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Assay Detail

CHEMBL617442

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

Binding
Displacement of [3H]ketanserin from 5-hydroxytryptamine 2 receptor of rat cortex
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis and evaluation of phenyl- and benzoylpiperazines as potential serotonergic agents.
Lyon RA, Titeler M, McKenney JD, Magee PS, Glennon RA.
J Med Chem (1986) 29 : 630 -634
PubMed 3701781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 4.92 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274866 1 6.80
CHEMBL348140 1 5.61
CHEMBL9666 1 5.46
CHEMBL160344 1 5.33
CHEMBL156216 1 5.07
CHEMBL156974 1 5.07
CHEMBL266250 1 4.76
CHEMBL349562 1 4.31
CHEMBL160911 1 4.25
CHEMBL348139 1 4.19
CHEMBL160121 1 4.12
CHEMBL158612 1 4.03
CHEMBL158884 1 -
CHEMBL160860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274866 Ki = 160.0 nM 6.80
CHEMBL348140 Ki = 2430.0 nM 5.61
CHEMBL9666 Ki = 3500.0 nM 5.46
CHEMBL160344 Ki = 4710.0 nM 5.33
CHEMBL156216 Ki = 8430.0 nM 5.07
CHEMBL156974 Ki = 8480.0 nM 5.07
CHEMBL266250 Ki = 17200.0 nM 4.76
CHEMBL349562 Ki = 49000.0 nM 4.31
CHEMBL160911 Ki = 55600.0 nM 4.25
CHEMBL348139 Ki = 64300.0 nM 4.19
CHEMBL160121 Ki = 76500.0 nM 4.12
CHEMBL158612 Ki = 93000.0 nM 4.03
CHEMBL158884 Ki > 100000.0 nM -
CHEMBL160860 Ki > 100000.0 nM -