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.

YTHDC1 m6A-RNA reader

Zalesak et al., compound 40

Reference Publication:
Structure-based design of a potent and selective YTHDC1 ligand

Relevant Data:
Kd of 49nM by ITC, low micromolecular GI50 values in cellular antiproliferation assay against different cell lines

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

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

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

YTHDC1 m6A-RNA reader

m6A-RNA writer METTL3/METTL14

Nudix hydrolase MTH1

Bromodomains

Tyrosine kinases

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