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Assay Detail

CHEMBL938538

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

Binding
Displacement of [3H]WAY-100635 from human 5HT1A receptor expressed in CHO cells
21
Total Activities
21
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

6-[2-(4-Aryl-1-piperazinyl)ethyl]-2H-1,4-benzoxazin-3(4H)-ones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors.
Bromidge SM, Bertani B, Borriello M, Faedo S, Gordon LJ, Granci E, Hill M, Marshall HR, Stasi LP, Zucchelli V, Merlo G, Vesentini A, Watson JM, Zonzini L.
Bioorg Med Chem Lett (2008) 18 : 5653 -5656
PubMed 18799312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.95 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL484260 1 9.90
CHEMBL497979 1 9.60
CHEMBL490417 1 9.60
CHEMBL496317 1 9.60
CHEMBL496520 1 9.60
CHEMBL521506 1 9.50
CHEMBL489195 1 9.40
CHEMBL522257 1 9.40
CHEMBL491839 1 9.30
CHEMBL489393 1 9.30
CHEMBL484059 1 9.20
CHEMBL495705 1 9.10
CHEMBL489394 1 8.90
CHEMBL521873 1 8.80
CHEMBL523095 1 8.80
CHEMBL485491 1 8.60
CHEMBL495703 1 8.50
CHEMBL444398 1 8.50
CHEMBL497980 1 8.40
CHEMBL490211 1 7.00
CHEMBL523064 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL484260 Ki = 0.1259 nM 9.90
CHEMBL497979 Ki = 0.2512 nM 9.60
CHEMBL490417 Ki = 0.2512 nM 9.60
CHEMBL496317 Ki = 0.2512 nM 9.60
CHEMBL496520 Ki = 0.2512 nM 9.60
CHEMBL521506 Ki = 0.3162 nM 9.50
CHEMBL489195 Ki = 0.3981 nM 9.40
CHEMBL522257 Ki = 0.3981 nM 9.40
CHEMBL491839 Ki = 0.5012 nM 9.30
CHEMBL489393 Ki = 0.5012 nM 9.30
CHEMBL484059 Ki = 0.631 nM 9.20
CHEMBL495705 Ki = 0.7943 nM 9.10
CHEMBL489394 Ki = 1.259 nM 8.90
CHEMBL521873 Ki = 1.585 nM 8.80
CHEMBL523095 Ki = 1.585 nM 8.80
CHEMBL485491 Ki = 2.512 nM 8.60
CHEMBL495703 Ki = 3.162 nM 8.50
CHEMBL444398 Ki = 3.162 nM 8.50
CHEMBL497980 Ki = 3.981 nM 8.40
CHEMBL490211 Ki = 100.0 nM 7.00
CHEMBL523064 Ki = 125.89 nM 6.90