Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | 4.5 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Mixed noncompetitive inhibition of recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate ... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00944 BindingDB Entry DOI: 10.7270/Q2QC074M | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 8.40 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay B, using 10-fold less enzyme and measuring absorbance for 3 hours to obtain IC50 values below the 10 nM lower limit of Assay A. Compounds were ... | US Patent US10787438 (2020) BindingDB Entry DOI: 10.7270/Q2VQ35RP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 8.40 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay B, using 10-fold less enzyme and measuring absorbance for 3 hours to obtain IC50 values below the 10 nM lower limit of Assay A. Compounds were ... | US Patent US10988463 (2021) BindingDB Entry DOI: 10.7270/Q2SJ1PRS | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 8.40 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Compounds having an IC50 value less than 20 nM were examined in a second KHK assay, referred to as Assay B, using 10-fold less enzyme and measuring a... | US Patent US10174007 (2019) BindingDB Entry DOI: 10.7270/Q20867DX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | n/a | n/a | 8.40 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details BindingDB Entry DOI: 10.7270/Q2B2807K | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c01511 BindingDB Entry DOI: 10.7270/Q22Z19M2 | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 10 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of 1 nM recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using fructose as substrate preincubated for... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00944 BindingDB Entry DOI: 10.7270/Q2QC074M | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
Terns Pharmaceuticals Curated by ChEMBL | Assay Description Inhibition of recombinant His-tagged human KHK expressed in Escherichia coli in presence of NADPH | J Med Chem 63: 5031-5073 (2020) Article DOI: 10.1021/acs.jmedchem.9b01701 BindingDB Entry DOI: 10.7270/Q2DJ5JXG | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 14.2 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay A, a 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepa... | US Patent US10787438 (2020) BindingDB Entry DOI: 10.7270/Q2VQ35RP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 14.2 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay A, a 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepa... | US Patent US10988463 (2021) BindingDB Entry DOI: 10.7270/Q2SJ1PRS | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 14.2 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description A 384-well format on a Corning 3653 assay plate is used, and monitored by UV-vis spectroscopy in continuous mode at rt. Compounds were prepared in DM... | US Patent US10174007 (2019) BindingDB Entry DOI: 10.7270/Q20867DX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | n/a | n/a | 14.2 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details BindingDB Entry DOI: 10.7270/Q2B2807K | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 28 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of recombinant human N-terminal His-tagged KHKC expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00944 BindingDB Entry DOI: 10.7270/Q2QC074M | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 37.3 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physiological concentrations of the nat... | US Patent US10787438 (2020) BindingDB Entry DOI: 10.7270/Q2VQ35RP | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 37.3 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description A third KHK assay, referred to as Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physi... | US Patent US10174007 (2019) BindingDB Entry DOI: 10.7270/Q20867DX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 37.3 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description Assay C, was performed at high fructose and ATP concentrations, conditions that would be more consistent with physiological concentrations of the nat... | US Patent US10988463 (2021) BindingDB Entry DOI: 10.7270/Q2SJ1PRS | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | n/a | n/a | 37.3 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details BindingDB Entry DOI: 10.7270/Q2B2807K | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | US Patent | n/a | n/a | 66 | n/a | n/a | n/a | n/a | n/a | n/a |
Pfizer Inc. US Patent | Assay Description A fourth assay, referred to as Assay D, was performed using human KHK-A to assess the potency of compounds in inhibiting activity of this enzyme. Com... | US Patent US10174007 (2019) BindingDB Entry DOI: 10.7270/Q20867DX | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | n/a | n/a | 66 | n/a | n/a | n/a | n/a | n/a | n/a | |
TBA | Citation and Details BindingDB Entry DOI: 10.7270/Q2B2807K | ||||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Homo sapiens (Human)) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 170 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of recombinant human N-terminal His-tagged KHKA expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00944 BindingDB Entry DOI: 10.7270/Q2QC074M | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Ketohexokinase (Rattus norvegicus) | BDBM319585 (US10174007, Example 4 | US10787438, Example 4 | US...) | PDB UniProtKB/SwissProt GoogleScholar AffyNet | Purchase PC cid PC sid UniChem | Article PubMed | n/a | n/a | 210 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA | Assay Description Inhibition of recombinant rat N-terminal His-tagged KHK expressed in Escherichia coli BL21 (DE3) using 8 mM fructose as substrate preincubated for 30... | Citation and Details Article DOI: 10.1021/acs.jmedchem.0c00944 BindingDB Entry DOI: 10.7270/Q2QC074M | |||||||||||
More data for this Ligand-Target Pair |