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Assay Detail

CHEMBL855891

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

Binding
Displacement of (+/-)-[125I]DOI from human cloned 5HT2A receptor
7
Total Activities
7
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

5-hydroxytryptamine receptor 2A (CHEMBL224)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1-Aminomethylbenzocycloalkanes: conformationally restricted hallucinogenic phenethylamine analogues as functionally selective 5-HT2A receptor agonists.
McLean TH, Parrish JC, Braden MR, Marona-Lewicka D, Gallardo-Godoy A, Nichols DE.
J Med Chem (2006) 49 : 5794 -5803
PubMed 16970404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.05 9.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379637 1 9.46
CHEMBL292821 1 9.18
CHEMBL212197 1 9.14
CHEMBL215781 1 7.82
CHEMBL424890 1 7.28
CHEMBL213612 1 6.77
CHEMBL214379 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379637 Ki = 0.35 nM 9.46
CHEMBL292821 Ki = 0.66 nM 9.18
CHEMBL212197 Ki = 0.73 nM 9.14
CHEMBL215781 Ki = 15.0 nM 7.82
CHEMBL424890 Ki = 53.0 nM 7.28
CHEMBL213612 Ki = 170.0 nM 6.77
CHEMBL214379 Ki = 200.0 nM 6.70