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Assay Detail

CHEMBL617147

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

Binding
Binding affinity for serotonin 5-hydroxytryptamine 2 receptor using [3H]ketanserin in guinea pig frontal cortex
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Frontal cortex
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2095200)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Piperidinyltetralin sigma ligands.
Gilligan PJ, Kergaye AA, Lewis BM, McElroy JF.
J Med Chem (1994) 37 : 364 -370
PubMed 7905926 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 33 6.78 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542942 1 8.38
CHEMBL330865 1 8.15
CHEMBL331470 1 8.15
CHEMBL545058 1 8.15
CHEMBL539288 1 8.14
CHEMBL543889 1 8.05
CHEMBL553311 1 8.00
CHEMBL543412 1 7.82
CHEMBL554873 1 7.80
CHEMBL124234 1 7.28
CHEMBL542709 1 7.04
CHEMBL122538 1 7.00
CHEMBL122761 1 6.92
CHEMBL124411 1 6.75
CHEMBL331172 1 6.74
CHEMBL552572 1 6.63
CHEMBL554874 1 6.58
CHEMBL543176 1 6.58
CHEMBL122165 1 6.56
CHEMBL123014 1 6.55
CHEMBL544594 1 6.53
CHEMBL545287 1 6.49
CHEMBL542217 1 6.44
CHEMBL544123 1 6.30
CHEMBL122758 1 5.86
CHEMBL123937 1 5.71
CHEMBL303336 1 5.71
CHEMBL275707 RIMCAZOLE 2.0 1 5.61
CHEMBL545285 1 5.35
CHEMBL542462 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542942 Ki = 4.2 nM 8.38
CHEMBL330865 Ki = 7.0 nM 8.15
CHEMBL545058 Ki = 7.0 nM 8.15
CHEMBL331470 Ki = 7.0 nM 8.15
CHEMBL539288 Ki = 7.3 nM 8.14
CHEMBL543889 Ki = 9.0 nM 8.05
CHEMBL553311 Ki = 10.0 nM 8.00
CHEMBL543412 Ki = 15.0 nM 7.82
CHEMBL554873 Ki = 16.0 nM 7.80
CHEMBL124234 Ki = 52.0 nM 7.28
CHEMBL542709 Ki = 91.0 nM 7.04
CHEMBL122538 Ki = 101.0 nM 7.00
CHEMBL122761 Ki = 119.0 nM 6.92
CHEMBL124411 Ki = 176.0 nM 6.75
CHEMBL331172 Ki = 183.0 nM 6.74
CHEMBL552572 Ki = 233.0 nM 6.63
CHEMBL554874 Ki = 264.0 nM 6.58
CHEMBL543176 Ki = 260.0 nM 6.58
CHEMBL122165 Ki = 276.0 nM 6.56
CHEMBL123014 Ki = 282.0 nM 6.55
CHEMBL544594 Ki = 294.0 nM 6.53
CHEMBL545287 Ki = 326.0 nM 6.49
CHEMBL542217 Ki = 365.0 nM 6.44
CHEMBL544123 Ki = 502.0 nM 6.30
CHEMBL122758 Ki = 1378.0 nM 5.86
CHEMBL123937 Ki = 1969.0 nM 5.71
CHEMBL303336 Ki = 1934.0 nM 5.71
CHEMBL275707 RIMCAZOLE Ki = 2482.0 nM 5.61
CHEMBL545285 Ki = 4448.0 nM 5.35
CHEMBL542462 Ki = 5358.0 nM 5.27
CHEMBL542946 Ki = 6275.0 nM 5.20
CHEMBL123488 Ki = 6336.0 nM 5.20
CHEMBL554437 Ki > 10000.0 nM -