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Assay Detail

CHEMBL663693

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

ADMET
Inhibition of heterologously expressed human Cytochrome P450 1A2 at 500 uM
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
Bromidge SM, Duckworth M, Forbes IT, Ham P, King FD, Thewlis KM, Blaney FE, Naylor CB, Blackburn TP, Kennett GA, Wood MD, Clarke SE.
J Med Chem (1997) 40 : 3494 -3496
PubMed 9357513 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.60 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276140 1 7.89
CHEMBL297784 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276140 IC50 = 13.0 nM 7.89
CHEMBL297784 IC50 = 50.0 nM 7.30