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Assay Detail

CHEMBL826384

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

Binding
Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells
76
Total Activities
75
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 Expert

Target

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

Publication

Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
Holenz J, Mercè R, Díaz JL, Guitart X, Codony X, Dordal A, Romero G, Torrens A, Mas J, Andaluz B, Hernández S, Monroy X, Sánchez E, Hernández E, Pérez R, Cubí R, Sanfeliu O, Buschmann H.
J Med Chem (2005) 48 : 1781 -1795
PubMed 15771424 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 76 7.71 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL368209 1 10.00
CHEMBL175835 1 9.70
CHEMBL179926 1 9.52
CHEMBL179408 1 9.40
CHEMBL179407 1 9.30
CHEMBL431298 1 9.10
CHEMBL368390 1 9.10
CHEMBL369759 1 9.00
CHEMBL362063 1 9.00
CHEMBL175940 1 8.72
CHEMBL362628 1 8.66
CHEMBL176028 1 8.48
CHEMBL180425 1 8.46
CHEMBL176292 1 8.41
CHEMBL175884 1 8.40
CHEMBL427134 1 8.37
CHEMBL367867 1 8.35
CHEMBL361230 1 8.33
CHEMBL175471 2 8.28
CHEMBL177605 1 8.28
CHEMBL180582 1 8.17
CHEMBL175529 1 8.14
CHEMBL177124 1 8.03
CHEMBL367481 1 8.02
CHEMBL367088 1 8.01
CHEMBL46071 1 7.83
CHEMBL176117 1 7.83
CHEMBL179492 1 7.82
CHEMBL176218 1 7.74
CHEMBL179006 1 7.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL368209 Ki = 0.1 nM 10.00
CHEMBL175835 Ki = 0.2 nM 9.70
CHEMBL179926 Ki = 0.3 nM 9.52
CHEMBL179408 Ki = 0.4 nM 9.40
CHEMBL179407 Ki = 0.5 nM 9.30
CHEMBL431298 Ki = 0.8 nM 9.10
CHEMBL368390 Ki = 0.8 nM 9.10
CHEMBL369759 Ki = 1.0 nM 9.00
CHEMBL362063 Ki = 1.0 nM 9.00
CHEMBL175940 Ki = 1.9 nM 8.72
CHEMBL362628 Ki = 2.2 nM 8.66
CHEMBL176028 Ki = 3.3 nM 8.48
CHEMBL180425 Ki = 3.5 nM 8.46
CHEMBL176292 Ki = 3.9 nM 8.41
CHEMBL175884 Ki = 4.0 nM 8.40
CHEMBL427134 Ki = 4.3 nM 8.37
CHEMBL367867 Ki = 4.5 nM 8.35
CHEMBL361230 Ki = 4.7 nM 8.33
CHEMBL175471 Ki = 5.3 nM 8.28
CHEMBL177605 Ki = 5.3 nM 8.28
CHEMBL180582 Ki = 6.8 nM 8.17
CHEMBL175529 Ki = 7.2 nM 8.14
CHEMBL177124 Ki = 9.3 nM 8.03
CHEMBL367481 Ki = 9.6 nM 8.02
CHEMBL367088 Ki = 9.8 nM 8.01
CHEMBL46071 Ki = 14.8 nM 7.83
CHEMBL176117 Ki = 14.9 nM 7.83
CHEMBL179492 Ki = 15.1 nM 7.82
CHEMBL176218 Ki = 18.4 nM 7.74
CHEMBL179006 Ki = 18.6 nM 7.73
CHEMBL179344 Ki = 19.8 nM 7.70
CHEMBL368959 Ki = 21.2 nM 7.67
CHEMBL367730 Ki = 24.3 nM 7.61
CHEMBL367305 Ki = 31.4 nM 7.50
CHEMBL175471 Ki = 40.8 nM 7.39
CHEMBL368871 Ki = 41.2 nM 7.38
CHEMBL433461 Ki = 44.7 nM 7.35
CHEMBL179034 Ki = 51.7 nM 7.29
CHEMBL367832 Ki = 52.2 nM 7.28
CHEMBL354418 Ki = 55.2 nM 7.26
CHEMBL368973 Ki = 57.7 nM 7.24
CHEMBL353739 Ki = 57.7 nM 7.24
CHEMBL175819 Ki = 64.7 nM 7.19
CHEMBL368069 Ki = 74.5 nM 7.13
CHEMBL175906 Ki = 74.6 nM 7.13
CHEMBL177119 Ki = 85.8 nM 7.07
CHEMBL579981 Ki = 90.2 nM 7.04
CHEMBL180110 Ki = 94.2 nM 7.03
CHEMBL2112986 Ki = 97.3 nM 7.01
CHEMBL177005 Ki = 100.8 nM 7.00