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Assay Detail

CHEMBL923320

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

Binding
Displacement of [3H]WAY 100635 from human recombinant 5HT1A receptor expressed in CHO cells
15
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

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.
Ward SE, Johnson CN, Lovell PJ, Scott CM, Smith PW, Stemp G, Thewlis KM, Vong AK, Watson JM.
Bioorg Med Chem Lett (2007) 17 : 5214 -5217
PubMed 17629698 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 8.04 8.60
Log Ki 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183460 1 8.60
CHEMBL443060 1 8.60
CHEMBL246598 1 8.50
CHEMBL247609 1 8.50
CHEMBL248456 1 8.30
CHEMBL246597 1 8.20
CHEMBL247428 1 8.10
CHEMBL399719 1 8.00
CHEMBL246599 1 7.60
CHEMBL248407 1 7.50
CHEMBL248458 1 7.40
CHEMBL248457 1 7.20
CHEMBL248231 1 -
CHEMBL248230 1 -
CHEMBL248229 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183460 Ki = 2.512 nM 8.60
CHEMBL443060 Ki = 2.512 nM 8.60
CHEMBL246598 Ki = 3.162 nM 8.50
CHEMBL247609 Ki = 3.162 nM 8.50
CHEMBL248456 Ki = 5.012 nM 8.30
CHEMBL246597 Ki = 6.31 nM 8.20
CHEMBL247428 Ki = 7.943 nM 8.10
CHEMBL399719 Ki = 10.0 nM 8.00
CHEMBL246599 Ki = 25.12 nM 7.60
CHEMBL248407 Ki = 31.62 nM 7.50
CHEMBL248458 Ki = 39.81 nM 7.40
CHEMBL248457 Ki = 63.1 nM 7.20
CHEMBL248231 Log Ki - -
CHEMBL248230 Log Ki - -
CHEMBL248229 Log Ki - -