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Assay Detail

CHEMBL980957

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Binding
Displacement of [3H]PK11195 from translocator protein in rat kidney mitochondrial membrane
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Kidney
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL4552) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
Da Settimo F, Simorini F, Taliani S, La Motta C, Marini AM, Salerno S, Bellandi M, Novellino E, Greco G, Cosimelli B, Da Pozzo E, Costa B, Simola N, Morelli M, Martini C.
J Med Chem (2008) 51 : 5798 -5806
PubMed 18729350 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 65 8.39 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL460998 — — 1 9.82
CHEMBL518789 — — 1 9.74
CHEMBL492686 — — 1 9.64
CHEMBL493301 — — 1 9.57
CHEMBL517895 — — 1 9.44
CHEMBL493705 — — 1 9.43
CHEMBL54349 ALPIDEM 4.0 1 9.30
CHEMBL518662 — — 1 9.26
CHEMBL55781 — — 1 9.21
CHEMBL492877 — — 1 9.02
CHEMBL523365 — — 1 9.02
CHEMBL492290 — — 1 9.00
CHEMBL462469 — — 1 9.00
CHEMBL492289 — — 1 8.94
CHEMBL459313 — — 1 8.89
CHEMBL461416 — — 1 8.88
CHEMBL294625 — — 1 8.85
CHEMBL517858 — — 1 8.78
CHEMBL462491 — — 1 8.78
CHEMBL523998 — — 1 8.77
CHEMBL460367 — — 1 8.74
CHEMBL459945 — — 1 8.72
CHEMBL461843 — — 1 8.64
CHEMBL461001 — — 1 8.62
CHEMBL461829 — — 1 8.58
CHEMBL492256 — — 1 8.57
CHEMBL461640 — — 1 8.55
CHEMBL54627 — — 1 8.55
CHEMBL461641 — — 1 8.52
CHEMBL461828 — — 1 8.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL460998 — Ki = 0.15 nM 9.82
CHEMBL518789 — Ki = 0.18 nM 9.74
CHEMBL492686 — Ki = 0.23 nM 9.64
CHEMBL493301 — Ki = 0.27 nM 9.57
CHEMBL517895 — Ki = 0.36 nM 9.44
CHEMBL493705 — Ki = 0.37 nM 9.43
CHEMBL54349 ALPIDEM Ki = 0.5 nM 9.30
CHEMBL518662 — Ki = 0.55 nM 9.26
CHEMBL55781 — Ki = 0.62 nM 9.21
CHEMBL492877 — Ki = 0.95 nM 9.02
CHEMBL523365 — Ki = 0.95 nM 9.02
CHEMBL492290 — Ki = 1.0 nM 9.00
CHEMBL462469 — Ki = 1.0 nM 9.00
CHEMBL492289 — Ki = 1.16 nM 8.94
CHEMBL459313 — Ki = 1.3 nM 8.89
CHEMBL461416 — Ki = 1.33 nM 8.88
CHEMBL294625 — Ki = 1.4 nM 8.85
CHEMBL517858 — Ki = 1.67 nM 8.78
CHEMBL462491 — Ki = 1.68 nM 8.78
CHEMBL523998 — Ki = 1.69 nM 8.77
CHEMBL460367 — Ki = 1.8 nM 8.74
CHEMBL459945 — Ki = 1.9 nM 8.72
CHEMBL461843 — Ki = 2.3 nM 8.64
CHEMBL461001 — Ki = 2.4 nM 8.62
CHEMBL461829 — Ki = 2.64 nM 8.58
CHEMBL492256 — Ki = 2.67 nM 8.57
CHEMBL54627 — Ki = 2.8 nM 8.55
CHEMBL461640 — Ki = 2.83 nM 8.55
CHEMBL461641 — Ki = 3.05 nM 8.52
CHEMBL461828 — Ki = 3.33 nM 8.48
CHEMBL516653 — Ki = 3.4 nM 8.47
CHEMBL462485 — Ki = 3.4 nM 8.47
CHEMBL462063 — Ki = 3.6 nM 8.44
CHEMBL460157 — Ki = 3.6 nM 8.44
CHEMBL460156 — Ki = 3.9 nM 8.41
CHEMBL461637 — Ki = 4.01 nM 8.40
CHEMBL523329 — Ki = 4.0 nM 8.40
CHEMBL492670 — Ki = 4.36 nM 8.36
CHEMBL461861 — Ki = 4.6 nM 8.34
CHEMBL294423 — Ki = 4.65 nM 8.33
CHEMBL461638 — Ki = 5.0 nM 8.30
CHEMBL461214 — Ki = 6.0 nM 8.22
CHEMBL522342 — Ki = 6.73 nM 8.17
CHEMBL431938 — Ki = 7.5 nM 8.12
CHEMBL518788 — Ki = 7.75 nM 8.11
CHEMBL481537 PK-11195 Ki = 9.3 nM 8.03
CHEMBL462268 — Ki = 9.54 nM 8.02
CHEMBL459946 — Ki = 11.0 nM 7.96
CHEMBL462062 — Ki = 11.0 nM 7.96
CHEMBL518189 — Ki = 12.1 nM 7.92