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Assay Detail

CHEMBL2078144

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

Functional
TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type S2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Solute carrier family 22 member 6 (CHEMBL1641347)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Interaction of human organic anion transporters with various cephalosporin antibiotics.
Takeda M, Babu E, Narikawa S, Endou H.
Eur J Pharmacol (2002) 438 : 137 -142
PubMed 11909604 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.39 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1146 CEFAMANDOLE 2.0 1 7.52
CHEMBL1435 CEFAZOLIN 4.0 1 6.75
CHEMBL507674 CEFOPERAZONE 4.0 1 6.68
CHEMBL617 CEPHALOTHIN 4.0 1 6.66
CHEMBL161 CEFTRIAXONE 4.0 1 6.64
CHEMBL316157 CEPHALORIDINE 4.0 1 6.13
CHEMBL1730 CEFOTAXIME 4.0 1 5.50
CHEMBL1644 CEFADROXIL 4.0 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1146 CEFAMANDOLE Ki = 30.0 nM 7.52
CHEMBL1435 CEFAZOLIN Ki = 180.0 nM 6.75
CHEMBL507674 CEFOPERAZONE Ki = 210.0 nM 6.68
CHEMBL617 CEPHALOTHIN Ki = 220.0 nM 6.66
CHEMBL161 CEFTRIAXONE Ki = 230.0 nM 6.64
CHEMBL316157 CEPHALORIDINE Ki = 740.0 nM 6.13
CHEMBL1730 CEFOTAXIME Ki = 3130.0 nM 5.50
CHEMBL1644 CEFADROXIL Ki = 6140.0 nM 5.21