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Assay Detail

CHEMBL802687

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

Functional
Compound was evaluated for its activity at solubilized receptor (CHAPS/salt-solubilized preparation) from rat frontal cortex
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Frontal cortex
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

In vitro labeling of serotonin-S2 receptors: synthesis and binding characteristics of [3H]-7-aminoketanserin.
Wouters W, Janssen CG, Van Dun J, Thijssen JB, Laduron PM.
J Med Chem (1986) 29 : 1663 -1668
PubMed 3746815 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.75 8.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18331 PIRENPERONE 2.0 1 8.45
CHEMBL267930 SPIPERONE 2.0 1 8.41
CHEMBL51 KETANSERIN 3.0 1 8.40
CHEMBL1065 METHYSERGIDE 4.0 1 8.17
CHEMBL267777 RITANSERIN 2.0 1 8.15
CHEMBL440294 PIPAMPERONE 3.0 1 8.02
CHEMBL6437 MIANSERIN 4.0 1 7.87
CHEMBL1255588 1 7.75
CHEMBL219916 DOMPERIDONE 3.0 1 6.00
CHEMBL25554 1 5.41
CHEMBL416526 BUFOTENINE 1 5.20
CHEMBL511 PYRILAMINE 4.0 1 5.00
CHEMBL6066837 (-)-BUTACLAMOL 1 4.86
CHEMBL39 SEROTONIN 3.0 1 4.85
CHEMBL2 PRAZOSIN 4.0 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18331 PIRENPERONE Ki = 3.54 nM 8.45
CHEMBL267930 SPIPERONE Ki = 3.88 nM 8.41
CHEMBL51 KETANSERIN Ki = 3.97 nM 8.40
CHEMBL1065 METHYSERGIDE Ki = 6.74 nM 8.17
CHEMBL267777 RITANSERIN Ki = 7.06 nM 8.15
CHEMBL440294 PIPAMPERONE Ki = 9.53 nM 8.02
CHEMBL6437 MIANSERIN Ki = 13.46 nM 7.87
CHEMBL1255588 Ki = 17.74 nM 7.75
CHEMBL219916 DOMPERIDONE Ki = 998.0 nM 6.00
CHEMBL25554 Ki = 3881.0 nM 5.41
CHEMBL416526 BUFOTENINE Ki = 6295.0 nM 5.20
CHEMBL511 PYRILAMINE Ki = 9976.0 nM 5.00
CHEMBL6066837 (-)-BUTACLAMOL Ki = 13771.0 nM 4.86
CHEMBL39 SEROTONIN Ki = 14092.0 nM 4.85
CHEMBL2 PRAZOSIN Ki = 19905.0 nM 4.70