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Assay Detail

CHEMBL615449

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

Binding
Binding affinity against [3H]8-OH-DPAT-labeled 5-hydroxytryptamine 1A receptor sites in bovine hippocampus
25
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 (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Centrally acting serotonergic and dopaminergic agents. 2. Synthesis and structure-activity relationships of 2,3,3a,4,9,9a-hexahydro-1H-benz[f]indole derivatives.
Lin CH, Haadsma-Svensson SR, Phillips G, Lahti RA, McCall RB, Piercey MF, Schreur PJ, Von Voigtlander PF, Smith MW, Chidester CG.
J Med Chem (1993) 36 : 1069 -1083
PubMed 8097538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.34 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.80
CHEMBL11386 1 7.96
CHEMBL11170 2 7.96
CHEMBL11388 2 7.77
CHEMBL275480 1 7.54
CHEMBL267769 1 7.54
CHEMBL11066 2 7.44
CHEMBL11363 2 7.25
CHEMBL11771 1 7.16
CHEMBL11770 1 6.98
CHEMBL11880 1 6.90
CHEMBL11365 1 6.84
CHEMBL11387 1 6.42
CHEMBL273601 1 6.14
CHEMBL12108 1 -
CHEMBL11381 1 -
CHEMBL275689 1 -
CHEMBL11065 1 -
CHEMBL11294 1 -
CHEMBL267557 1 -
CHEMBL275057 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 1.6 nM 8.80
CHEMBL11386 Ki = 11.0 nM 7.96
CHEMBL11170 Ki = 11.0 nM 7.96
CHEMBL11388 Ki = 17.0 nM 7.77
CHEMBL275480 Ki = 29.0 nM 7.54
CHEMBL267769 Ki = 29.0 nM 7.54
CHEMBL11066 Ki = 36.0 nM 7.44
CHEMBL11388 Ki = 37.0 nM 7.43
CHEMBL11170 Ki = 41.0 nM 7.39
CHEMBL11363 Ki = 56.0 nM 7.25
CHEMBL11066 Ki = 62.0 nM 7.21
CHEMBL11771 Ki = 69.0 nM 7.16
CHEMBL11770 Ki = 104.0 nM 6.98
CHEMBL11880 Ki = 127.0 nM 6.90
CHEMBL11365 Ki = 145.0 nM 6.84
CHEMBL11387 Ki = 384.0 nM 6.42
CHEMBL273601 Ki = 721.0 nM 6.14
CHEMBL275689 Ki > 1000.0 nM -
CHEMBL11381 Ki > 5000.0 nM -
CHEMBL12108 Ki > 1000.0 nM -
CHEMBL267557 Ki > 470.0 nM -
CHEMBL11065 Ki > 470.0 nM -
CHEMBL275057 Ki > 1000.0 nM -
CHEMBL11363 Ki > 470.0 nM -
CHEMBL11294 Ki > 1000.0 nM -