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Assay Detail

CHEMBL839446

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Binding
Binding affinity for 5-HT2A serotonin receptor
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 2A (CHEMBL322)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Beta-oxygenated analogues of the 5-HT2A serotonin receptor agonist 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane.
Glennon RA, Bondarev ML, Khorana N, Young R, May JA, Hellberg MR, McLaughlin MA, Sharif NA.
J Med Chem (2004) 47 : 6034 -6041
PubMed 15537358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 8.58 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6607 BROLAMFETAMINE 2.0 1 10.00
CHEMBL365958 1 9.52
CHEMBL188709 1 9.30
CHEMBL364718 1 9.10
CHEMBL191286 1 8.96
CHEMBL191051 1 8.70
CHEMBL191050 1 8.68
CHEMBL191420 1 8.22
CHEMBL365711 1 8.12
CHEMBL6737 1 8.04
CHEMBL364723 1 8.04
CHEMBL435297 1 8.00
CHEMBL363772 1 7.76
CHEMBL187715 1 7.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6607 BROLAMFETAMINE Ki = 0.1 nM 10.00
CHEMBL365958 Ki = 0.3 nM 9.52
CHEMBL188709 Ki = 0.5 nM 9.30
CHEMBL364718 Ki = 0.8 nM 9.10
CHEMBL191286 Ki = 1.1 nM 8.96
CHEMBL191051 Ki = 2.0 nM 8.70
CHEMBL191050 Ki = 2.1 nM 8.68
CHEMBL191420 Ki = 6.0 nM 8.22
CHEMBL365711 Ki = 7.6 nM 8.12
CHEMBL6737 Ki = 9.2 nM 8.04
CHEMBL364723 Ki = 9.2 nM 8.04
CHEMBL435297 Ki = 10.0 nM 8.00
CHEMBL363772 Ki = 17.4 nM 7.76
CHEMBL187715 Ki = 20.3 nM 7.69