Chemical Probes

This page has an incomplete list of chemical probes developed in the past and published in the scientific literature. Some activity information is provided.

Bromodomains

US13A (Compound 16)

Reference Publication:
Chemical space expansion of bromodomain ligands guided by in silico virtual couplings (AutoCouple)

Relevant Data:
35 nM activity against CREBBP (CREB-binding protein) bromodomain

m6A-RNA writer METTL3/METTL14

UZH1a

Reference Publication:
METTL3 inhibitors for epitranscriptomic modulation of cellular processes

Relevant Data:
IC50 of 280nM in biochemical assay, 4000nM in cellular (HEK293T) target engagement assay
UZH2

Reference Publication:
1,4,9-Triazaspiro[5.5]undecan-2-one derivatives as potent and selective METTL3 inhibitors

Relevant Data:
IC50 of 5nM in biochemical assay, 2000nM in cellular (HEK293T) target engagement assay

Nudix hydrolase MTH1

MTH1 fragment11

Reference Publication:
Ligand retargeting by binding site analogy

Relevant Data:
100 nM vs. MTH1

Tyrosine kinases

EphA3/EphB4_11d

Reference Publication:
Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: Structure-based design, synthesis, and in vivo validation

Relevant Data:
5 nM vs. EphA3/EphB4
EphA3/EphB4_7b

Reference Publication:
Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: Structure-based design, synthesis, and in vivo validation

Relevant Data:
20 nM vs. EphA3/EphB4
EphA3/EphB4_7g

Reference Publication:
Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: Structure-based design, synthesis, and in vivo validation

Relevant Data:
20 nM vs. EphA3/EphB4
EphA3/EphB4_7m

Reference Publication:
Pyrrolo[3,2-b]quinoxaline derivatives as types I1/2 and II Eph tyrosine kinase inhibitors: Structure-based design, synthesis, and in vivo validation

Relevant Data:
89 nM vs. EphA3/EphB4

Chemical Probes

Bromodomains

m6A-RNA writer METTL3/METTL14

Nudix hydrolase MTH1

Tyrosine kinases

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