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Assay Detail

CHEMBL863412

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

Functional
Activity against 5HT2A mediated intracellular calcium mobilization by FLIPR in rat vascular smooth muscle cells
26
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

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
EC50 13 7.11 7.70
Emax 13 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134519 2 7.70
CHEMBL371300 2 7.37
CHEMBL31115 2 7.32
CHEMBL199775 2 7.27
CHEMBL39 SEROTONIN 3.0 2 7.24
CHEMBL275854 2 7.24
CHEMBL197653 2 7.24
CHEMBL373245 2 7.22
CHEMBL199385 2 7.13
CHEMBL200104 2 7.09
CHEMBL201132 2 6.69
CHEMBL437314 2 6.63
CHEMBL7257 MEBUFOTENIN 2.0 2 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134519 EC50 = 19.8 nM 7.70
CHEMBL371300 EC50 = 42.7 nM 7.37
CHEMBL31115 EC50 = 47.5 nM 7.32
CHEMBL199775 EC50 = 54.0 nM 7.27
CHEMBL275854 EC50 = 58.0 nM 7.24
CHEMBL39 SEROTONIN EC50 = 57.9 nM 7.24
CHEMBL197653 EC50 = 58.1 nM 7.24
CHEMBL373245 EC50 = 59.7 nM 7.22
CHEMBL199385 EC50 = 74.4 nM 7.13
CHEMBL200104 EC50 = 81.3 nM 7.09
CHEMBL201132 EC50 = 204.0 nM 6.69
CHEMBL437314 EC50 = 236.0 nM 6.63
CHEMBL7257 MEBUFOTENIN EC50 = 462.0 nM 6.33
CHEMBL371300 Emax = 81.0 % -
CHEMBL134519 Emax = 35.0 % -
CHEMBL199385 Emax = 75.0 % -
CHEMBL275854 Emax = 96.0 % -
CHEMBL39 SEROTONIN Emax = 99.0 % -
CHEMBL437314 Emax = 61.0 % -
CHEMBL199775 Emax = 90.0 % -
CHEMBL7257 MEBUFOTENIN Emax = 70.0 % -
CHEMBL201132 Emax = 73.0 % -
CHEMBL373245 Emax = 87.0 % -
CHEMBL197653 Emax = 80.0 % -
CHEMBL31115 Emax = 96.0 % -
CHEMBL200104 Emax = 89.0 % -