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Assay Detail

CHEMBL617681

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

Binding
The ability to inhibit [3H]ketanserin binding to 5-hydroxytryptamine 2 receptor in rat whole brain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.
Flynn DL, Zabrowski DL, Becker DP, Nosal R, Villamil CI, Gullikson GW, Moummi C, Yang DC.
J Med Chem (1992) 35 : 1486 -1489
PubMed 1573641 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.30 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1729 CISAPRIDE 4.0 1 8.21
CHEMBL27846 (R)ZACOPRIDE 1 6.38
CHEMBL38041 1 -
CHEMBL296522 RENZAPRIDE 3.0 1 -
CHEMBL1907770 1 -
CHEMBL34291 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1729 CISAPRIDE Ki = 6.1 nM 8.21
CHEMBL27846 (R)ZACOPRIDE Ki = 415.0 nM 6.38
CHEMBL38041 Ki > 10000.0 nM -
CHEMBL296522 RENZAPRIDE Ki > 10000.0 nM -
CHEMBL1907770 Ki > 10000.0 nM -
CHEMBL34291 Ki > 10000.0 nM -