.67
CHEMBL406399 — Ki = 25.7 nM 7.59
CHEMBL270910 — Ki = 26.92 nM 7.57
CHEMBL409647 — Ki = 30.2 nM 7.52
CHEMBL271814 — Ki = 32.36 nM 7.49
CHEMBL1836189 — IC50 = 40.1 nM 7.40
CHEMBL272189 — Ki = 58.88 nM 7.23
CHEMBL270968 — Ki = 61.66 nM 7.21
CHEMBL272658 — Ki = 72.44 nM 7.14
CHEMBL411673 — Ki = 91.2 nM 7.04
CHEMBL271837 — Ki = 109.65 nM 6.96
CHEMBL410313 — Ki = 112.2 nM 6.95
CHEMBL409231 — Ki = 234.42 nM 6.63
CHEMBL271805 — Ki = 239.88 nM 6.62
CHEMBL272659 — Ki = 263.03 nM 6.58