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Assay Detail

CHEMBL953250

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

Binding
Displacement of [3H]8-OH-DPAT from human recombinant 5HT1A receptor
12
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of potent, orally bioavailable, selective 5-HT1A/B/D receptor antagonists.
Ward SE, Eddershaw PJ, Scott CM, Gordon LJ, Lovell PJ, Moore SH, Smith PW, Starr KR, Thewlis KM, Watson JM.
J Med Chem (2008) 51 : 2887 -2890
PubMed 18433113 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.31 9.80
pKi 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31354 WAY-100,635 1 9.80
CHEMBL183460 1 9.50
CHEMBL56 8-OH-DPAT 1 9.10
CHEMBL39 SEROTONIN 3.0 1 8.90
CHEMBL494806 1 8.70
CHEMBL494991 1 8.30
CHEMBL494992 1 7.90
CHEMBL494631 1 7.60
CHEMBL495160 1 6.80
CHEMBL425190 1 6.50
CHEMBL506942 1 -
CHEMBL495161 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31354 WAY-100,635 Ki = 0.1585 nM 9.80
CHEMBL183460 Ki = 0.3162 nM 9.50
CHEMBL56 8-OH-DPAT Ki = 0.7943 nM 9.10
CHEMBL39 SEROTONIN Ki = 1.259 nM 8.90
CHEMBL494806 Ki = 1.995 nM 8.70
CHEMBL494991 Ki = 5.012 nM 8.30
CHEMBL494992 Ki = 12.59 nM 7.90
CHEMBL494631 Ki = 25.12 nM 7.60
CHEMBL495160 Ki = 158.49 nM 6.80
CHEMBL425190 Ki = 316.23 nM 6.50
CHEMBL506942 pKi - -
CHEMBL495161 pKi - -