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Assay Detail

CHEMBL615941

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

Binding
In vitro affinity at 5-hydroxytryptamine 1A receptor of rat hippocampus by [3H]8-OH-DPAT displacement.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Hippocampus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

10-substituted 11-oxygenated (R)-aporphines: synthesis, pharmacology, and modeling of 5-HT1A receptor interactions.
Hedberg MH, Jansen JM, Nordvall G, Hjorth S, Unelius L, Johansson AM.
J Med Chem (1996) 39 : 3491 -3502
PubMed 8784447 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.03 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53510 1 9.35
CHEMBL116367 1 8.49
CHEMBL332178 1 8.12
CHEMBL115524 1 8.04
CHEMBL119455 1 8.02
CHEMBL118771 1 7.97
CHEMBL119593 1 7.91
CHEMBL117730 1 7.90
CHEMBL331005 1 7.76
CHEMBL331100 1 6.97
CHEMBL324372 1 6.82
CHEMBL435779 1 6.62
CHEMBL53 APOMORPHINE 4.0 1 6.53
CHEMBL332490 1 6.19
CHEMBL332771 1 6.11
CHEMBL119150 1 6.00
CHEMBL119577 1 5.96
CHEMBL119223 1 5.86
CHEMBL334116 1 5.79
CHEMBL326159 1 5.76
CHEMBL119900 1 5.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53510 Ki = 0.45 nM 9.35
CHEMBL116367 Ki = 3.2 nM 8.49
CHEMBL332178 Ki = 7.5 nM 8.12
CHEMBL115524 Ki = 9.2 nM 8.04
CHEMBL119455 Ki = 9.6 nM 8.02
CHEMBL118771 Ki = 10.8 nM 7.97
CHEMBL119593 Ki = 12.3 nM 7.91
CHEMBL117730 Ki = 12.6 nM 7.90
CHEMBL331005 Ki = 17.5 nM 7.76
CHEMBL331100 Ki = 108.0 nM 6.97
CHEMBL324372 Ki = 150.0 nM 6.82
CHEMBL435779 Ki = 241.0 nM 6.62
CHEMBL53 APOMORPHINE Ki = 296.0 nM 6.53
CHEMBL332490 Ki = 640.0 nM 6.19
CHEMBL332771 Ki = 772.0 nM 6.11
CHEMBL119150 Ki = 995.0 nM 6.00
CHEMBL119577 Ki = 1090.0 nM 5.96
CHEMBL119223 Ki = 1380.0 nM 5.86
CHEMBL334116 Ki = 1621.0 nM 5.79
CHEMBL326159 Ki = 1720.0 nM 5.76
CHEMBL119900 Ki = 3300.0 nM 5.48