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Assay Detail

CHEMBL672043

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

Functional
Evaluated for its ability to displace tritiated receptor ligand in rat striatal membranes 3[H]spiperone, a dopamine antagonist
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

D(2) dopamine receptor (CHEMBL339)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and dopaminergic activity of some 3-(1,2,3,6-tetrahydro-1-pyridylalkyl)indoles. A novel conformational model to explain structure-activity relationships.
Böttcher H, Barnickel G, Hausberg HH, Haase AF, Seyfried CA, Eiermann V.
J Med Chem (1992) 35 : 4020 -4026
PubMed 1359142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 7.31 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL130502 1 8.10
CHEMBL130659 1 8.05
CHEMBL338710 1 8.00
CHEMBL130327 1 7.70
CHEMBL132270 1 7.70
CHEMBL130614 1 7.40
CHEMBL338849 1 7.30
CHEMBL131841 1 7.30
CHEMBL132446 1 7.30
CHEMBL419957 1 7.22
CHEMBL64344 1 7.05
CHEMBL131356 1 7.00
CHEMBL131711 1 7.00
CHEMBL130501 1 7.00
CHEMBL127609 1 7.00
CHEMBL44231 1 6.98
CHEMBL339954 1 6.16
CHEMBL59335 1 -
CHEMBL130605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL130502 IC50 = 8.0 nM 8.10
CHEMBL130659 IC50 = 9.0 nM 8.05
CHEMBL338710 IC50 = 10.0 nM 8.00
CHEMBL130327 IC50 = 20.0 nM 7.70
CHEMBL132270 IC50 = 20.0 nM 7.70
CHEMBL130614 IC50 = 40.0 nM 7.40
CHEMBL338849 IC50 = 50.0 nM 7.30
CHEMBL131841 IC50 = 50.0 nM 7.30
CHEMBL132446 IC50 = 50.0 nM 7.30
CHEMBL419957 IC50 = 60.0 nM 7.22
CHEMBL64344 IC50 = 90.0 nM 7.05
CHEMBL131356 IC50 = 100.0 nM 7.00
CHEMBL131711 IC50 = 100.0 nM 7.00
CHEMBL130501 IC50 = 100.0 nM 7.00
CHEMBL127609 IC50 = 100.0 nM 7.00
CHEMBL44231 IC50 = 105.0 nM 6.98
CHEMBL339954 IC50 = 700.0 nM 6.16
CHEMBL59335 IC50 > 100.0 nM -
CHEMBL130605 IC50 > 1000.0 nM -