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Assay Detail

CHEMBL785004

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

Functional
In vitro inhibition of [3H]5-HT uptake in rat brain (minus pons, medulla oblongata and cerebellum) homogenates.
18
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Cerebellum
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Enhanced D1 affinity in a series of piperazine ring substituted 1-piperazino-3-arylindans with potential atypical antipsychotic activity.
Bøgesø KP, Arnt J, Frederiksen K, Hansen HO, Hyttel J, Pedersen H.
J Med Chem (1995) 38 : 4380 -4392
PubMed 7473566 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 5.46 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307717 2 6.21
CHEMBL136683 2 5.75
CHEMBL343922 1 5.75
CHEMBL343282 2 5.70
CHEMBL136822 1 5.62
CHEMBL136260 2 5.58
CHEMBL136235 2 5.43
CHEMBL137960 2 5.40
CHEMBL136722 2 5.28
CHEMBL136630 2 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307717 IC50 = 610.0 nM 6.21
CHEMBL343922 IC50 = 1800.0 nM 5.75
CHEMBL136683 IC50 = 1800.0 nM 5.75
CHEMBL343282 IC50 = 2000.0 nM 5.70
CHEMBL136822 IC50 = 2400.0 nM 5.62
CHEMBL136260 IC50 = 2600.0 nM 5.58
CHEMBL136260 IC50 = 3500.0 nM 5.46
CHEMBL136235 IC50 = 3700.0 nM 5.43
CHEMBL307717 IC50 = 3900.0 nM 5.41
CHEMBL137960 IC50 = 4000.0 nM 5.40
CHEMBL343282 IC50 = 4500.0 nM 5.35
CHEMBL137960 IC50 = 5300.0 nM 5.28
CHEMBL136722 IC50 = 5200.0 nM 5.28
CHEMBL136630 IC50 = 7200.0 nM 5.14
CHEMBL136722 IC50 = 10000.0 nM 5.00
CHEMBL136235 IC50 = 12000.0 nM 4.92
CHEMBL136630 IC50 > 1000.0 nM -
CHEMBL136683 IC50 > 100.0 nM -