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Assay Detail

CHEMBL954042

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

Binding
Displacement of [3H]5HT from human recombinant 5HT1D receptor
22
Total Activities
22
Compounds Tested
1
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 1D (CHEMBL1983)
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 22 8.82 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL525362 1 9.60
CHEMBL506942 1 9.50
CHEMBL495213 1 9.40
CHEMBL525712 1 9.30
CHEMBL494806 1 9.30
CHEMBL497963 1 9.30
CHEMBL498354 1 9.20
CHEMBL425190 1 9.10
CHEMBL494631 1 9.00
CHEMBL496098 1 9.00
CHEMBL498356 1 8.90
CHEMBL498355 1 8.90
CHEMBL495046 1 8.80
CHEMBL497127 1 8.80
CHEMBL183460 1 8.80
CHEMBL522708 1 8.80
CHEMBL495895 1 8.70
CHEMBL494992 1 8.60
CHEMBL495161 1 8.30
CHEMBL495217 1 8.20
CHEMBL494991 1 7.90
CHEMBL495160 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL525362 Ki = 0.2512 nM 9.60
CHEMBL506942 Ki = 0.3162 nM 9.50
CHEMBL495213 Ki = 0.3981 nM 9.40
CHEMBL525712 Ki = 0.5012 nM 9.30
CHEMBL494806 Ki = 0.5012 nM 9.30
CHEMBL497963 Ki = 0.5012 nM 9.30
CHEMBL498354 Ki = 0.631 nM 9.20
CHEMBL425190 Ki = 0.7943 nM 9.10
CHEMBL494631 Ki = 1.0 nM 9.00
CHEMBL496098 Ki = 1.0 nM 9.00
CHEMBL498356 Ki = 1.259 nM 8.90
CHEMBL498355 Ki = 1.259 nM 8.90
CHEMBL495046 Ki = 1.585 nM 8.80
CHEMBL497127 Ki = 1.585 nM 8.80
CHEMBL183460 Ki = 1.585 nM 8.80
CHEMBL522708 Ki = 1.585 nM 8.80
CHEMBL495895 Ki = 1.995 nM 8.70
CHEMBL494992 Ki = 2.512 nM 8.60
CHEMBL495161 Ki = 5.012 nM 8.30
CHEMBL495217 Ki = 6.31 nM 8.20
CHEMBL494991 Ki = 12.59 nM 7.90
CHEMBL495160 Ki = 199.53 nM 6.70