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Assay Detail

CHEMBL961473

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Binding
Binding affinity to human PBR
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Translocator protein (CHEMBL5742)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor.
Yu W, Wang E, Voll RJ, Miller AH, Goodman MM.
Bioorg Med Chem (2008) 16 : 6145 -6155
PubMed 18472268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 8.45 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481537 PK-11195 1 8.70
CHEMBL517539 1 8.46
CHEMBL63154 1 8.40
CHEMBL286346 RO-54864 1 8.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481537 PK-11195 Kd = 2.0 nM 8.70
CHEMBL517539 Kd = 3.5 nM 8.46
CHEMBL63154 Kd = 4.0 nM 8.40
CHEMBL286346 RO-54864 Kd = 6.0 nM 8.22