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Assay Detail

CHEMBL615939

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

Binding
In vitro displacement of [3H]8-OH-DPAT binding to rat hippocampal 5-hydroxytryptamine 1A receptor
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

11-substituted (R)-aporphines: synthesis, pharmacology, and modeling of D2A and 5-HT1A receptor interactions.
Hedberg MH, Linnanen T, Jansen JM, Nordvall G, Hjorth S, Unelius L, Johansson AM.
J Med Chem (1996) 39 : 3503 -3513
PubMed 8784448 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.48 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25924 1 8.74
CHEMBL118254 1 8.35
CHEMBL117841 1 8.29
CHEMBL332332 1 8.24
CHEMBL119656 1 8.22
CHEMBL333836 1 8.11
CHEMBL119132 1 8.08
CHEMBL119455 1 8.02
CHEMBL27940 1 7.84
CHEMBL333085 1 7.57
CHEMBL119154 1 7.50
CHEMBL27559 1 7.40
CHEMBL115969 1 7.39
CHEMBL333134 1 7.24
CHEMBL281357 1 7.10
CHEMBL324073 1 6.70
CHEMBL53 APOMORPHINE 4.0 1 6.53
CHEMBL115402 1 6.43
CHEMBL333725 1 6.36
CHEMBL119401 1 5.49
CHEMBL119384 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25924 Ki = 1.8 nM 8.74
CHEMBL118254 Ki = 4.5 nM 8.35
CHEMBL117841 Ki = 5.1 nM 8.29
CHEMBL332332 Ki = 5.7 nM 8.24
CHEMBL119656 Ki = 6.0 nM 8.22
CHEMBL333836 Ki = 7.7 nM 8.11
CHEMBL119132 Ki = 8.3 nM 8.08
CHEMBL119455 Ki = 9.6 nM 8.02
CHEMBL27940 Ki = 14.4 nM 7.84
CHEMBL333085 Ki = 26.9 nM 7.57
CHEMBL119154 Ki = 31.3 nM 7.50
CHEMBL27559 Ki = 39.5 nM 7.40
CHEMBL115969 Ki = 41.1 nM 7.39
CHEMBL333134 Ki = 57.1 nM 7.24
CHEMBL281357 Ki = 80.0 nM 7.10
CHEMBL324073 Ki = 198.0 nM 6.70
CHEMBL53 APOMORPHINE Ki = 296.0 nM 6.53
CHEMBL115402 Ki = 375.0 nM 6.43
CHEMBL333725 Ki = 437.0 nM 6.36
CHEMBL119401 Ki = 3220.0 nM 5.49
CHEMBL119384 Ki > 5000.0 nM -