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Assay Detail

CHEMBL652453

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

Binding
Binding affinity against rat benzodiazepine (BZD) receptor
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Relating the structure, activity, and physical properties of ultrashort-acting benzodiazepine receptor agonists.
Pacofsky GJ, Stafford JA, Cox RF, Cowan JR, Dorsey GF, Gonzales SS, Kaldor I, Koszalka GW, Lovell GG, McIntyre MS, Tidwell JH, Todd D, Whitesell G, Wiard RP, Feldman PL.
Bioorg Med Chem Lett (2002) 12 : 3219 -3222
PubMed 12372538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.96 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL655 MIDAZOLAM 4.0 1 8.70
CHEMBL111633 1 8.15
CHEMBL108991 1 8.15
CHEMBL320277 1 8.15
CHEMBL321824 1 8.10
CHEMBL320728 1 7.96
CHEMBL325802 1 7.22
CHEMBL111056 1 7.10
CHEMBL109507 1 7.02
CHEMBL322701 1 7.01
CHEMBL111030 1 6.89
CHEMBL108446 1 6.86
CHEMBL111073 1 6.84
CHEMBL326440 1 6.68
CHEMBL321595 1 6.52
CHEMBL451 CHLORDIAZEPOXIDE 4.0 1 6.36
CHEMBL321596 1 6.10
CHEMBL109694 1 6.06
CHEMBL110953 1 6.00
CHEMBL111701 1 5.97
CHEMBL109187 1 5.91
CHEMBL108709 1 5.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL655 MIDAZOLAM Ki = 2.0 nM 8.70
CHEMBL111633 Ki = 7.0 nM 8.15
CHEMBL108991 Ki = 7.0 nM 8.15
CHEMBL320277 Ki = 7.0 nM 8.15
CHEMBL321824 Ki = 8.0 nM 8.10
CHEMBL320728 Ki = 11.0 nM 7.96
CHEMBL325802 Ki = 60.0 nM 7.22
CHEMBL111056 Ki = 79.0 nM 7.10
CHEMBL109507 Ki = 96.0 nM 7.02
CHEMBL322701 Ki = 98.0 nM 7.01
CHEMBL111030 Ki = 130.0 nM 6.89
CHEMBL108446 Ki = 139.0 nM 6.86
CHEMBL111073 Ki = 146.0 nM 6.84
CHEMBL326440 Ki = 208.0 nM 6.68
CHEMBL321595 Ki = 303.0 nM 6.52
CHEMBL451 CHLORDIAZEPOXIDE Ki = 438.0 nM 6.36
CHEMBL321596 Ki = 792.0 nM 6.10
CHEMBL109694 Ki = 875.0 nM 6.06
CHEMBL110953 Ki = 1012.0 nM 6.00
CHEMBL111701 Ki = 1075.0 nM 5.97
CHEMBL109187 Ki = 1230.0 nM 5.91
CHEMBL108709 Ki = 3572.0 nM 5.45