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Assay Detail

CHEMBL650286

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Binding
Displacement of [3H]-PK 11195 from rat peripheral (mitochondrial) benzodiazepine receptor
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A comparative molecular field analysis model for 6-arylpyrrolo[2,1-d] [1,5]benzothiazepines binding selectively to the mitochondrial benzodiazepine receptor.
Greco G, Novellino E, Fiorini I, Nacci V, Campiani G, Ciani SM, Garofalo A, Bernasconi P, Mennini T.
J Med Chem (1994) 37 : 4100 -4108
PubMed 7990110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.38 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL117589 — — 1 8.40
CHEMBL285078 — — 1 8.12
CHEMBL33096 — — 1 8.04
CHEMBL288551 — — 1 8.04
CHEMBL33083 — — 1 7.71
CHEMBL284532 — — 1 7.69
CHEMBL284623 — — 1 7.67
CHEMBL416214 — — 1 7.63
CHEMBL33609 — — 1 7.56
CHEMBL335287 — — 1 7.55
CHEMBL32716 — — 1 7.53
CHEMBL116087 — — 1 7.52
CHEMBL133406 — — 1 7.51
CHEMBL33165 — — 1 7.47
CHEMBL133407 — — 1 7.42
CHEMBL416040 — — 1 7.32
CHEMBL34048 — — 1 7.24
CHEMBL32254 — — 1 7.18
CHEMBL286909 — — 1 7.02
CHEMBL324500 — — 1 6.95
CHEMBL33999 — — 1 6.78
CHEMBL286225 — — 1 6.64
CHEMBL287390 — — 1 6.62
CHEMBL284154 — — 1 6.57
CHEMBL33641 — — 1 6.53
CHEMBL286381 — — 1 6.31
CHEMBL33042 — — 1 6.25
CHEMBL33530 — — 1 6.20
CHEMBL32657 — — 1 6.19
CHEMBL326066 — — 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL117589 — IC50 = 3.981 nM 8.40
CHEMBL285078 — IC50 = 7.586 nM 8.12
CHEMBL288551 — IC50 = 9.12 nM 8.04
CHEMBL33096 — IC50 = 9.12 nM 8.04
CHEMBL33083 — IC50 = 19.5 nM 7.71
CHEMBL284532 — IC50 = 20.42 nM 7.69
CHEMBL284623 — IC50 = 21.38 nM 7.67
CHEMBL416214 — IC50 = 23.44 nM 7.63
CHEMBL33609 — IC50 = 27.54 nM 7.56
CHEMBL335287 — IC50 = 28.18 nM 7.55
CHEMBL32716 — IC50 = 29.51 nM 7.53
CHEMBL116087 — IC50 = 30.2 nM 7.52
CHEMBL133406 — IC50 = 30.9 nM 7.51
CHEMBL33165 — IC50 = 33.88 nM 7.47
CHEMBL133407 — IC50 = 38.02 nM 7.42
CHEMBL416040 — IC50 = 47.86 nM 7.32
CHEMBL34048 — IC50 = 57.54 nM 7.24
CHEMBL32254 — IC50 = 66.07 nM 7.18
CHEMBL286909 — IC50 = 95.5 nM 7.02
CHEMBL324500 — IC50 = 112.2 nM 6.95
CHEMBL33999 — IC50 = 165.96 nM 6.78
CHEMBL286225 — IC50 = 229.09 nM 6.64
CHEMBL287390 — IC50 = 239.88 nM 6.62
CHEMBL284154 — IC50 = 269.15 nM 6.57
CHEMBL33641 — IC50 = 295.12 nM 6.53
CHEMBL286381 — IC50 = 489.78 nM 6.31
CHEMBL33042 — IC50 = 562.34 nM 6.25
CHEMBL33530 — IC50 = 630.96 nM 6.20
CHEMBL32657 — IC50 = 645.65 nM 6.19
CHEMBL326066 — IC50 = 676.08 nM 6.17
CHEMBL34056 — IC50 = 691.83 nM 6.16
CHEMBL33619 — IC50 = 812.83 nM 6.09
CHEMBL441964 — IC50 = 1148.15 nM 5.94
CHEMBL32718 — IC50 = 1230.27 nM 5.91
CHEMBL285555 — IC50 = 1412.54 nM 5.85
CHEMBL290787 — IC50 = 1819.7 nM 5.74
CHEMBL284232 — IC50 = 2089.3 nM 5.68
CHEMBL285068 — IC50 = 2089.3 nM 5.68
CHEMBL32765 — IC50 = 2951.21 nM 5.53
CHEMBL33488 — IC50 = 4570.88 nM 5.34
CHEMBL32268 — IC50 = 6165.95 nM 5.21
CHEMBL284130 — IC50 = 14791.08 nM 4.83
CHEMBL416406 — IC50 = 22908.68 nM 4.64
CHEMBL284371 — IC50 = 100000.0 nM 4.00
CHEMBL284279 — IC50 = 100000.0 nM 4.00
CHEMBL316826 — IC50 = 100000.0 nM 4.00
CHEMBL317219 — IC50 = 100000.0 nM 4.00
CHEMBL32647 — IC50 = 100000.0 nM 4.00
CHEMBL100175 — IC50 = 100000.0 nM 4.00