Kinases

Our services lead to smarter selection of promising drugs through a detailed understanding of compound-target interactions. Maximize your research using our hit-to-lead and lead optimization tools to iterate medicinal chemistry, understand PK/PD disconnects and build better models to define therapeutic windows.

Maximize your kinase drug discovery efforts

Protein kinases constitute one of the largest protein families in the human genome consisting of more than 500 members. Alteration of kinase functions due to mutations or overexpression often leads to a diverse range of diseases. Thus, targeting protein kinases offers opportunities for the development of new medicines.

Technology

KINETICfinder®

KINETICfinder® is Enzymlogic’s patented kinetic screening platform that delivers rapid and accurate compound-target interaction data (Kd, kon, koff and residence time) with total confidence.

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COVALfinder®

COVALfinder® is a kinetic screening platform that provides in-depth understanding of the binding mechanism of reversible and irreversible drugs to iterate medicinal chemistry, understand PK/PD disconnects and build better models to define therapeutic windows.

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List of targets ready to use

Our expertise extends beyond kinases to GPCR and other target types.

Search our database to discover whether your target is:
  • May be possible: We have a strong track record of achievement where others fail! Contact us to find out more.
  • Clear line of sight: Establishment requires finalization / validation, which typically takes 2-4 weeks to complete.
  • Good to go: Data within 2 weeks of compound receipt.

* Full length and partial length forms are available.

Target name Alternative names KINETICfinder COVALfinder
AAK1 KIAA1048, DKFZp686K16132 Clear line of sight
ABL1 ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Good to go
ABL1 E255K ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL1 G250E ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL1 H396P ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL1 M351T ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL1 Q252H ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL1 Y253F ABL, c-ABL1, BCR-ABL, CHDSKM, JTK7, bcr/abl, c-ABL, p150, v-abl Clear line of sight
ABL2 (ARG) ARG, ABL isoform b, ABLL Good to go
ACK (TNK2) TNK2, ACK-1, ACK1, p21cdc42Hs Good to go
ACVR2A ACTRII, ACTR2, ACVR2 Clear line of sight
ACVR2B ACTRIIB, ActR-IIB, HTX4 Clear line of sight
AKT1 AKT1, PKB, PKB-ALPHA, PRKBA, RAC, RAC-ALPHA, Good to go
ALK ALK, CD246, NBLST3 Good to go May be possible
ALK C1156Y ALK, CD246, NBLST3 Clear line of sight
ALK F1174L ALK, CD246, NBLST3 Clear line of sight
ALK L1196M ALK, CD246, NBLST3 Clear line of sight
ALK R1275Q ALK, CD246, NBLST3 Clear line of sight
ALK T1151_L1152insT ALK, CD246, NBLST3 Clear line of sight
ALK1 (ACVRL1) ALK1, ALK-1, ACVRLK1, HHT, HHT2, ORW2, SKR3, TSR-I Good to go May be possible

Helpful resources

Enhancing Reversible Covalent Drug Design Case study
Affinity doesn’t tell the whole story of MET inhibitor Foretinib Case study
Selectivity profiling of irreversible EGFR inhibitors using COVALfinder® Case study
Approved FLT3 drugs are kinetic and conformation selective Case study
COVALfinder®, the ideal tool for irreversible drug discovery programs Case study
Approved KIT inhibitors show longer residence time Case study
FGFR1 inhibitors stabilize different binding modes Case study
Validation of a Novel Type II HER2 Inhibitor Through Preclinical Studies Across Various Cancer Models Poster
ELVN-002: a Potent, Selective, Irreversible and CNS Penetrant HER2 and pan-HER2 Mutant Small-Molecule Inhibitor Poster
Preclinical Characterization of CGT1786, a Novel EGFR Sparing ErbB2 Inhibitor with Activity Against Oncogenic ErbB2 Mutations Poster
KME-0584, a Highly Potent IRAK1/IRAK4/panFLT3 Inhibitor, Is a Promising Clinical Candidate for Hypomethylating Agent Plus Venetoclax Resistant AML/MDS Patients. Poster
Comparative Efficacy and Selectivity of Pharmacological Inhibitors of DYRK and CLK Protein Kinases Publication
A Selective and Orally Bioavailable Quinoline-6-Carbonitrile-Based Inhibitor of CDK8/19 Mediator Kinase with Tumor-Enriched Pharmacokinetics. Publication
Alkynyl nicotinamides show antileukemic activity in drug-resistant acute myeloid leukemia Publication
Chemical, Biochemical, Cellular, and Physiological Characterization of Leucettinib-21, a Down Syndrome and Alzheimer’s Disease Drug Candidate Publication
Protein Synthesis Rates and Target Vulnerability: Inhibitors and Degraders Poster
Evaluation of covalent BTK inhibitors using COVALfinder® Poster
Synthesis and Preclinical Evaluation of a Novel Fluorine-18-Labeled Tracer for Positron Emission Tomography Imaging of Bruton’s Tyrosine Kinase Publication
Benefits and Drawbacks of Binding Kinetic Methodologies Application note
KINETICfinder®: better by design Application note
View all resources

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