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Assay Detail

CHEMBL4670708

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

Binding
Inhibition of LDHA in human MIA PaCa-2 cells assessed as decrease in lactate production incubated for 2 hrs by lactate oxidase-coupled fluorescence based assay
ChEMBL ↗
89
Total Activities
89
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MIA PaCa-2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

L-lactate dehydrogenase A chain (CHEMBL4835) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrazole-Based Lactate Dehydrogenase Inhibitors with Optimized Cell Activity and Pharmacokinetic Properties.
Rai G,Urban DJ,Mott BT,Hu X,Yang SM,Benavides GA,Johnson MS,Squadrito GL,Brimacombe KR,Lee TD,Cheff DM,Zhu H,Henderson MJ,Pohida K,Sulikowski GA,Dranow DM,Kabir M,Shah P,Padilha E,Tao D,Fang Y,Christov PP,Kim K,Jana S,Muttil P,Anderson T,Kunda NK,Hathaway HJ,Kusewitt DF,Oshima N,Cherukuri M,Davies DR,Norenberg JP,Sklar LA,Moore WJ,Dang CV,Stott GM,Neckers L,Flint AJ,Darley-Usmar VM,Simeonov A,Waterson AG,Jadhav A,Hall MD,Maloney DJ
J Med Chem (2020) 63 : 10984 -11011
PubMed 32902275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 89 6.17 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4784731 — — 1 6.86
CHEMBL4764953 — — 1 6.83
CHEMBL4758255 — — 1 6.76
CHEMBL4759404 — — 1 6.73
CHEMBL4747737 — — 1 6.71
CHEMBL4792760 — — 1 6.69
CHEMBL4751956 — — 1 6.66
CHEMBL4764044 — — 1 6.66
CHEMBL4754755 — — 1 6.64
CHEMBL4788048 — — 1 6.60
CHEMBL4753360 — — 1 6.59
CHEMBL4742726 — — 1 6.59
CHEMBL4744588 — — 1 6.59
CHEMBL4751209 — — 1 6.55
CHEMBL4747960 — — 1 6.54
CHEMBL4762840 — — 1 6.53
CHEMBL4791940 — — 1 6.51
CHEMBL4752751 — — 1 6.49
CHEMBL4782843 — — 1 6.48
CHEMBL4294999 — — 1 6.48
CHEMBL4785391 — — 1 6.48
CHEMBL4778221 — — 1 6.47
CHEMBL4752866 — — 1 6.44
CHEMBL4753379 — — 1 6.43
CHEMBL4745150 — — 1 6.42
CHEMBL4799344 — — 1 6.41
CHEMBL4752366 — — 1 6.39
CHEMBL4748782 — — 1 6.39
CHEMBL4786289 — — 1 6.39
CHEMBL4779276 — — 1 6.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4784731 — IC50 = 137.0 nM 6.86
CHEMBL4764953 — IC50 = 149.0 nM 6.83
CHEMBL4758255 — IC50 = 172.0 nM 6.76
CHEMBL4759404 — IC50 = 188.0 nM 6.73
CHEMBL4747737 — IC50 = 197.0 nM 6.71
CHEMBL4792760 — IC50 = 203.0 nM 6.69
CHEMBL4751956 — IC50 = 218.0 nM 6.66
CHEMBL4764044 — IC50 = 218.0 nM 6.66
CHEMBL4754755 — IC50 = 231.0 nM 6.64
CHEMBL4788048 — IC50 = 253.0 nM 6.60
CHEMBL4753360 — IC50 = 255.0 nM 6.59
CHEMBL4742726 — IC50 = 259.0 nM 6.59
CHEMBL4744588 — IC50 = 254.0 nM 6.59
CHEMBL4751209 — IC50 = 281.0 nM 6.55
CHEMBL4747960 — IC50 = 286.0 nM 6.54
CHEMBL4762840 — IC50 = 298.0 nM 6.53
CHEMBL4791940 — IC50 = 307.0 nM 6.51
CHEMBL4752751 — IC50 = 321.0 nM 6.49
CHEMBL4782843 — IC50 = 333.0 nM 6.48
CHEMBL4294999 — IC50 = 331.0 nM 6.48
CHEMBL4785391 — IC50 = 334.0 nM 6.48
CHEMBL4778221 — IC50 = 337.0 nM 6.47
CHEMBL4752866 — IC50 = 361.0 nM 6.44
CHEMBL4753379 — IC50 = 367.0 nM 6.43
CHEMBL4745150 — IC50 = 379.0 nM 6.42
CHEMBL4799344 — IC50 = 387.0 nM 6.41
CHEMBL4748782 — IC50 = 403.0 nM 6.39
CHEMBL4786289 — IC50 = 409.0 nM 6.39
CHEMBL4752366 — IC50 = 408.0 nM 6.39
CHEMBL4779276 — IC50 = 417.0 nM 6.38
CHEMBL4793796 — IC50 = 417.0 nM 6.38
CHEMBL4762895 — IC50 = 417.0 nM 6.38
CHEMBL4754861 — IC50 = 432.0 nM 6.37
CHEMBL4787852 — IC50 = 424.0 nM 6.37
CHEMBL4786241 — IC50 = 428.0 nM 6.37
CHEMBL4756159 — IC50 = 434.0 nM 6.36
CHEMBL4787940 — IC50 = 450.0 nM 6.35
CHEMBL4740977 — IC50 = 450.0 nM 6.35
CHEMBL4758312 — IC50 = 459.0 nM 6.34
CHEMBL4777976 — IC50 = 454.0 nM 6.34
CHEMBL4762989 — IC50 = 470.0 nM 6.33
CHEMBL4784359 — IC50 = 487.0 nM 6.31
CHEMBL4761628 — IC50 = 487.0 nM 6.31
CHEMBL4745734 — IC50 = 491.0 nM 6.31
CHEMBL4784520 — IC50 = 487.0 nM 6.31
CHEMBL4753493 — IC50 = 507.0 nM 6.29
CHEMBL4759279 — IC50 = 515.0 nM 6.29
CHEMBL4783945 — IC50 = 525.0 nM 6.28
CHEMBL4783252 — IC50 = 525.0 nM 6.28
CHEMBL4799233 — IC50 = 547.0 nM 6.26