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Assay Detail

CHEMBL2076201

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

Functional
TP_TRANSPORTER: inhibition of Gly-Sar uptake (pH6.0) in SKPT cells
31
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Solute carrier family 15 member 2 (CHEMBL3325)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
Luckner P, Brandsch M.
Eur J Pharm Biopharm (2005) 59 : 17 -24
PubMed 15567297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 4.55 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1644 CEFADROXIL 4.0 1 5.52
CHEMBL316157 CEPHALORIDINE 4.0 1 5.07
CHEMBL680 CEFACLOR ANHYDROUS 4.0 1 4.54
CHEMBL1200356 CYCLACILLIN 4.0 1 4.36
CHEMBL1604 CEPHRADINE 4.0 1 4.19
CHEMBL1727 CEPHALEXIN ANHYDROUS 4.0 1 4.12
CHEMBL74632 MOXALACTAM 4.0 1 4.06
CHEMBL3351077 CEFSULODIN 2.0 1 -
CHEMBL65794 CEFPIROME 2.0 1 -
CHEMBL161 CEFTRIAXONE 4.0 1 -
CHEMBL1599 CEPHAPIRIN 4.0 1 -
CHEMBL44354 CEFTAZIDIME 4.0 1 -
CHEMBL1730 CEFOTAXIME 4.0 1 -
CHEMBL1236749 1 -
CHEMBL186 CEFEPIME 4.0 1 -
CHEMBL29 PENICILLIN G 4.0 1 -
CHEMBL1436 CEFUROXIME 4.0 2 -
CHEMBL891 CLOXACILLIN 4.0 1 -
CHEMBL174 AMPICILLIN 4.0 1 -
CHEMBL1541 CEFIXIME 4.0 1 -
CHEMBL1146 CEFAMANDOLE 2.0 1 -
CHEMBL2303613 CEFODIZIME 2.0 1 -
CHEMBL819 OXACILLIN 4.0 1 -
CHEMBL893 DICLOXACILLIN 4.0 1 -
CHEMBL1201195 CEFMETAZOLE 4.0 1 -
CHEMBL1082 AMOXICILLIN 4.0 1 -
CHEMBL1615585 1 -
CHEMBL1908324 METAMPICILLIN 2.0 1 -
CHEMBL617 CEPHALOTHIN 4.0 1 -
CHEMBL1605 CEFTIBUTEN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1644 CEFADROXIL Ki = 3000.0 nM 5.52
CHEMBL316157 CEPHALORIDINE Ki = 8500.0 nM 5.07
CHEMBL680 CEFACLOR ANHYDROUS Ki = 29000.0 nM 4.54
CHEMBL1200356 CYCLACILLIN Ki = 44000.0 nM 4.36
CHEMBL1604 CEPHRADINE Ki = 65000.0 nM 4.19
CHEMBL1727 CEPHALEXIN ANHYDROUS Ki = 75000.0 nM 4.12
CHEMBL74632 MOXALACTAM Ki = 87000.0 nM 4.06
CHEMBL3351077 CEFSULODIN Ki > 30000000.0 nM -
CHEMBL65794 CEFPIROME Ki = 9500000.0 nM -
CHEMBL161 CEFTRIAXONE Ki > 20000000.0 nM -
CHEMBL1599 CEPHAPIRIN Ki > 10000000.0 nM -
CHEMBL44354 CEFTAZIDIME Ki > 10000000.0 nM -
CHEMBL1730 CEFOTAXIME Ki = 20000000.0 nM -
CHEMBL1236749 Ki = 19000000.0 nM -
CHEMBL1436 CEFUROXIME Ki = 12600000.0 nM -
CHEMBL186 CEFEPIME Ki = 11400000.0 nM -
CHEMBL29 PENICILLIN G Ki = 11100000.0 nM -
CHEMBL1436 CEFUROXIME Ki > 3000.0 nM -
CHEMBL891 CLOXACILLIN Ki = 950000.0 nM -
CHEMBL174 AMPICILLIN Ki = 1300000.0 nM -
CHEMBL1541 CEFIXIME Ki = 2600000.0 nM -
CHEMBL2303613 CEFODIZIME Ki = 9000000.0 nM -
CHEMBL1605 CEFTIBUTEN Ki = 280000.0 nM -
CHEMBL819 OXACILLIN Ki = 3300000.0 nM -
CHEMBL893 DICLOXACILLIN Ki = 420000.0 nM -
CHEMBL1201195 CEFMETAZOLE Ki = 4300000.0 nM -
CHEMBL1082 AMOXICILLIN Ki = 430000.0 nM -
CHEMBL1615585 Ki = 4900000.0 nM -
CHEMBL1908324 METAMPICILLIN Ki = 730000.0 nM -
CHEMBL617 CEPHALOTHIN Ki = 8300000.0 nM -
CHEMBL1146 CEFAMANDOLE Ki = 2800000.0 nM -