PF-06835919

PF-06835919 : Inhibitor of KHK

Structure

SERP Rating

Probe PF-06835919 is in the process of SERP review.

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Information

Inhibitor

up to 1 uM

Probe Availability:

MolPort

In Vitro Validations

Uniprot ID: P50053

Target Class: Kinase

Target SubClass: Sugar Kinase

Potency: IC50

Potency Value: 28 nM

Potency Assay: Biochemical assay, measured at 2 mM ATP and 8 mM fructose for Isoform C (KHK-C)

PDB ID for probe-target interaction (3D structure): 6W0Z

Target aliases:

Ketohexokinase, KHK, KHK_HUMAN, Hepatic fructokina ...

DOI Reference: 10.1021/acs.jmedchem.0c00944

Uniprot ID: P50053

Target Class: Kinase

Target SubClass: Sugar Kinase

Potency: IC50

Potency Value: 170 nM

Potency Assay: Biochemical assay, measured at 2 mM ATP and 8 mM fructose for Isoform A (KHK-A)

PDB ID for probe-target interaction (3D structure): 6W0Z

Target aliases:

Ketohexokinase, KHK, KHK_HUMAN, Hepatic fructokina ...

DOI Reference: 10.1021/acs.jmedchem.0c00944

Uniprot ID: P50053

Target Class: Kinase

Target SubClass: Sugar Kinase

Potency: Ki

Potency Value: 4.53 nM

Potency Assay: Biochemical Assay

PDB ID for probe-target interaction (3D structure): 6W0Z

Target aliases:

Ketohexokinase, KHK, KHK_HUMAN, Hepatic fructokina ...

DOI Reference: 10.1021/acs.jmedchem.0c00944

Uniprot ID: P50053

Target Class: Kinase

Target SubClass: Sugar Kinase

Potency: IC50

Potency Value: 10 nM

Potency Assay: Biochemical assay, measured at [ATP], [fructose] at Km for Isoform C (KHK-C)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Ketohexokinase, KHK, KHK_HUMAN, Hepatic fructokina ...

DOI Reference: 10.1021/acs.jmedchem.0c00944

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Tested against other sugar kinases Human ribokinase 0.1 mM ATP >100 uM, Human glucokinase 0.8 mM ATP >100 uM, Human hexokinase-1 0.8 mM ATP >100 uM, Human hexokinase-2 0.8 mM ATP >100 uM, PF-06835919 exhibited a clean off-target selectivity profile as assessed by the CEREP panel (<53% at 30 μM). No significant inhibitions were observed on hERG (human ether-a-go-go-related gene, patch clamp IC50 > 100 μM), various kinases in the kinase selectivity panel, and PDE selectivity panel (the lowest IC50 = 11 μM against PDE10A).

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