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Assay Detail

CHEMBL802686

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

Functional
Compound was evaluated for its activity at membrane-bound receptor (M+L+P fraction) 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 7.55 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18331 PIRENPERONE 2.0 1 9.33
CHEMBL267930 SPIPERONE 2.0 1 9.21
CHEMBL51 KETANSERIN 3.0 1 9.17
CHEMBL267777 RITANSERIN 2.0 1 9.05
CHEMBL440294 PIPAMPERONE 3.0 1 8.86
CHEMBL1065 METHYSERGIDE 4.0 1 8.72
CHEMBL6437 MIANSERIN 4.0 1 8.52
CHEMBL1255588 1 8.47
CHEMBL219916 DOMPERIDONE 3.0 1 6.82
CHEMBL416526 BUFOTENINE 1 6.47
CHEMBL25554 1 6.16
CHEMBL39 SEROTONIN 3.0 1 6.04
CHEMBL511 PYRILAMINE 4.0 1 5.99
CHEMBL6066837 (-)-BUTACLAMOL 1 5.49
CHEMBL2 PRAZOSIN 4.0 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18331 PIRENPERONE Ki = 0.47 nM 9.33
CHEMBL267930 SPIPERONE Ki = 0.62 nM 9.21
CHEMBL51 KETANSERIN Ki = 0.68 nM 9.17
CHEMBL267777 RITANSERIN Ki = 0.9 nM 9.05
CHEMBL440294 PIPAMPERONE Ki = 1.39 nM 8.86
CHEMBL1065 METHYSERGIDE Ki = 1.92 nM 8.72
CHEMBL6437 MIANSERIN Ki = 3.04 nM 8.52
CHEMBL1255588 Ki = 3.41 nM 8.47
CHEMBL219916 DOMPERIDONE Ki = 152.0 nM 6.82
CHEMBL416526 BUFOTENINE Ki = 341.0 nM 6.47
CHEMBL25554 Ki = 697.0 nM 6.16
CHEMBL39 SEROTONIN Ki = 919.0 nM 6.04
CHEMBL511 PYRILAMINE Ki = 1032.0 nM 5.99
CHEMBL6066837 (-)-BUTACLAMOL Ki = 3261.0 nM 5.49
CHEMBL2 PRAZOSIN Ki = 11572.0 nM 4.94