Setting the Standard in DEL Discovery for More Than 15 Years

We have delivered over 90 programs to our partners and clients, comprising over 1,000 novel, validated hit compounds across more than 30 different target classes. Most of these projects are actively progressed by our clients and remain confidential, but examples have been published in peer-reviewed journals. We have compiled these examples into the list below: They span a wide variety of therapy areas and target classes. Some represent our older and more peptidic libraries and others exemplify more contemporary and lead-like library designs. We continue to be at the forefront of DEL development technology, incorporating AI in drug discovery to explore greater chemical space.

Take a tour through X-Chem’s track record of success below.

Categories

ENZYMES

ENZYMES

TARGET:
SARS-CoV-2, Mpro IC50= 6 nM, antiviral EC50 33 nM

THERAPY AREA:
Antiviral

MOLECULAR WEIGHT:
612.6

CLOGP:
0.67

LE:
0.27

LLE:
6.34

CATEGORY OF COMPOUND:
Non-Covalent Lead Series Member

ENZYMES

TARGET:
Pks13, MIC = 250 nM

THERAPY AREA:
Infectious Disease

MOLECULAR WEIGHT:
457.5

CLOGP:
3.86

LE:
0.26

LLE:
2.74

CATEGORY OF COMPOUND:
Lead

ENZYMES

TARGET:
LpxA Inhibitor, IC50= 19 nM

THERAPY AREA:
Infectious Disease

MOLECULAR WEIGHT:
413.88

CLOGP:
1.80

LE:
0.39

LIPE:
5.9

CATEGORY OF COMPOUND:
Improved Hit

ENZYMES

TARGET:
HAO1 Inhibitor, IC50= 25 nM

THERAPY AREA:
Rare Disease: Primary Hyperoxaluria

MOLECULAR WEIGHT:
394.45

CLOGP:
3.84

LE:
0.37

LIPE:
3.8

CATEGORY OF COMPOUND:
Improved Hit

ENZYMES

TARGET:
ATX Inhibitor, IC50= 55 nM

THERAPY AREA:
Inflammation

MOLECULAR WEIGHT:
588.56

CLOGP:
2.68

LE:
0.24

LIPE:
4.6

CATEGORY OF COMPOUND:
Clinical Candidate

ENZYMES

TARGET:
sEH Inhibitor, IC50= 2 nM

THERAPY AREA:
Inflammation

MOLECULAR WEIGHT:
430.55

CLOGP:
4.36

LE:
0.38

LIPE:
4.33

CATEGORY OF COMPOUND:
Screening Hit

ENZYMES

TARGET:
KMO Inhibitor, IC50= 14 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
496.33

CLOGP:
5.41

LE:
0.34

LIPE:
2.44

CATEGORY OF COMPOUND:
Screening Hit

ENZYMES

TARGET:
InhA Inhibitor, IC50 = 26 nM

THERAPY AREA:
Tuberculosis

MOLECULAR WEIGHT:
487.68

CLOGP:
3.10

LE:
0.32

LIPE:
4.48

CATEGORY OF COMPOUND:
Screening Hit

KINASES

KINASES

TARGET:
cMet mutant, IC50 = 90 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
460.5

CLOGP:
5.0

LE:
0.29

LIPE:
2.0

CATEGORY OF COMPOUND:
Screening Hit

KINASES

TARGET:
TAK1 Inhibitor, IC50= 5 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
526.5

CLOGP:
0.10

LE:
0.31

LIPE:
8.2

CATEGORY OF COMPOUND:
Improved Hit

KINASES

TARGET:
MerTK Inhibitor, IC50= 5 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
415.88

CLOGP:
5.06

LE:
0.39

LIPE:
3.24

CATEGORY OF COMPOUND:
Screening Hit

KINASES

TARGET:
BTK Inhibitor, IC50= 2 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
480.53

CLOGP:
2.34

LE:
0.34

LIPE:
6.36

CATEGORY OF COMPOUND:
Screening Hit

KINASES

TARGET:
BTK Inhibitor, IC50= 60 nM (1h)

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
444.53

CLOGP:
1.95

LE:
–

LIPE:
–

CATEGORY OF COMPOUND:
Covalent Screening Hit

PROTEIN PROTEIN INTERACTION

PROTEIN PROTEIN INTERACTION

TARGET:
Bfl1, IC50 = 4.3μM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
446.4

CLOGP:
4.50

LE:
0.235

LLE:
0.86

CATEGORY OF COMPOUND:
Improved Reversible Covalent Hit

PROTEIN PROTEIN INTERACTION

TARGET:
IL-17A, HeLa IC50 = 5 nM

THERAPY AREA:
Inflammation

MOLECULAR WEIGHT:
612.6

CLOGP:
0.67

LE:
0.27

LLE:
6.34

CATEGORY OF COMPOUND:
Advanced Lead

PROTEIN PROTEIN INTERACTION

TARGET:
Mcl-1, IC50 = 31 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
925.4

CLOGP:
3.4

LE:
0.16

LLE:
2.0

CATEGORY OF COMPOUND:
Lead Candidate

PROTEIN PROTEIN INTERACTION

TARGET:
WDR91, Kd = 6µM

THERAPY AREA:
Virology

MOLECULAR WEIGHT:
372.9

CLOGP:
2.6

LE:
0.28

LIPE:
2.6

CATEGORY OF COMPOUND:
Tool Compound

PROTEIN PROTEIN INTERACTION

TARGET:
DCAF1, SPR KD = 38 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
439.24

CLOGP:
3.57

LE:
0.35

LLE:
3.39

CATEGORY OF COMPOUND:
Improved Hit

PROTEIN PROTEIN INTERACTION

TARGET:
ATAD2 Inhibitor, IC50= 25 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
640.23

CLOGP:
3.80

LE:
0.23

LIPE:
3.8

CATEGORY OF COMPOUND:
–

PROTEIN PROTEIN INTERACTION

TARGET:
Mcl-1 Inhibitor, IC50= <3 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
826.45

CLOGP:
6.56

LE:
0.21

LIPE:
1.96

CATEGORY OF COMPOUND:
Improved Hit

PROTEIN PROTEIN INTERACTION

TARGET:
STUB1, KD 9 uM

THERAPY AREA:
Neurodegeneration

MOLECULAR WEIGHT:
421.4

CLOGD_7.4:
1.3

LE:
0.25

LLE:
3.7

CATEGORY OF COMPOUND:
Lead

RECEPTORS

RECEPTORS

TARGET:
ERa Degrader, DC50= 37 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
–

CLOGP:
–

LE:
–

LIPE:
–

CATEGORY OF COMPOUND:
Lead Degrader

RECEPTORS

TARGET:
ERa Binder, IC50= 50 nM

THERAPY AREA:
Oncology

MOLECULAR WEIGHT:
321.77

CLOGP:
4.65

LE:
0.49

LIPE:
2.7

CATEGORY OF COMPOUND:
Screening Hit

RECEPTORS

TARGET:
PAR2 Antagonist, IC50= 23

THERAPY AREA:
Neurology

MOLECULAR WEIGHT:
571.48

CLOGP:
7.96

LE:
0.29

LIPE:
0.32

CATEGORY OF COMPOUND:
Improved Hit

RECEPTORS

TARGET:
PAR2 Agonist, EC50= 230 nM

THERAPY AREA:
Neurology

MOLECULAR WEIGHT:
542.68

CLOGP:
3.39

LE:
0.23

LIPE:
3.3

CATEGORY OF COMPOUND:
Screening Hit