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Assay Detail

CHEMBL1913590

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Binding
Displacement of [3H]PK11195 from TSPO in Sprague-Dawley rat brain homogenates after 90 mins by liquid scintillation spectrometry
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Translocator protein (CHEMBL4552)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationship studies in translocator protein ligands based on a pyrazolo[3,4-b]quinoline scaffold.
Cappelli A, Bini G, Valenti S, Giuliani G, Paolino M, Anzini M, Vomero S, Giorgi G, Giordani A, Stasi LP, Makovec F, Ghelardini C, Di Cesare Mannelli L, Concas A, Porcu P, Biggio G.
J Med Chem (2011) 54 : 7165 -7175
PubMed 21916402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.56 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1911623 1 9.89
CHEMBL1911624 1 9.89
CHEMBL1911620 1 9.85
CHEMBL1911625 1 9.55
CHEMBL1911622 1 9.47
CHEMBL1911621 1 9.08
CHEMBL481537 PK-11195 1 8.89
CHEMBL1911606 1 8.74
CHEMBL1911616 1 8.17
CHEMBL1911619 1 7.80
CHEMBL1911607 1 7.77
CHEMBL1911600 1 7.19
CHEMBL1911615 1 7.06
CHEMBL1911603 1 7.05
CHEMBL1911618 1 7.05
CHEMBL1911613 1 6.96
CHEMBL1911605 1 6.93
CHEMBL1911617 1 6.84
CHEMBL1911604 1 6.82
CHEMBL1911601 1 6.75
CHEMBL1911609 1 6.66
CHEMBL1911610 1 6.52
CHEMBL1911611 1 6.16
CHEMBL1911608 1 6.05
CHEMBL1911602 1 5.86
CHEMBL1911614 1 5.64
CHEMBL1911612 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1911623 IC50 = 0.13 nM 9.89
CHEMBL1911624 IC50 = 0.13 nM 9.89
CHEMBL1911620 IC50 = 0.14 nM 9.85
CHEMBL1911625 IC50 = 0.28 nM 9.55
CHEMBL1911622 IC50 = 0.34 nM 9.47
CHEMBL1911621 IC50 = 0.83 nM 9.08
CHEMBL481537 PK-11195 IC50 = 1.3 nM 8.89
CHEMBL1911606 IC50 = 1.8 nM 8.74
CHEMBL1911616 IC50 = 6.8 nM 8.17
CHEMBL1911619 IC50 = 16.0 nM 7.80
CHEMBL1911607 IC50 = 17.0 nM 7.77
CHEMBL1911600 IC50 = 65.0 nM 7.19
CHEMBL1911615 IC50 = 87.0 nM 7.06
CHEMBL1911603 IC50 = 90.0 nM 7.05
CHEMBL1911618 IC50 = 90.0 nM 7.05
CHEMBL1911613 IC50 = 110.0 nM 6.96
CHEMBL1911605 IC50 = 117.0 nM 6.93
CHEMBL1911617 IC50 = 144.0 nM 6.84
CHEMBL1911604 IC50 = 152.0 nM 6.82
CHEMBL1911601 IC50 = 180.0 nM 6.75
CHEMBL1911609 IC50 = 220.0 nM 6.66
CHEMBL1911610 IC50 = 304.0 nM 6.52
CHEMBL1911611 IC50 = 697.0 nM 6.16
CHEMBL1911608 IC50 = 881.0 nM 6.05
CHEMBL1911602 IC50 = 1392.0 nM 5.86
CHEMBL1911614 IC50 = 2271.0 nM 5.64
CHEMBL1911612 IC50 = 3464.0 nM 5.46