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Assay Detail

CHEMBL899647

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

Binding
Displacement of [3H]DPAT from human 5HT1A receptor
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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 24 7.28 8.88

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL393648 1 8.88
CHEMBL396185 1 8.45
CHEMBL236514 1 8.41
CHEMBL237749 1 8.17
CHEMBL237572 1 8.03
CHEMBL237787 1 7.97
CHEMBL236515 1 7.95
CHEMBL393522 1 7.74
CHEMBL500 PINDOLOL 4.0 1 7.65
CHEMBL397053 1 7.58
CHEMBL237789 1 7.54
CHEMBL410364 1 7.50
CHEMBL238007 1 7.39
CHEMBL391230 1 7.12
CHEMBL237790 1 7.11
CHEMBL392392 1 7.03
CHEMBL236518 1 6.90
CHEMBL236517 1 6.26
CHEMBL237759 1 6.08
CHEMBL236315 1 6.06
CHEMBL396430 1 6.06
CHEMBL236312 1 5.84
CHEMBL412022 1 5.75
CHEMBL236733 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL393648 Ki = 1.33 nM 8.88
CHEMBL396185 Ki = 3.58 nM 8.45
CHEMBL236514 Ki = 3.89 nM 8.41
CHEMBL237749 Ki = 6.82 nM 8.17
CHEMBL237572 Ki = 9.29 nM 8.03
CHEMBL237787 Ki = 10.6 nM 7.97
CHEMBL236515 Ki = 11.2 nM 7.95
CHEMBL393522 Ki = 18.3 nM 7.74
CHEMBL500 PINDOLOL Ki = 22.4 nM 7.65
CHEMBL397053 Ki = 26.1 nM 7.58
CHEMBL237789 Ki = 28.6 nM 7.54
CHEMBL410364 Ki = 32.0 nM 7.50
CHEMBL238007 Ki = 40.6 nM 7.39
CHEMBL391230 Ki = 76.1 nM 7.12
CHEMBL237790 Ki = 78.4 nM 7.11
CHEMBL392392 Ki = 94.3 nM 7.03
CHEMBL236518 Ki = 125.0 nM 6.90
CHEMBL236517 Ki = 551.0 nM 6.26
CHEMBL237759 Ki = 833.0 nM 6.08
CHEMBL236315 Ki = 868.0 nM 6.06
CHEMBL396430 Ki = 872.0 nM 6.06
CHEMBL236312 Ki = 1450.0 nM 5.84
CHEMBL412022 Ki = 1772.0 nM 5.75
CHEMBL236733 Ki > 3000.0 nM -