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Assay Detail

CHEMBL863411

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

Binding
Inhibition of [125I]DOI binding to 5HT2A receptor in rat cerebral cortex
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-((S)-2-aminopropyl)-1H-indazol-6-ol: a potent peripherally acting 5-HT2 receptor agonist with ocular hypotensive activity.
May JA, Dantanarayana AP, Zinke PW, McLaughlin MA, Sharif NA.
J Med Chem (2006) 49 : 318 -328
PubMed 16392816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.92 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134519 1 9.68
CHEMBL373245 1 9.27
CHEMBL371300 1 9.24
CHEMBL197653 1 9.14
CHEMBL200104 1 9.13
CHEMBL199385 1 9.11
CHEMBL39 SEROTONIN 3.0 1 9.03
CHEMBL201132 1 8.78
CHEMBL199775 1 8.72
CHEMBL31115 1 8.70
CHEMBL437314 1 8.68
CHEMBL275854 1 8.46
CHEMBL7257 MEBUFOTENIN 2.0 1 8.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134519 IC50 = 0.21 nM 9.68
CHEMBL373245 IC50 = 0.54 nM 9.27
CHEMBL371300 IC50 = 0.58 nM 9.24
CHEMBL197653 IC50 = 0.73 nM 9.14
CHEMBL200104 IC50 = 0.74 nM 9.13
CHEMBL199385 IC50 = 0.77 nM 9.11
CHEMBL39 SEROTONIN IC50 = 0.94 nM 9.03
CHEMBL201132 IC50 = 1.68 nM 8.78
CHEMBL199775 IC50 = 1.91 nM 8.72
CHEMBL31115 IC50 = 2.0 nM 8.70
CHEMBL437314 IC50 = 2.08 nM 8.68
CHEMBL275854 IC50 = 3.5 nM 8.46
CHEMBL7257 MEBUFOTENIN IC50 = 9.53 nM 8.02