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Compound Detail

CHEMBL3673452

GZ-389988
🧪 Phase II
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🧪 Phase II
COc1ccc(COc2ccc(Cn3c(N)nc4cc(-c5cnn(C)c5)cnc43)cc2OC)cc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL3673452
Name GZ-389988
Phase Phase II
Structure Type MOL
InChI Key HVRWZFQFSQUILC-UHFFFAOYSA-N

Known Names

Gz-389988 Gz389988
4
Targets
17
Activities
1
Assay Types
0
PK Parameters
0
Publications
2
Known Names
1
Indications
1
Mechanisms

Molecular Properties

470.5
MW (Da)
4.06
ALogP
9
HBA
1
HBD
102.2
PSA (Ų)
0.36
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral

Extended Properties

Molecular Formula C26H26N6O3
MW 470.53
Aromatic Rings 5
Heavy Atoms 35
NP-Likeness -1.32

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Nerve growth factor receptor Trk-A inhibitor INHIBITOR High affinity nerve growth factor receptor ✓ ✓

Indications

Osteoarthritis

Activity Summary

IC50 17 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BDNF/NT-3 growth factors receptor
CHEMBL4898
 IC50 10.0 10.0 0.1 4
High affinity nerve growth factor receptor
CHEMBL2815
 IC50 9.52 9.52 0.3 4
NT-3 growth factor receptor
CHEMBL5608
 IC50 9.3 9.3 0.5 4
Macrophage colony-stimulating factor 1 receptor
CHEMBL1844
 IC50 8.7 8.7 2.0 5

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
BDNF/NT-3 growth factors receptor IC50 = 0.1 nM 10.0 In Vitro TrkB Activity: In a 384 well polypropylene plate, TrkB (0.6 nM, Carna 0... -
BDNF/NT-3 growth factors receptor IC50 = 0.1 nM 10.0 TrkB Activity: Reagents and consumables were purchased from Sigma Aldrich, Carna... -
BDNF/NT-3 growth factors receptor IC50 = 0.1 nM 10.0 TrkB Activity: Reagents and consumables were purchased from Sigma Aldrich, Carna... -
BDNF/NT-3 growth factors receptor IC50 = 0.1 nM 10.0 Inhibition Assay: Reagents and consumables were purchased from Sigma Aldrich, Ca... -
High affinity nerve growth factor receptor IC50 = 0.3 nM 9.52 Inhibition Assay: Reagents and consumables were purchased from Sigma Aldrich, Ca... -
High affinity nerve growth factor receptor IC50 = 0.3 nM 9.52 In Vitro TrkA Activity: In a 384 well polypropylene plate, TrkA (0.4 nM, Carna 0... -
High affinity nerve growth factor receptor IC50 = 0.3 nM 9.52 TrkA Activity: Reagents and consumables were purchased from Sigma Aldrich, Carna... -
High affinity nerve growth factor receptor IC50 = 0.3 nM 9.52 TrkA Activity: Reagents and consumables were purchased from Sigma Aldrich, Carna... -
NT-3 growth factor receptor IC50 = 0.503 nM 9.3 Inhibition Assay: Human TrkC, catalytic domain [456-825(end) amino acids of acce... -
NT-3 growth factor receptor IC50 = 0.503 nM 9.3 TrkC Activity: Human TrkC, catalytic domain [456-825 (end) amino acids of access... -
NT-3 growth factor receptor IC50 = 0.503 nM 9.3 TrkC Activity: Human TrkC, catalytic domain [456-825(end) amino acids of accessi... -
NT-3 growth factor receptor IC50 = 0.503 nM 9.3 In Vitro TrkC Activity: Human TrkC, catalytic domain [456-825(end) amino acids o... -
Macrophage colony-stimulating factor 1 receptor IC50 = 2.0 nM 8.7 Inhibition Assay: Reagents and consumables were purchased from Sigma Aldrich, Ca... -
Macrophage colony-stimulating factor 1 receptor IC50 = 2.0 nM 8.7 Inhibition Assay: Reagents and consumables were purchased from Sigma Aldrich, Ca... -
Macrophage colony-stimulating factor 1 receptor IC50 = 2.0 nM 8.7 In Vitro c-FMS Activity: In a 384 well polypropylene plate, c-FMS (0.14 nM, Carn... -
Macrophage colony-stimulating factor 1 receptor IC50 = 2.0 nM 8.7 c-FMS Activity: Reagents and consumables were purchased from Sigma Aldrich, Carn... -
Macrophage colony-stimulating factor 1 receptor IC50 = 2.0 nM 8.7 c-FMS Activity: Reagents and consumables were purchased from Sigma Aldrich, Carn... -

Data from ChEMBL 36 via Core Engine