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Assay Detail

CHEMBL621533

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

Binding
Binding affinity at cloned rat 5-hydroxytryptamine 2A receptor using [3H]DOB as radioligand
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Enantiospecific synthesis and pharmacological evaluation of a series of super-potent, conformationally restricted 5-HT(2A/2C) receptor agonists.
Chambers JJ, Kurrasch-Orbaugh DM, Parker MA, Nichols DE.
J Med Chem (2001) 44 : 1003 -1010
PubMed 11300881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.41 9.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7132 1 9.54
CHEMBL6706 1 9.51
CHEMBL6907 1 9.49
CHEMBL263083 1 9.17
CHEMBL6452 1 9.15
CHEMBL6710 1 8.92
CHEMBL6871 1 8.82
CHEMBL268542 1 8.70
CHEMBL6607 BROLAMFETAMINE 2.0 1 8.66
CHEMBL6620 1 8.66
CHEMBL263078 1 8.59
CHEMBL6838 1 7.42
CHEMBL268072 1 7.26
CHEMBL268587 1 6.64
CHEMBL6737 1 5.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7132 Ki = 0.29 nM 9.54
CHEMBL6706 Ki = 0.31 nM 9.51
CHEMBL6907 Ki = 0.32 nM 9.49
CHEMBL263083 Ki = 0.68 nM 9.17
CHEMBL6452 Ki = 0.7 nM 9.15
CHEMBL6710 Ki = 1.2 nM 8.92
CHEMBL6871 Ki = 1.5 nM 8.82
CHEMBL268542 Ki = 2.0 nM 8.70
CHEMBL6607 BROLAMFETAMINE Ki = 2.2 nM 8.66
CHEMBL6620 Ki = 2.2 nM 8.66
CHEMBL263078 Ki = 2.6 nM 8.59
CHEMBL6838 Ki = 37.9 nM 7.42
CHEMBL268072 Ki = 54.4 nM 7.26
CHEMBL268587 Ki = 227.0 nM 6.64
CHEMBL6737 Ki = 2340.0 nM 5.63