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Assay Detail

CHEMBL899645

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

Functional
Antagonist activity at human 5HT1A expressed in mouse LM(tK-) cells assessed as inhibition of 5-HT-stimulated [35S]GTP-gamma-S binding
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
Krushinski JH, Schaus JM, Thompson DC, Calligaro DO, Nelson DL, Luecke SH, Wainscott DB, Wong DT.
Bioorg Med Chem Lett (2007) 17 : 5600 -5604
PubMed 17804228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.62 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL236514 1 8.33
CHEMBL393648 1 8.18
CHEMBL237572 1 8.11
CHEMBL396185 1 8.01
CHEMBL237749 1 7.95
CHEMBL236515 1 7.62
CHEMBL393522 1 7.52
CHEMBL237787 1 7.45
CHEMBL237789 1 7.30
CHEMBL397053 1 7.29
CHEMBL500 PINDOLOL 4.0 1 7.09
CHEMBL392392 1 6.63
CHEMBL236312 1 -
CHEMBL236315 1 -
CHEMBL237790 1 -
CHEMBL238007 1 -
CHEMBL410364 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL236514 Ki = 4.65 nM 8.33
CHEMBL393648 Ki = 6.68 nM 8.18
CHEMBL237572 Ki = 7.84 nM 8.11
CHEMBL396185 Ki = 9.83 nM 8.01
CHEMBL237749 Ki = 11.3 nM 7.95
CHEMBL236515 Ki = 24.0 nM 7.62
CHEMBL393522 Ki = 29.9 nM 7.52
CHEMBL237787 Ki = 35.5 nM 7.45
CHEMBL237789 Ki = 49.8 nM 7.30
CHEMBL397053 Ki = 50.8 nM 7.29
CHEMBL500 PINDOLOL Ki = 81.1 nM 7.09
CHEMBL392392 Ki = 233.0 nM 6.63
CHEMBL236312 Ki - -
CHEMBL236315 Ki - -
CHEMBL237790 Ki - -
CHEMBL238007 Ki - -
CHEMBL410364 Ki - -