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HDM2004 | HDM2004 : Inhibitor of MAP4K1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
MAP4K1
  • IC50:1.89 nM
  • EC50:38.9 nM
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

Molecular Formula C28H35N7O
SMILEs CCN1CCC(n2cc(-c3c[nH]c4ncc(-c5ccc(N6C[C@@H](C)O[C@H](C)C6)cc5)nc34)cn2)CC1
InChI InChI=1S/C28H35N7O/c1-4-33-11-9-24(10-12-33)35-18-22(13-31-35)25-14-29-28-27(25)32-26(15-30-28)21-5-7-23(8-6-21)34-16-19(2)36-20(3)17-34/h5-8,13-15,18-20,24H,4,9-12,16-17H2,1-3H3,(H,29,30)/t19-,20-/m1/s1
Molecular weight 485.29 Da
AlogP 4.758800000000004
HBond acceptors 8
HBond donors 1
Atoms 71

References

Publications

Cross References

canSAR: 7719216 PubChem: 179077239

Expert Reviews

by SERP
(on 4 Apr 2026)
Cellular Use Rating
In Model Organisms
The primary concern with this molecule in cellular testing is kinome selectivity. It hits at least 10 of the 60 tested kinase targets at 90%+ at 1 µM. Researchers dosing this molecule in vivo should be...
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