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Assay Detail

CHEMBL763472

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

Functional
Displacement of [3H]TCP from PCP receptor in tissue preparation of whole rat brain minus cerebellum.
45
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Brain
Confidence 1 — Organism
Curated By Expert

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Analogues of the dioxolanes dexoxadrol and etoxadrol as potential phencyclidine-like agents. Synthesis and structure-activity relationships.
Thurkauf A, Mattson MV, Richardson S, Mirsadeghi S, Ornstein PL, Harrison EA, Rice KC, Jacobson AE, Monn JA.
J Med Chem (1992) 35 : 1323 -1329
PubMed 1349351 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 5.89 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL287572 1 7.92
CHEMBL26639 1 7.84
CHEMBL26714 1 7.44
CHEMBL281422 1 7.35
CHEMBL280739 1 7.23
CHEMBL284666 1 7.16
CHEMBL275528 PHENCYCLIDINE 2.0 1 7.10
CHEMBL305904 ETOXADROL 2.0 1 6.97
CHEMBL1165411 DEXOXADROL 2.0 1 6.95
CHEMBL282809 1 6.91
CHEMBL26985 1 6.70
CHEMBL287645 1 6.69
CHEMBL284404 1 6.53
CHEMBL281053 1 6.49
CHEMBL26022 1 6.31
CHEMBL282383 1 6.23
CHEMBL28121 1 6.22
CHEMBL416562 1 6.19
CHEMBL282598 1 6.15
CHEMBL417117 1 6.07
CHEMBL284633 1 5.91
CHEMBL26840 1 5.88
CHEMBL26735 1 5.85
CHEMBL284413 1 5.55
CHEMBL412875 1 5.48
CHEMBL424408 1 5.46
CHEMBL26481 1 5.36
CHEMBL430915 1 5.17
CHEMBL27946 1 5.16
CHEMBL287654 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL287572 Ki = 12.0 nM 7.92
CHEMBL26639 Ki = 14.3 nM 7.84
CHEMBL26714 Ki = 36.0 nM 7.44
CHEMBL281422 Ki = 45.0 nM 7.35
CHEMBL280739 Ki = 59.0 nM 7.23
CHEMBL284666 Ki = 69.0 nM 7.16
CHEMBL275528 PHENCYCLIDINE Ki = 80.0 nM 7.10
CHEMBL305904 ETOXADROL Ki = 107.0 nM 6.97
CHEMBL1165411 DEXOXADROL Ki = 112.0 nM 6.95
CHEMBL282809 Ki = 124.0 nM 6.91
CHEMBL26985 Ki = 200.0 nM 6.70
CHEMBL287645 Ki = 205.0 nM 6.69
CHEMBL284404 Ki = 293.0 nM 6.53
CHEMBL281053 Ki = 325.0 nM 6.49
CHEMBL26022 Ki = 489.0 nM 6.31
CHEMBL282383 Ki = 590.0 nM 6.23
CHEMBL28121 Ki = 607.0 nM 6.22
CHEMBL416562 Ki = 649.0 nM 6.19
CHEMBL282598 Ki = 703.0 nM 6.15
CHEMBL417117 Ki = 847.0 nM 6.07
CHEMBL284633 Ki = 1230.0 nM 5.91
CHEMBL26840 Ki = 1320.0 nM 5.88
CHEMBL26735 Ki = 1400.0 nM 5.85
CHEMBL284413 Ki = 2800.0 nM 5.55
CHEMBL412875 Ki = 3300.0 nM 5.48
CHEMBL424408 Ki = 3450.0 nM 5.46
CHEMBL26481 Ki = 4400.0 nM 5.36
CHEMBL430915 Ki = 6800.0 nM 5.17
CHEMBL287654 Ki = 6900.0 nM 5.16
CHEMBL27946 Ki = 7000.0 nM 5.16
CHEMBL26724 Ki = 7300.0 nM 5.14
CHEMBL27050 Ki = 8300.0 nM 5.08
CHEMBL28119 Ki = 8400.0 nM 5.08
CHEMBL283893 Ki = 9000.0 nM 5.05
CHEMBL263720 Ki = 10100.0 nM 5.00
CHEMBL27830 Ki = 15200.0 nM 4.82
CHEMBL442107 Ki = 15500.0 nM 4.81
CHEMBL27595 Ki = 19900.0 nM 4.70
CHEMBL284186 Ki = 21200.0 nM 4.67
CHEMBL432263 Ki = 25000.0 nM 4.60
CHEMBL26849 Ki = 43000.0 nM 4.37
CHEMBL27050 Ki = 52000.0 nM 4.28
CHEMBL25962 Ki = 87000.0 nM 4.06
CHEMBL28065 Ki > 100000.0 nM -
CHEMBL283825 Ki > 10000.0 nM -