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Assay Detail

CHEMBL886472

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

Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor expressed in HEK293 cells
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

5-hydroxytryptamine receptor 6 (CHEMBL3371)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3,4-Dihydro-2H-benzo[1,4]oxazine derivatives as 5-HT6 receptor antagonists.
Zhao SH, Berger J, Clark RD, Sethofer SG, Krauss NE, Brothers JM, Martin RS, Misner DL, Schwab D, Alexandrova L.
Bioorg Med Chem Lett (2007) 17 : 3504 -3507
PubMed 17485206 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 8.53 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL398034 1 10.20
CHEMBL394690 1 9.80
CHEMBL246918 1 9.50
CHEMBL246706 1 9.40
CHEMBL246705 1 9.40
CHEMBL246499 1 9.40
CHEMBL246291 1 9.30
CHEMBL246704 1 9.20
CHEMBL394691 1 9.20
CHEMBL246498 1 9.20
CHEMBL398036 1 9.10
CHEMBL246917 1 8.90
CHEMBL246078 1 8.90
CHEMBL246500 1 8.70
CHEMBL246079 1 8.70
CHEMBL394689 1 8.60
CHEMBL398035 1 8.50
CHEMBL247121 1 8.40
CHEMBL394949 1 8.40
CHEMBL438675 1 8.30
CHEMBL246916 1 8.10
CHEMBL246080 1 8.00
CHEMBL246077 1 7.90
CHEMBL247120 1 7.40
CHEMBL247325 1 6.90
CHEMBL246289 1 6.70
CHEMBL246290 1 6.50
CHEMBL247119 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398034 Ki = 0.0631 nM 10.20
CHEMBL394690 Ki = 0.1585 nM 9.80
CHEMBL246918 Ki = 0.3162 nM 9.50
CHEMBL246706 Ki = 0.3981 nM 9.40
CHEMBL246705 Ki = 0.3981 nM 9.40
CHEMBL246499 Ki = 0.3981 nM 9.40
CHEMBL246291 Ki = 0.5012 nM 9.30
CHEMBL246704 Ki = 0.631 nM 9.20
CHEMBL394691 Ki = 0.631 nM 9.20
CHEMBL246498 Ki = 0.631 nM 9.20
CHEMBL398036 Ki = 0.7943 nM 9.10
CHEMBL246917 Ki = 1.259 nM 8.90
CHEMBL246078 Ki = 1.259 nM 8.90
CHEMBL246500 Ki = 1.995 nM 8.70
CHEMBL246079 Ki = 1.995 nM 8.70
CHEMBL394689 Ki = 2.512 nM 8.60
CHEMBL398035 Ki = 3.162 nM 8.50
CHEMBL247121 Ki = 3.981 nM 8.40
CHEMBL394949 Ki = 3.981 nM 8.40
CHEMBL438675 Ki = 5.012 nM 8.30
CHEMBL246916 Ki = 7.943 nM 8.10
CHEMBL246080 Ki = 10.0 nM 8.00
CHEMBL246077 Ki = 12.59 nM 7.90
CHEMBL247120 Ki = 39.81 nM 7.40
CHEMBL247325 Ki = 125.89 nM 6.90
CHEMBL246289 Ki = 199.53 nM 6.70
CHEMBL246290 Ki = 316.23 nM 6.50
CHEMBL247119 Ki = 630.96 nM 6.20