HDM2004 |
HDM2004 : Inhibitor of MAP4K1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| MAP4K1 |
|
|
Inhibitor
up to 1 uM
Selectivity
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Kinase profiling screening against a panel of 60 wild-type kinases was conducted under a concentrati ...
Selectivity Assessment Description:
HDM2004 displayed moderate kinome selectivity. Potent “off target” kinase hits mainly include ROCK1, ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
Screening HDM2004 against a Safety Panel of 47 targets, including receptors, enzymes, kinases, and t ...
Selectivity Assessment Description:
At a screening concentration of 1 μM, HDM2004 inhibited ROCK1 (94.04% inhibition), VEGFR2 (91.39%), ...
Potency Cellular
In Vitro
MAP4K1
Mode of Action: Inhibitor
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1016/j.ejmech.2026.118708
In Vivo Validations
Mouse
Dose: 2 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
1.25 h
Systemic clearance:
42.9 mL/min/Kg
Area Under the Curve::
792 hr·ng/mL
Volume of Distribution at Steady-State:
4.63 L/Kg
DOI Reference: 10.1016/j.ejmech.2026.118708
Dose: 10 mg/Kg
Route of delivery:
Oral
Cmax:
486 ng/mL
Tmax:
2.00 h
Area Under the Curve::
1968 hr·ng/mL
Bioavailability:
52.0%
DOI Reference: 10.1016/j.ejmech.2026.118708
Rat
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
8.00 h
Systemic clearance:
25.8 mL/min/Kg
Area Under the Curve::
445 hr·ng/mL
Volume of Distribution at Steady-State:
14.2 L/Kg
DOI Reference: 10.1016/j.ejmech.2026.118708
Dose: 5 mg/Kg
Route of delivery:
Oral
Cmax:
83.5 ng/mL
Tmax:
7.33 h
Area Under the Curve::
1130 hr·ng/mL
Bioavailability:
55.4%
DOI Reference: 10.1016/j.ejmech.2026.118708
Monkey (Cynomolgus)
Dose: 1 mg/Kg
Route of delivery:
Intravenous
Plasma half life:
2.14 h
Systemic clearance:
41.5 mL/min/Kg
Area Under the Curve::
413 hr·ng/mL
Volume of Distribution at Steady-State:
7.48 L/Kg
DOI Reference: 10.1016/j.ejmech.2026.118708
Dose: 20 mg/Kg
Route of delivery:
Oral
Plasma half life:
11.02 h
Cmax:
306 ng/mL
Tmax:
11.02 h
Area Under the Curve::
8011 hr·ng/mL
Bioavailability:
101%
DOI Reference: 10.1016/j.ejmech.2026.118708
Dose: 60 mg/Kg
Route of delivery:
Oral
Plasma half life:
15.32 h
Cmax:
537 ng/mL
Tmax:
15.32 h
Area Under the Curve::
29254 hr·ng/mL
Bioavailability:
78.7%
DOI Reference: 10.1016/j.ejmech.2026.118708
Chemical Information
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