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Assay Detail

CHEMBL938540

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

Binding
Displacement of [3H]5HT from human 5HT1D 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 1D (CHEMBL1983)
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 9.37 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490417 1 9.80
CHEMBL521506 1 9.80
CHEMBL491839 1 9.80
CHEMBL444398 1 9.70
CHEMBL489394 1 9.70
CHEMBL497980 1 9.70
CHEMBL485491 1 9.70
CHEMBL490211 1 9.60
CHEMBL496317 1 9.60
CHEMBL523095 1 9.60
CHEMBL497979 1 9.50
CHEMBL489195 1 9.50
CHEMBL522257 1 9.50
CHEMBL495705 1 9.50
CHEMBL484260 1 9.40
CHEMBL496520 1 9.40
CHEMBL489393 1 9.40
CHEMBL521873 1 9.30
CHEMBL495703 1 8.80
CHEMBL484059 1 7.90
CHEMBL523064 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490417 Ki = 0.1585 nM 9.80
CHEMBL521506 Ki = 0.1585 nM 9.80
CHEMBL491839 Ki = 0.1585 nM 9.80
CHEMBL444398 Ki = 0.1995 nM 9.70
CHEMBL489394 Ki = 0.1995 nM 9.70
CHEMBL497980 Ki = 0.1995 nM 9.70
CHEMBL485491 Ki = 0.1995 nM 9.70
CHEMBL490211 Ki = 0.2512 nM 9.60
CHEMBL496317 Ki = 0.2512 nM 9.60
CHEMBL523095 Ki = 0.2512 nM 9.60
CHEMBL497979 Ki = 0.3162 nM 9.50
CHEMBL489195 Ki = 0.3162 nM 9.50
CHEMBL522257 Ki = 0.3162 nM 9.50
CHEMBL495705 Ki = 0.3162 nM 9.50
CHEMBL484260 Ki = 0.3981 nM 9.40
CHEMBL496520 Ki = 0.3981 nM 9.40
CHEMBL489393 Ki = 0.3981 nM 9.40
CHEMBL521873 Ki = 0.5012 nM 9.30
CHEMBL495703 Ki = 1.585 nM 8.80
CHEMBL484059 Ki = 12.59 nM 7.90
CHEMBL523064 Ki = 25.12 nM 7.60