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Assay Detail

CHEMBL802685

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
IC50 15 6.45 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18331 PIRENPERONE 2.0 1 8.15
CHEMBL267930 SPIPERONE 2.0 1 8.11
CHEMBL51 KETANSERIN 3.0 1 8.10
CHEMBL1065 METHYSERGIDE 4.0 1 7.87
CHEMBL267777 RITANSERIN 2.0 1 7.85
CHEMBL440294 PIPAMPERONE 3.0 1 7.72
CHEMBL6437 MIANSERIN 4.0 1 7.57
CHEMBL1255588 1 7.45
CHEMBL219916 DOMPERIDONE 3.0 1 5.70
CHEMBL25554 1 5.11
CHEMBL416526 BUFOTENINE 1 4.90
CHEMBL511 PYRILAMINE 4.0 1 4.70
CHEMBL6066837 (-)-BUTACLAMOL 1 4.56
CHEMBL39 SEROTONIN 3.0 1 4.55
CHEMBL2 PRAZOSIN 4.0 1 4.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18331 PIRENPERONE IC50 = 7.079 nM 8.15
CHEMBL267930 SPIPERONE IC50 = 7.762 nM 8.11
CHEMBL51 KETANSERIN IC50 = 7.943 nM 8.10
CHEMBL1065 METHYSERGIDE IC50 = 13.49 nM 7.87
CHEMBL267777 RITANSERIN IC50 = 14.13 nM 7.85
CHEMBL440294 PIPAMPERONE IC50 = 19.05 nM 7.72
CHEMBL6437 MIANSERIN IC50 = 26.92 nM 7.57
CHEMBL1255588 IC50 = 35.48 nM 7.45
CHEMBL219916 DOMPERIDONE IC50 = 1995.26 nM 5.70
CHEMBL25554 IC50 = 7762.47 nM 5.11
CHEMBL416526 BUFOTENINE IC50 = 12589.25 nM 4.90
CHEMBL511 PYRILAMINE IC50 = 19952.62 nM 4.70
CHEMBL6066837 (-)-BUTACLAMOL IC50 = 27542.29 nM 4.56
CHEMBL39 SEROTONIN IC50 = 28183.83 nM 4.55
CHEMBL2 PRAZOSIN IC50 = 39810.72 nM 4.40