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Assay Detail

CHEMBL5138280

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Functional
Inhibition of lactate production in human MIA PaCa-2 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MIA PaCa-2
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-based optimization of hydroxylactam as potent, cell-active inhibitors of lactate dehydrogenase.
Wei B, Robarge K, Labadie SS, Chen J, Corson LB, DiPasquale A, Dragovich PS, Eigenbrot C, Evangelista M, Fauber BP, Hitz A, Hong R, Lai KW, Liu W, Ma S, Malek S, O'Brien T, Pang J, Peterson D, Salphati L, Sampath D, Sideris S, Ultsch M, Xu Z, Yen I, Yu D, Yue Q, Zhou A, Purkey HE.
Bioorg Med Chem Lett (2022) 59 : 128576 -128576
PubMed 35065235 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.43 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201115 1 5.77
CHEMBL5183539 1 5.70
CHEMBL5181496 1 5.66
CHEMBL5188480 1 5.44
CHEMBL5194549 1 5.28
CHEMBL5196929 1 5.14
CHEMBL5202219 1 5.04
CHEMBL5171701 1 -
CHEMBL5196259 1 -
CHEMBL5185237 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201115 IC50 = 1700.0 nM 5.77
CHEMBL5183539 IC50 = 2000.0 nM 5.70
CHEMBL5181496 IC50 = 2200.0 nM 5.66
CHEMBL5188480 IC50 = 3600.0 nM 5.44
CHEMBL5194549 IC50 = 5300.0 nM 5.28
CHEMBL5196929 IC50 = 7200.0 nM 5.14
CHEMBL5202219 IC50 = 9100.0 nM 5.04
CHEMBL5171701 IC50 - -
CHEMBL5196259 IC50 - -
CHEMBL5185237 IC50 - -