BDBM197160 GNE-140 (6)

SMILES c1ccc(c(c1)SC2=C(C[C@@](NC2=O)(c3ccc(cc3)N4CCOCC4)c5ccsc5)O)Cl

InChI Key InChIKey=SUFXXEIVBZJOAP-UHFFFAOYSA-N

Data  12 IC50  3 EC50

PDB links: 1 PDB ID matches this monomer.

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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 15 hits for monomerid = 197160   

TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 3nMAssay Description:LDHA, LDHB, LDHC, MDH1 and MDH2 enzymatic assays have been described in detail previously [Dragovich, P.S. et al, Bioorg. Med. Chem. Lett. 24:3764-37...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase B chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 5nMAssay Description:LDHA, LDHB, LDHC, MDH1 and MDH2 enzymatic assays have been described in detail previously [Dragovich, P.S. et al, Bioorg. Med. Chem. Lett. 24:3764-37...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/18/2016
Entry Details Article
PubMed
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataEC50:  7.20nMAssay Description:Inhibition of human LDH5 using pyruvate as substrate after 10 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetIsocitrate dehydrogenase [NADP] cytoplasmic(Human)
National Center For Advancing Translational Sciences

Curated by ChEMBL
LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 5.70E+4nMAssay Description:Inhibition of wild type IDH1 (unknown origin) using isocitrate as substrate preincubated for 30 mins followed by substrate addition in presence of NA...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMed
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 424nMAssay Description:Binding affinity to human His-tagged LDHA in presence of NADH by SPR assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase B chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 441nMAssay Description:Inhibition of human erythrocytes LDHB using sodium pyruvate as substrate after 5 mins in presence of NAPDH by diaphorase/resazurin based fluorescence...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMed
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 1.44E+3nMAssay Description:Inhibition of LDH in human A673 cells assessed as reduction in lactate production preincubated for 2 hrs measured after 30 mins by high throughput fl...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 10nMAssay Description:Inhibition of human LDHA using sodium pyruvate as substrate in presence of NAPDHMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 424nMAssay Description:Inhibition of human liver LDHA using sodium pyruvate as substrate after 5 mins in presence of NAPDH and in absence of EDTA by diaphorase/resazurin ba...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 877nMAssay Description:Inhibition of LDH in human MIAPaCa2 cells assessed as reduction in lactate production preincubated for 2 hrs measured after 30 mins by high throughpu...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataEC50:  1.26E+3nMAssay Description:Stabilization of LDHA in human A673 cell lysate preincubated for 20 mins followed by incubation at 70 degreeC for 10 mins by cellular thermal shift a...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/25/2019
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataEC50:  8.90nMAssay Description:Inhibition of recombinant human full-length N-terminal His-tagged LDHA (1 to 332 residues) expressed in Escherichia coli using sodium pyruvate as sub...More data for this Ligand-Target Pair
In Depth
Date in BDB:
2/24/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 670nMAssay Description:Inhibition of LDHA in human MiPaca2 cells assessed as inhibition of lactate productionMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetL-lactate dehydrogenase B chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 5nMAssay Description:Inhibition of human recombinant carboxy-terminal His-tagged LDHB by UV endpoint assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMed
TargetL-lactate dehydrogenase A chain(Human)
Genentech

LigandPNGBDBM197160(GNE-140 (6))
Affinity DataIC50: 3nMAssay Description:Inhibition of human recombinant carboxy-terminal His-tagged LDHA by UV endpoint assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/28/2021
Entry Details Article
PubMedPDB3D3D Structure (crystal)