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Assay Detail

CHEMBL4670710

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

Binding
Inhibition of GS[HiBiT]GS-tagged LDHA (unknown origin) expressed in HEK-293T cells measured after 1 hr by CESTA
86
Total Activities
86
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK-293T
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 86 6.59 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4763797 1 7.42
CHEMBL4784731 1 7.12
CHEMBL4799233 1 7.10
CHEMBL4762895 1 7.08
CHEMBL4751495 1 7.08
CHEMBL4784520 1 7.05
CHEMBL4751209 1 7.05
CHEMBL4791940 1 7.05
CHEMBL4742726 1 7.05
CHEMBL4788048 1 7.05
CHEMBL4747300 1 7.05
CHEMBL4784359 1 7.05
CHEMBL4793796 1 7.02
CHEMBL4780015 1 7.02
CHEMBL4777976 1 7.02
CHEMBL4777867 1 7.00
CHEMBL4783367 1 7.00
CHEMBL4762840 1 6.97
CHEMBL4752866 1 6.97
CHEMBL4748782 1 6.97
CHEMBL4764953 1 6.97
CHEMBL4753360 1 6.95
CHEMBL4782843 1 6.95
CHEMBL4752366 1 6.95
CHEMBL4762989 1 6.95
CHEMBL4778221 1 6.95
CHEMBL4783945 1 6.92
CHEMBL4779276 1 6.92
CHEMBL4753379 1 6.92
CHEMBL4787940 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4763797 IC50 = 38.0 nM 7.42
CHEMBL4784731 IC50 = 75.0 nM 7.12
CHEMBL4799233 IC50 = 79.0 nM 7.10
CHEMBL4762895 IC50 = 84.0 nM 7.08
CHEMBL4751495 IC50 = 84.0 nM 7.08
CHEMBL4784359 IC50 = 89.0 nM 7.05
CHEMBL4747300 IC50 = 89.0 nM 7.05
CHEMBL4788048 IC50 = 90.0 nM 7.05
CHEMBL4742726 IC50 = 89.0 nM 7.05
CHEMBL4791940 IC50 = 89.0 nM 7.05
CHEMBL4751209 IC50 = 89.0 nM 7.05
CHEMBL4784520 IC50 = 90.0 nM 7.05
CHEMBL4793796 IC50 = 95.0 nM 7.02
CHEMBL4780015 IC50 = 95.0 nM 7.02
CHEMBL4777976 IC50 = 95.0 nM 7.02
CHEMBL4777867 IC50 = 100.0 nM 7.00
CHEMBL4783367 IC50 = 101.0 nM 7.00
CHEMBL4762840 IC50 = 106.0 nM 6.97
CHEMBL4752866 IC50 = 106.0 nM 6.97
CHEMBL4748782 IC50 = 106.0 nM 6.97
CHEMBL4764953 IC50 = 108.0 nM 6.97
CHEMBL4778221 IC50 = 113.0 nM 6.95
CHEMBL4762989 IC50 = 112.0 nM 6.95
CHEMBL4782843 IC50 = 112.0 nM 6.95
CHEMBL4753360 IC50 = 112.0 nM 6.95
CHEMBL4752366 IC50 = 113.0 nM 6.95
CHEMBL4783945 IC50 = 119.0 nM 6.92
CHEMBL4779276 IC50 = 119.0 nM 6.92
CHEMBL4753379 IC50 = 119.0 nM 6.92
CHEMBL4787940 IC50 = 119.0 nM 6.92
CHEMBL4740977 IC50 = 119.0 nM 6.92
CHEMBL4759378 IC50 = 126.0 nM 6.90
CHEMBL4763489 IC50 = 127.0 nM 6.90
CHEMBL4752751 IC50 = 126.0 nM 6.90
CHEMBL4786241 IC50 = 133.0 nM 6.88
CHEMBL4747960 IC50 = 134.0 nM 6.87
CHEMBL4754755 IC50 = 134.0 nM 6.87
CHEMBL4741188 IC50 = 141.0 nM 6.85
CHEMBL4744588 IC50 = 142.0 nM 6.85
CHEMBL4758227 IC50 = 150.0 nM 6.82
CHEMBL4749903 IC50 = 150.0 nM 6.82
CHEMBL4783252 IC50 = 150.0 nM 6.82
CHEMBL4758255 IC50 = 152.0 nM 6.82
CHEMBL4294999 IC50 = 158.0 nM 6.80
CHEMBL4758290 IC50 = 163.0 nM 6.79
CHEMBL4754861 IC50 = 168.0 nM 6.78
CHEMBL4763863 IC50 = 170.0 nM 6.77
CHEMBL4758312 IC50 = 175.0 nM 6.76
CHEMBL4792760 IC50 = 179.0 nM 6.75
CHEMBL4794789 IC50 = 178.0 nM 6.75