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Assay Detail

CHEMBL616503

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

Binding
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor in rat cortical membranes
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Selective, centrally acting serotonin 5-HT2 antagonists. 2. Substituted 3-(4-fluorophenyl)-1H-indoles.
Andersen K, Perregaard J, Arnt J, Nielsen JB, Begtrup M.
J Med Chem (1992) 35 : 4823 -4831
PubMed 1336054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.50 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12713 SERTINDOLE 4.0 1 9.41
CHEMBL343034 1 8.82
CHEMBL331545 1 8.82
CHEMBL144767 1 8.80
CHEMBL422130 1 8.72
CHEMBL356799 1 8.66
CHEMBL144710 1 8.64
CHEMBL145712 1 8.57
CHEMBL143617 1 8.55
CHEMBL359031 1 8.51
CHEMBL144318 1 8.49
CHEMBL343444 1 8.47
CHEMBL144901 1 8.44
CHEMBL344335 1 8.35
CHEMBL144362 1 8.28
CHEMBL357019 1 8.24
CHEMBL141667 1 8.24
CHEMBL342730 1 8.10
CHEMBL355917 1 8.03
CHEMBL141721 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12713 SERTINDOLE IC50 = 0.39 nM 9.41
CHEMBL343034 IC50 = 1.5 nM 8.82
CHEMBL331545 IC50 = 1.5 nM 8.82
CHEMBL144767 IC50 = 1.6 nM 8.80
CHEMBL422130 IC50 = 1.9 nM 8.72
CHEMBL356799 IC50 = 2.2 nM 8.66
CHEMBL144710 IC50 = 2.3 nM 8.64
CHEMBL145712 IC50 = 2.7 nM 8.57
CHEMBL143617 IC50 = 2.8 nM 8.55
CHEMBL359031 IC50 = 3.1 nM 8.51
CHEMBL144318 IC50 = 3.2 nM 8.49
CHEMBL343444 IC50 = 3.4 nM 8.47
CHEMBL144901 IC50 = 3.6 nM 8.44
CHEMBL344335 IC50 = 4.5 nM 8.35
CHEMBL144362 IC50 = 5.3 nM 8.28
CHEMBL357019 IC50 = 5.7 nM 8.24
CHEMBL141667 IC50 = 5.8 nM 8.24
CHEMBL342730 IC50 = 7.9 nM 8.10
CHEMBL355917 IC50 = 9.3 nM 8.03
CHEMBL141721 IC50 = 15.0 nM 7.82