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Assay Detail

CHEMBL617210

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

Binding
In vitro binding affinity for serotonin 5-hydroxytryptamine (5-HT) 2 receptors
104
Total Activities
104
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2096671)
Type PROTEIN FAMILY
Organism Mus musculus

Publication

Novel piperidine sigma receptor ligands as potential antipsychotic drugs.
Gilligan PJ, Cain GA, Christos TE, Cook L, Drummond S, Johnson AL, Kergaye AA, McElroy JF, Rohrbach KW, Schmidt WK.
J Med Chem (1992) 35 : 4344 -4361
PubMed 1360026 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 104 6.83 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL136794 1 8.48
CHEMBL136064 1 8.44
CHEMBL138281 1 8.22
CHEMBL134527 1 8.10
CHEMBL139963 1 8.08
CHEMBL335327 1 8.05
CHEMBL337337 1 8.00
CHEMBL544616 1 7.92
CHEMBL543412 1 7.82
CHEMBL136615 1 7.82
CHEMBL136509 1 7.77
CHEMBL342267 1 7.70
CHEMBL137085 1 7.62
CHEMBL136963 1 7.62
CHEMBL545552 1 7.60
CHEMBL555865 1 7.58
CHEMBL136768 1 7.58
CHEMBL539358 1 7.55
CHEMBL136381 1 7.51
CHEMBL540322 1 7.50
CHEMBL136835 1 7.42
CHEMBL539302 1 7.40
CHEMBL538532 1 7.39
CHEMBL136701 1 7.39
CHEMBL137658 1 7.33
CHEMBL139110 1 7.28
CHEMBL137159 1 7.26
CHEMBL136622 1 7.19
CHEMBL543439 1 7.06
CHEMBL136621 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL136794 Ki = 3.3 nM 8.48
CHEMBL136064 Ki = 3.6 nM 8.44
CHEMBL138281 Ki = 6.0 nM 8.22
CHEMBL134527 Ki = 8.0 nM 8.10
CHEMBL139963 Ki = 8.4 nM 8.08
CHEMBL335327 Ki = 9.0 nM 8.05
CHEMBL337337 Ki = 10.0 nM 8.00
CHEMBL544616 Ki = 12.0 nM 7.92
CHEMBL136615 Ki = 15.0 nM 7.82
CHEMBL543412 Ki = 15.0 nM 7.82
CHEMBL136509 Ki = 17.0 nM 7.77
CHEMBL342267 Ki = 20.0 nM 7.70
CHEMBL137085 Ki = 24.0 nM 7.62
CHEMBL136963 Ki = 24.0 nM 7.62
CHEMBL545552 Ki = 25.0 nM 7.60
CHEMBL136768 Ki = 26.0 nM 7.58
CHEMBL555865 Ki = 26.0 nM 7.58
CHEMBL539358 Ki = 28.0 nM 7.55
CHEMBL136381 Ki = 31.0 nM 7.51
CHEMBL540322 Ki = 32.0 nM 7.50
CHEMBL136835 Ki = 38.0 nM 7.42
CHEMBL539302 Ki = 40.0 nM 7.40
CHEMBL136701 Ki = 41.0 nM 7.39
CHEMBL538532 Ki = 41.0 nM 7.39
CHEMBL137658 Ki = 47.0 nM 7.33
CHEMBL139110 Ki = 53.0 nM 7.28
CHEMBL137159 Ki = 55.0 nM 7.26
CHEMBL136622 Ki = 65.0 nM 7.19
CHEMBL543439 Ki = 87.0 nM 7.06
CHEMBL136621 Ki = 101.0 nM 7.00
CHEMBL423355 Ki = 112.0 nM 6.95
CHEMBL545549 Ki = 114.0 nM 6.94
CHEMBL342948 Ki = 116.0 nM 6.94
CHEMBL440345 Ki = 118.0 nM 6.93
CHEMBL542737 Ki = 127.0 nM 6.90
CHEMBL542246 Ki = 137.0 nM 6.86
CHEMBL424281 Ki = 173.0 nM 6.76
CHEMBL543440 Ki = 186.0 nM 6.73
CHEMBL539042 Ki = 187.0 nM 6.73
CHEMBL337148 Ki = 204.0 nM 6.69
CHEMBL136789 Ki = 208.0 nM 6.68
CHEMBL136395 Ki = 215.0 nM 6.67
CHEMBL554678 Ki = 224.0 nM 6.65
CHEMBL542740 Ki = 251.0 nM 6.60
CHEMBL337810 Ki = 260.0 nM 6.58
CHEMBL540578 Ki = 272.0 nM 6.57
CHEMBL136495 Ki = 272.0 nM 6.57
CHEMBL543917 Ki = 278.0 nM 6.56
CHEMBL539567 Ki = 281.0 nM 6.55
CHEMBL442965 Ki = 290.0 nM 6.54