Selecting drug candidates with suitable safety profiles

Selectivity is highly dynamic in the human body and evolves over the course of treatment as a function of the temporal binding between the drug and the main and secondary targets. Consequently, the therapeutic window is maximized when a drug shows long residence time when bound to its main target and short residence times for collateral targets.

Applications

  • Maximize therapeutic windows: Modify on- and off-target kinetics earlier and with confidence to build greater safety margins and reduce adverse events.
  • Easier decision-making: Gain a greater understanding of compound safety and tolerability profiles earlier in the discovery process.
  • Build better models: PK/PD models that integrate kinetics better predict target engagement and consequently real selectivity and potential adverse events.
  • Drug repositioning: Understanding the time that a drug engages with a panel of promising targets can identify new therapeutic indications.

Technology

KINETICfinder®

KINETICfinder® is Enzymlogic’s patented high-throughput screening platform that delivers all key binding kinetic (kon / koff / residence time) and affinity (kd) parameters for reversible binders quickly and at scale.

Our highly robust platform provides accurate and reproducible compound – target interaction data that enables improved screening of compounds in early discovery: to iterate medicinal chemistry, understand PK/PD disconnects and build better models to define therapeutic windows.

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) ACK, ACK-1, ACK1, p21cdc42Hs Clear line of sight
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

How can we help?

Our experienced project manager will work with you to identify the best way forward for your project.