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Assay Detail

CHEMBL674826

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 [3H]ADTN, a dopamine agonist
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
Ki 19 8.12 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431367 ROXINDOLE 2.0 1 9.06
CHEMBL338710 1 8.80
CHEMBL130659 1 8.74
CHEMBL130502 1 8.60
CHEMBL132446 1 8.51
CHEMBL132270 1 8.40
CHEMBL130614 1 8.37
CHEMBL130327 1 8.36
CHEMBL338849 1 8.27
CHEMBL131841 1 7.92
CHEMBL419957 1 7.89
CHEMBL131356 1 7.82
CHEMBL64344 1 7.82
CHEMBL131711 1 7.68
CHEMBL339954 1 7.39
CHEMBL130501 1 7.34
CHEMBL127609 1 7.09
CHEMBL59335 1 -
CHEMBL130605 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431367 ROXINDOLE Ki = 0.88 nM 9.06
CHEMBL338710 Ki = 1.6 nM 8.80
CHEMBL130659 Ki = 1.8 nM 8.74
CHEMBL130502 Ki = 2.5 nM 8.60
CHEMBL132446 Ki = 3.1 nM 8.51
CHEMBL132270 Ki = 4.0 nM 8.40
CHEMBL130614 Ki = 4.3 nM 8.37
CHEMBL130327 Ki = 4.4 nM 8.36
CHEMBL338849 Ki = 5.4 nM 8.27
CHEMBL131841 Ki = 12.0 nM 7.92
CHEMBL419957 Ki = 13.0 nM 7.89
CHEMBL131356 Ki = 15.0 nM 7.82
CHEMBL64344 Ki = 15.0 nM 7.82
CHEMBL131711 Ki = 21.0 nM 7.68
CHEMBL339954 Ki = 41.0 nM 7.39
CHEMBL130501 Ki = 46.0 nM 7.34
CHEMBL127609 Ki = 81.0 nM 7.09
CHEMBL59335 Ki > 100.0 nM -
CHEMBL130605 Ki > 1000.0 nM -