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Assay Detail

CHEMBL1065705

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

Binding
Displacement of [3H]8-OH-DPAT from 5HT1A receptor expressed in CHO cells by liquid scintillation counting
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of dihydrofuroaporphine derivatives: identification of a potent and selective serotonin 5-HT 1A receptor agonist.
Liu Z, Zhang H, Ye N, Zhang J, Wu Q, Sun P, Li L, Zhen X, Zhang A.
J Med Chem (2010) 53 : 1319 -1328
PubMed 20041669 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.17 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.92
CHEMBL597094 1 8.51
CHEMBL609317 1 8.17
CHEMBL591916 1 7.96
CHEMBL598037 1 7.92
CHEMBL608728 1 7.92
CHEMBL596885 1 7.85
CHEMBL49 BUSPIRONE 4.0 1 7.70
CHEMBL607559 1 7.54
CHEMBL27559 1 7.35
CHEMBL609611 1 7.34
CHEMBL119455 1 7.31
CHEMBL591448 1 7.26
CHEMBL596886 1 7.18
CHEMBL599065 1 7.05
CHEMBL596678 1 6.90
CHEMBL596884 1 6.87
CHEMBL603752 1 6.84
CHEMBL599080 1 6.83
CHEMBL270426 1 6.59
CHEMBL598759 1 6.55
CHEMBL597881 1 6.50
CHEMBL599064 1 6.47
CHEMBL598760 1 6.43
CHEMBL597882 1 6.29
CHEMBL611973 1 6.20
CHEMBL604588 1 6.20
CHEMBL596865 1 6.10
CHEMBL597095 1 -
CHEMBL604179 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 1.2 nM 8.92
CHEMBL597094 Ki = 3.1 nM 8.51
CHEMBL609317 Ki = 6.7 nM 8.17
CHEMBL591916 Ki = 11.0 nM 7.96
CHEMBL598037 Ki = 12.0 nM 7.92
CHEMBL608728 Ki = 12.0 nM 7.92
CHEMBL596885 Ki = 14.0 nM 7.85
CHEMBL49 BUSPIRONE Ki = 20.0 nM 7.70
CHEMBL607559 Ki = 29.0 nM 7.54
CHEMBL27559 Ki = 45.0 nM 7.35
CHEMBL609611 Ki = 45.3 nM 7.34
CHEMBL119455 Ki = 49.0 nM 7.31
CHEMBL591448 Ki = 55.0 nM 7.26
CHEMBL596886 Ki = 66.0 nM 7.18
CHEMBL599065 Ki = 90.0 nM 7.05
CHEMBL596678 Ki = 125.0 nM 6.90
CHEMBL596884 Ki = 135.0 nM 6.87
CHEMBL603752 Ki = 144.0 nM 6.84
CHEMBL599080 Ki = 149.0 nM 6.83
CHEMBL270426 Ki = 258.0 nM 6.59
CHEMBL598759 Ki = 279.0 nM 6.55
CHEMBL597881 Ki = 320.0 nM 6.50
CHEMBL599064 Ki = 340.0 nM 6.47
CHEMBL598760 Ki = 373.0 nM 6.43
CHEMBL597882 Ki = 510.0 nM 6.29
CHEMBL611973 Ki = 630.0 nM 6.20
CHEMBL604588 Ki = 626.0 nM 6.20
CHEMBL596865 Ki = 793.0 nM 6.10
CHEMBL597095 Ki > 10000.0 nM -
CHEMBL604179 Ki > 10000.0 nM -
CHEMBL596866 Ki - -
CHEMBL603542 Ki - -