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Assay Detail

CHEMBL994692

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

Binding
Displacement of [3H]LSD from human recombinant 5HT6 receptor
54
Total Activities
54
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and SAR of tolylamine 5-HT6 antagonists.
Singer JM, Wilson MW, Johnson PD, Graham SR, Cooke LW, Roof RL, Boxer PA, Gold LH, Meltzer LT, Janssen A, Roush N, Campbell JE, Su TZ, Hurst SI, Stoner CL, Schwarz JB.
Bioorg Med Chem Lett (2009) 19 : 2409 -2412
PubMed 19346128 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 54 7.84 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483358 1 9.22
CHEMBL431298 1 9.18
CHEMBL483148 1 8.89
CHEMBL520638 1 8.82
CHEMBL482989 1 8.62
CHEMBL450673 1 8.60
CHEMBL527098 1 8.57
CHEMBL484164 1 8.55
CHEMBL485147 1 8.48
CHEMBL482937 1 8.46
CHEMBL482990 1 8.37
CHEMBL482737 1 8.24
CHEMBL482938 1 8.19
CHEMBL482988 1 8.19
CHEMBL506736 1 8.16
CHEMBL484009 1 8.09
CHEMBL483560 1 8.03
CHEMBL484533 1 8.00
CHEMBL483149 1 7.99
CHEMBL484337 1 7.98
CHEMBL482749 1 7.95
CHEMBL483559 1 7.94
CHEMBL519513 1 7.87
CHEMBL484534 1 7.82
CHEMBL483558 1 7.82
CHEMBL519536 1 7.75
CHEMBL519670 1 7.75
CHEMBL482541 1 7.74
CHEMBL484010 1 7.72
CHEMBL482939 1 7.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483358 Ki = 0.6 nM 9.22
CHEMBL431298 Ki = 0.66 nM 9.18
CHEMBL483148 Ki = 1.3 nM 8.89
CHEMBL520638 Ki = 1.5 nM 8.82
CHEMBL482989 Ki = 2.4 nM 8.62
CHEMBL450673 Ki = 2.5 nM 8.60
CHEMBL527098 Ki = 2.7 nM 8.57
CHEMBL484164 Ki = 2.8 nM 8.55
CHEMBL485147 Ki = 3.3 nM 8.48
CHEMBL482937 Ki = 3.5 nM 8.46
CHEMBL482990 Ki = 4.3 nM 8.37
CHEMBL482737 Ki = 5.8 nM 8.24
CHEMBL482938 Ki = 6.5 nM 8.19
CHEMBL482988 Ki = 6.4 nM 8.19
CHEMBL506736 Ki = 6.9 nM 8.16
CHEMBL484009 Ki = 8.1 nM 8.09
CHEMBL483560 Ki = 9.3 nM 8.03
CHEMBL484533 Ki = 10.1 nM 8.00
CHEMBL483149 Ki = 10.3 nM 7.99
CHEMBL484337 Ki = 10.5 nM 7.98
CHEMBL482749 Ki = 11.3 nM 7.95
CHEMBL483559 Ki = 11.6 nM 7.94
CHEMBL519513 Ki = 13.6 nM 7.87
CHEMBL484534 Ki = 15.1 nM 7.82
CHEMBL483558 Ki = 15.3 nM 7.82
CHEMBL519536 Ki = 17.9 nM 7.75
CHEMBL519670 Ki = 17.8 nM 7.75
CHEMBL482541 Ki = 18.4 nM 7.74
CHEMBL484010 Ki = 19.1 nM 7.72
CHEMBL482939 Ki = 19.6 nM 7.71
CHEMBL484532 Ki = 24.7 nM 7.61
CHEMBL453732 Ki = 26.1 nM 7.58
CHEMBL482748 Ki = 28.9 nM 7.54
CHEMBL485531 Ki = 39.5 nM 7.40
CHEMBL485010 Ki = 39.8 nM 7.40
CHEMBL455332 Ki = 42.0 nM 7.38
CHEMBL484964 Ki = 45.6 nM 7.34
CHEMBL474089 Ki = 48.5 nM 7.31
CHEMBL475902 Ki = 50.0 nM 7.30
CHEMBL482568 Ki = 61.6 nM 7.21
CHEMBL484965 Ki = 70.7 nM 7.15
CHEMBL484608 Ki = 92.5 nM 7.03
CHEMBL482573 Ki = 126.0 nM 6.90
CHEMBL452402 Ki = 174.0 nM 6.76
CHEMBL485016 Ki = 208.0 nM 6.68
CHEMBL519359 Ki = 219.0 nM 6.66
CHEMBL474088 Ki = 239.0 nM 6.62
CHEMBL449581 Ki > 440.0 nM -
CHEMBL484008 Ki > 440.0 nM -
CHEMBL475901 Ki > 440.0 nM -