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Compound Detail

CHEMBL5557372

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CC[C@H](C)[C@@H]1NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc(O)cc2)NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](C)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O

Basic Information

ChEMBL ID CHEMBL5557372
Phase Preclinical
Structure Type MOL
InChI Key JORFENHUBPMMNJ-ZLKHBANCSA-N
9
Targets
11
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

1937.2
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C96H117N19O23S
MW 1937.17

Activity Summary

IC50 11 meas. best 6.59

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Methylcytosine dioxygenase TET1
CHEMBL4523402
IC50 6.59 6.585 257.0 2
Methylcytosine dioxygenase TET2
CHEMBL4523344
IC50 5.27 4.945 5370.3 2
Methylcytosine dioxygenase TET3
CHEMBL4879414
IC50 5.23 5.23 5888.4 1
Methylcytosine dioxygenase TET1
CHEMBL5465312
IC50 5.22 5.22 6025.6 1
Aspartyl/asparaginyl beta-hydroxylase
CHEMBL4680030
IC50 4.97 4.97 10715.2 1
Hypoxia-inducible factor 1-alpha
CHEMBL4261
IC50 4.83 4.83 14791.1 1
Lysine-specific demethylase 5B
CHEMBL3774295
IC50 4.63 4.63 23442.3 1
Lysine-specific demethylase 6B
CHEMBL1938211
IC50 4.58 4.58 26302.7 1
Egl nine homolog 1
CHEMBL5697
IC50 4.51 4.51 30903.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Methylcytosine dioxygenase TET1 IC50 = 257.04 nM 6.59 Inhibition of N-terminal 3xFlag-tagged recombinant human TET1 catalytic domain (... 38262305
Methylcytosine dioxygenase TET1 IC50 = 260.0 nM 6.58 Inhibition of N-terminal 3xFlag-tagged recombinant human TET1 catalytic domain (... 38262305
Methylcytosine dioxygenase TET2 IC50 = 5370.32 nM 5.27 Inhibition of N-terminal His-tagged recombinant human TET2 catalytic domain LCId... 38262305
Methylcytosine dioxygenase TET3 IC50 = 5888.44 nM 5.23 Inhibition of recombinant human TET3 catalytic domain (E824 to I1795 residues) e... 38262305
Methylcytosine dioxygenase TET1 IC50 = 6025.6 nM 5.22 Inhibition of recombinant mouse TET1 catalytic domain (E1367 to V2039 residues) ... 38262305
Aspartyl/asparaginyl beta-hydroxylase IC50 = 10715.19 nM 4.97 Inhibition of recombinant human N-terminal His6-tagged ASPH (R315 to I758 residu... 38262305
Hypoxia-inducible factor 1-alpha IC50 = 14791.08 nM 4.83 Inhibition of recombinant human N-terminal His6-tagged FIH (M1 to N349 residues)... 38262305
Lysine-specific demethylase 5B IC50 = 23442.29 nM 4.63 Inhibition of recombinant human KDM5B (1 to 822 residues) expressed in baculovir... 38262305
Methylcytosine dioxygenase TET2 IC50 = 23988.33 nM 4.62 Inhibition of N-terminal His-tagged recombinant human TET2 catalytic domain LCId... 38262305
Lysine-specific demethylase 6B IC50 = 26302.68 nM 4.58 Inhibition of recombinant human KDM6B (D1141 to E1590 residues) expressed in Esc... 38262305
Egl nine homolog 1 IC50 = 30902.95 nM 4.51 Inhibition of recombinant human PHD2 (P181 to F426 residues) expressed in Escher... 38262305

Literature References

PubMed DOI Target Context # Activities
38262305 10.1016/j.bmc.2024.117597 Unchecked 7
38262305 10.1016/j.bmc.2024.117597 Methylcytosine dioxygenase TET1 5
38262305 10.1016/j.bmc.2024.117597 Methylcytosine dioxygenase TET2 3
38262305 10.1016/j.bmc.2024.117597 Methylcytosine dioxygenase TET3 2
38262305 10.1016/j.bmc.2024.117597 Lysine-specific demethylase 5B 1
38262305 10.1016/j.bmc.2024.117597 Lysine-specific demethylase 6B 1
38262305 10.1016/j.bmc.2024.117597 Egl nine homolog 1 1
38262305 10.1016/j.bmc.2024.117597 Hypoxia-inducible factor 1-alpha 1
38262305 10.1016/j.bmc.2024.117597 Aspartyl/asparaginyl beta-hydroxylase 1
38262305 10.1016/j.bmc.2024.117597 U2OS 1

Data from ChEMBL 36 via Core Engine