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Assay Detail

CHEMBL872918

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 cortical membrane homogenates
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

5-HT1 and 5-HT2 binding characteristics of some quipazine analogues.
Glennon RA, Slusher RM, Lyon RA, Titeler M, McKenney JD.
J Med Chem (1986) 29 : 2375 -2380
PubMed 3783595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.49 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277120 1 7.75
CHEMBL278509 1 7.16
CHEMBL18772 QUIPAZINE 2.0 1 6.64
CHEMBL80691 1 6.51
CHEMBL80775 1 5.92
CHEMBL9434 PHENYLPIPERAZINE 1 5.68
CHEMBL30294 1 4.96
CHEMBL77072 1 4.46
CHEMBL78878 1 4.30
CHEMBL80988 1 4.30
CHEMBL75983 1 4.15
CHEMBL61236 1 4.10
CHEMBL76495 1 -
CHEMBL80298 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277120 Ki = 18.0 nM 7.75
CHEMBL278509 Ki = 70.0 nM 7.16
CHEMBL18772 QUIPAZINE Ki = 230.0 nM 6.64
CHEMBL80691 Ki = 310.0 nM 6.51
CHEMBL80775 Ki = 1200.0 nM 5.92
CHEMBL9434 PHENYLPIPERAZINE Ki = 2100.0 nM 5.68
CHEMBL30294 Ki = 11100.0 nM 4.96
CHEMBL77072 Ki = 35000.0 nM 4.46
CHEMBL78878 Ki = 50000.0 nM 4.30
CHEMBL80988 Ki = 50000.0 nM 4.30
CHEMBL75983 Ki = 71000.0 nM 4.15
CHEMBL61236 Ki = 79000.0 nM 4.10
CHEMBL76495 Ki > 150000.0 nM -
CHEMBL80298 Ki > 300000.0 nM -