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Assay Detail

CHEMBL4337306

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Binding
Displacement of [3H]PK11195 from human TSPO A147T mutant expressed in HEK293 cell membranes after 90 mins by scintillation counting method
30
Total Activities
30
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 Autocuration

Target

Translocator protein (CHEMBL5742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

First Nondiscriminating Translocator Protein Ligands Produced from a Carbazole Scaffold.
Cheng HWA, Sokias R, Werry EL, Ittner LM, Reekie TA, Du J, Gao Q, Hibbs DE, Kassiou M.
J Med Chem (2019) 62 : 8235 -8248
PubMed 31419132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 6.54 7.59

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4459176 1 7.59
CHEMBL416715 (R)PK-11195 1 7.57
CHEMBL4439049 1 7.00
CHEMBL4447335 1 6.88
CHEMBL4173118 1 6.75
CHEMBL4560218 1 6.68
CHEMBL4563441 1 6.67
CHEMBL4161842 1 6.50
CHEMBL4532562 1 6.43
CHEMBL4461372 1 6.38
CHEMBL4475609 1 6.33
CHEMBL4535242 1 6.19
CHEMBL4440548 1 5.81
CHEMBL4536533 1 5.77
CHEMBL4466212 1 5.50
CHEMBL4554031 1 -
CHEMBL4447625 1 -
CHEMBL4445371 1 -
CHEMBL4551915 1 -
CHEMBL4580702 1 -
CHEMBL4585880 1 -
CHEMBL4458416 1 -
CHEMBL4446805 1 -
CHEMBL4587084 1 -
CHEMBL4451744 1 -
CHEMBL4440106 1 -
CHEMBL4436847 1 -
CHEMBL4460152 1 -
CHEMBL4571475 1 -
CHEMBL4518499 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4459176 Ki = 25.4 nM 7.59
CHEMBL416715 (R)PK-11195 Ki = 26.7 nM 7.57
CHEMBL4439049 Ki = 100.4 nM 7.00
CHEMBL4447335 Ki = 132.0 nM 6.88
CHEMBL4173118 Ki = 176.6 nM 6.75
CHEMBL4560218 Ki = 208.4 nM 6.68
CHEMBL4563441 Ki = 214.0 nM 6.67
CHEMBL4161842 Ki = 318.5 nM 6.50
CHEMBL4532562 Ki = 369.0 nM 6.43
CHEMBL4461372 Ki = 418.2 nM 6.38
CHEMBL4475609 Ki = 462.3 nM 6.33
CHEMBL4535242 Ki = 639.4 nM 6.19
CHEMBL4440548 Ki = 1551.0 nM 5.81
CHEMBL4536533 Ki = 1696.0 nM 5.77
CHEMBL4466212 Ki = 3123.2 nM 5.50
CHEMBL4554031 Ki > 10000.0 nM -
CHEMBL4447625 Ki > 10000.0 nM -
CHEMBL4445371 Ki > 10000.0 nM -
CHEMBL4551915 Ki > 10000.0 nM -
CHEMBL4580702 Ki > 10000.0 nM -
CHEMBL4585880 Ki > 10000.0 nM -
CHEMBL4458416 Ki > 10000.0 nM -
CHEMBL4446805 Ki > 10000.0 nM -
CHEMBL4587084 Ki > 10000.0 nM -
CHEMBL4451744 Ki > 10000.0 nM -
CHEMBL4440106 Ki > 10000.0 nM -
CHEMBL4436847 Ki > 10000.0 nM -
CHEMBL4460152 Ki > 10000.0 nM -
CHEMBL4571475 Ki > 10000.0 nM -
CHEMBL4518499 Ki > 10000.0 nM -