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Assay Detail

CHEMBL839710

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

Binding
Inhibition of [3H]8-OH-DPAT binding to rat 5-hydroxytryptamine 1A receptor
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel 2-aminotetralin and 3-aminochroman derivatives as selective serotonin 5-HT7 receptor agonists and antagonists.
Holmberg P, Sohn D, Leideborg R, Caldirola P, Zlatoidsky P, Hanson S, Mohell N, Rosqvist S, Nordvall G, Johansson AM, Johansson R.
J Med Chem (2004) 47 : 3927 -3930
PubMed 15267230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.33 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL362540 1 9.06
CHEMBL186112 1 8.91
CHEMBL186758 1 8.88
CHEMBL188176 1 8.83
CHEMBL186316 1 7.99
CHEMBL184535 1 7.93
CHEMBL28056 1 6.85
CHEMBL182792 1 6.76
CHEMBL361875 1 6.46
CHEMBL273921 1 6.32
CHEMBL314055 1 6.29
CHEMBL362354 1 6.25
CHEMBL361287 1 6.17
CHEMBL363466 1 5.85
CHEMBL184666 1 -
CHEMBL183329 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL362540 Ki = 0.87 nM 9.06
CHEMBL186112 Ki = 1.23 nM 8.91
CHEMBL186758 Ki = 1.31 nM 8.88
CHEMBL188176 Ki = 1.49 nM 8.83
CHEMBL186316 Ki = 10.3 nM 7.99
CHEMBL184535 Ki = 11.7 nM 7.93
CHEMBL28056 Ki = 142.0 nM 6.85
CHEMBL182792 Ki = 174.0 nM 6.76
CHEMBL361875 Ki = 347.0 nM 6.46
CHEMBL273921 Ki = 479.0 nM 6.32
CHEMBL314055 Ki = 513.0 nM 6.29
CHEMBL362354 Ki = 562.0 nM 6.25
CHEMBL361287 Ki = 680.0 nM 6.17
CHEMBL363466 Ki = 1420.0 nM 5.85
CHEMBL184666 Ki > 1000.0 nM -
CHEMBL183329 Ki > 1000.0 nM -