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Compound Detail

CHEMBL3644587

2X-121
🧪 Phase II
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🧪 Phase II
O=c1[nH]nc2c3c(cccc13)N=C(CN1Cc3ccccc3C1)N2

Basic Information

ChEMBL ID CHEMBL3644587
Name 2X-121
Phase Phase II
Structure Type MOL
InChI Key JLFSBHQQXIAQEC-UHFFFAOYSA-N

Known Names

2x-121 E-7449 E7449 Parp inhibitor 2x-121 Stenoparib
9
Targets
20
Activities
1
Assay Types
0
PK Parameters
20
Publications
5
Known Names
3
Indications
3
Mechanisms

Molecular Properties

317.4
MW (Da)
2.39
ALogP
5
HBA
2
HBD
73.4
PSA (Ų)
0.76
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Flags

Chemical Probe

Extended Properties

Molecular Formula C18H15N5O
MW 317.35
Aromatic Rings 3
Heavy Atoms 24
NP-Likeness -0.95

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Poly [ADP-ribose] polymerase-1 inhibitor INHIBITOR Poly [ADP-ribose] polymerase 1
Poly [ADP-ribose] polymerase 2 inhibitor INHIBITOR Poly [ADP-ribose] polymerase 2
Tankyrase 1/2 inhibitor INHIBITOR Tankyrase 1/2

Indications

Ovarian Neoplasms Breast Neoplasms Neoplasms

Activity Summary

IC50 20 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Poly [ADP-ribose] polymerase 2
CHEMBL2794
IC50 9.0 8.96 1.0 2
Poly [ADP-ribose] polymerase 1
CHEMBL3105
IC50 9.0 8.72 1.0 6
Poly [ADP-ribose] polymerase 2
CHEMBL5366
IC50 9.0 8.85 1.0 2
Tankyrase 1/2
CHEMBL3038515
IC50 7.3 7.3 50.0 1
Poly [ADP-ribose] polymerase tankyrase-2
CHEMBL6154
IC50 7.3 7.1733 50.0 3
Poly [ADP-ribose] polymerase tankyrase-1
CHEMBL6164
IC50 7.3 7.3 50.0 3
MDA-MB-231
CHEMBL400
IC50 5.54 5.54 2890.0 1
MDA-MB-468
CHEMBL614335
IC50 5.38 5.38 4170.0 1
HCT-116
CHEMBL394
IC50 5.17 5.17 6710.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Poly [ADP-ribose] polymerase 2 IC50 = 1.0 nM 9.0 Inhibition of mouse recombinant PARP2 35306814
Poly [ADP-ribose] polymerase 1 IC50 = 1.0 nM 9.0 Inhibition of human recombinant PARP1 by chemiluminescent assay 34998039
Poly [ADP-ribose] polymerase 1 IC50 = 1.0 nM 9.0 Inhibition of human recombinant PARP-1 27416328
Poly [ADP-ribose] polymerase 1 IC50 = 1.0 nM 9.0 Inhibition of PARP1 (unknown origin) 36598465
Poly [ADP-ribose] polymerase 2 IC50 = 1.0 nM 9.0 Inhibition of recombinant human PARP2 using DNase I-activated herring sperm DNA ... 29107427
Poly [ADP-ribose] polymerase 2 IC50 = 1.2 nM 8.92 Inhibition of mouse recombinant PARP-2 27416328
Poly [ADP-ribose] polymerase 1 IC50 = 2.0 nM 8.7 Inhibition of recombinant human PARP1 using DNase I-activated herring sperm DNA ... 29107427
Poly [ADP-ribose] polymerase 1 IC50 = 2.0 nM 8.7 Inhibition of human recombinant PARP1 35306814
Poly [ADP-ribose] polymerase 2 IC50 = 2.0 nM 8.7 Inhibition of PARP2 (unknown origin) 36598465
Poly [ADP-ribose] polymerase 1 IC50 = 12.0 nM 7.92 Enzyme Assay: A convenient method to determine IC50 of a PARP inhibitor compound... -
Poly [ADP-ribose] polymerase tankyrase-1 IC50 = 50.0 nM 7.3 Inhibition of human recombinant TNKS1 by chemiluminescent assay 29107427
Poly [ADP-ribose] polymerase tankyrase-2 IC50 = 50.0 nM 7.3 Inhibition of TNKS2 (unknown origin) 36598465
Poly [ADP-ribose] polymerase tankyrase-1 IC50 = 50.0 nM 7.3 Inhibition of TNKS1 (unknown origin) 36598465
Tankyrase 1/2 IC50 = 50.0 nM 7.3 Inhibition of human recombinant TNKS1/TNKS2 (unknown origin) by chemiluminescent... 34998039
Poly [ADP-ribose] polymerase tankyrase-2 IC50 = 50.0 nM 7.3 Inhibition of human recombinant TNKS2 35306814
Poly [ADP-ribose] polymerase tankyrase-1 IC50 = 50.0 nM 7.3 Inhibition of human recombinant TNKS1 35306814
Poly [ADP-ribose] polymerase tankyrase-2 IC50 = 120.0 nM 6.92 Inhibition of human recombinant TNKS2 by chemiluminescent assay 29107427
MDA-MB-231 IC50 = 2890.0 nM 5.54 Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition... 35504210
MDA-MB-468 IC50 = 4170.0 nM 5.38 Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition... 35504210
HCT-116 IC50 = 6710.0 nM 5.17 Antiproliferative activity against human HCT-116 cells assessed as inhibition of... 35504210

Literature References

PubMed DOI Target Context # Activities
35504210 10.1016/j.ejmech.2022.114417 HCT-116 9
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
35504210 10.1016/j.ejmech.2022.114417 Unchecked 3
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 2
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
35306814 10.1021/acs.jmedchem.1c02139 Poly [ADP-ribose] polymerase tankyrase-1 1
36598465 10.1021/acs.jmedchem.2c01460 Poly [ADP-ribose] polymerase tankyrase-2 1
27416328 10.1021/acs.jmedchem.6b00055 Poly [ADP-ribose] polymerase 1 1
34998039 10.1016/j.ejmech.2021.114094 Tankyrase 1/2 1
34998039 10.1016/j.ejmech.2021.114094 Poly [ADP-ribose] polymerase 1 1
35504210 10.1016/j.ejmech.2022.114417 AML12 1
35504210 10.1016/j.ejmech.2022.114417 MDA-MB-468 1
35504210 10.1016/j.ejmech.2022.114417 MDA-MB-231 1
35306814 10.1021/acs.jmedchem.1c02139 Poly [ADP-ribose] polymerase tankyrase-2 1
29107427 10.1016/j.ejmech.2017.09.030 Poly [ADP-ribose] polymerase 1 1
35306814 10.1021/acs.jmedchem.1c02139 Poly [ADP-ribose] polymerase 2 1
35306814 10.1021/acs.jmedchem.1c02139 Poly [ADP-ribose] polymerase 1 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
29107427 10.1016/j.ejmech.2017.09.030 Poly [ADP-ribose] polymerase tankyrase-2 1
29107427 10.1016/j.ejmech.2017.09.030 Poly [ADP-ribose] polymerase tankyrase-1 1

Data from ChEMBL 36 via Core Engine