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Assay Detail

CHEMBL1035839

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

Binding
Displacement of [125I]WAY100635 from human 5HT1A receptor expressed in CHO cells
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.
Ward SE, Eddershaw P, Flynn ST, Gordon L, Lovell PJ, Moore SH, Scott CM, Smith PW, Thewlis KM, Wyman PA.
Bioorg Med Chem Lett (2009) 19 : 428 -432
PubMed 19071020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 8.22 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL458199 1 9.00
CHEMBL461670 1 8.70
CHEMBL497963 1 8.60
CHEMBL514429 1 8.60
CHEMBL513955 1 8.60
CHEMBL517170 1 8.60
CHEMBL459282 1 8.50
CHEMBL518545 1 8.40
CHEMBL459061 1 8.40
CHEMBL457982 1 8.30
CHEMBL457765 1 8.30
CHEMBL516997 1 8.30
CHEMBL459067 1 8.20
CHEMBL458200 1 8.10
CHEMBL462916 1 8.10
CHEMBL462915 1 8.10
CHEMBL456684 1 8.00
CHEMBL459068 1 7.90
CHEMBL496098 1 7.80
CHEMBL456458 1 7.70
CHEMBL456460 1 7.50
CHEMBL456459 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL458199 Ki = 1.0 nM 9.00
CHEMBL461670 Ki = 1.995 nM 8.70
CHEMBL497963 Ki = 2.512 nM 8.60
CHEMBL514429 Ki = 2.512 nM 8.60
CHEMBL513955 Ki = 2.512 nM 8.60
CHEMBL517170 Ki = 2.512 nM 8.60
CHEMBL459282 Ki = 3.162 nM 8.50
CHEMBL518545 Ki = 3.981 nM 8.40
CHEMBL459061 Ki = 3.981 nM 8.40
CHEMBL457982 Ki = 5.012 nM 8.30
CHEMBL457765 Ki = 5.012 nM 8.30
CHEMBL516997 Ki = 5.012 nM 8.30
CHEMBL459067 Ki = 6.31 nM 8.20
CHEMBL458200 Ki = 7.943 nM 8.10
CHEMBL462916 Ki = 7.943 nM 8.10
CHEMBL462915 Ki = 7.943 nM 8.10
CHEMBL456684 Ki = 10.0 nM 8.00
CHEMBL459068 Ki = 12.59 nM 7.90
CHEMBL496098 Ki = 15.85 nM 7.80
CHEMBL456458 Ki = 19.95 nM 7.70
CHEMBL456460 Ki = 31.62 nM 7.50
CHEMBL456459 Ki = 63.1 nM 7.20