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Compound Detail

CHEMBL2151322

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CC(C)Oc1cc(-n2cnc3ccc(N[C@@H](CO)c4ccc(F)cn4)nc32)n[nH]1

Basic Information

ChEMBL ID CHEMBL2151322
Phase Preclinical
Structure Type MOL
InChI Key CEDQYWYBSMPQAF-HNNXBMFYSA-N
2
Targets
2
Activities
1
Assay Types
7
PK Parameters
11
Publications
0
Known Names

Molecular Properties

397.4
MW (Da)
2.61
ALogP
8
HBA
3
HBD
113.8
PSA (Ų)
0.44
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20FN7O2
MW 397.41
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.17

Activity Summary

IC50 2 meas. best 8.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
High affinity nerve growth factor receptor
CHEMBL2815
IC50 8.52 8.52 3.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.28 4.28 52000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 46.0 mL.min-1.kg-1 Rattus norvegicus
CL 15.2 mL.min-1.kg-1 Canis lupus familiaris
F 29.0 % Rattus norvegicus
F 17.0 % Canis lupus familiaris
Fu 0.081 - Homo sapiens
T1/2 2.3 hr Rattus norvegicus
T1/2 1.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24900538 10.1021/ml300074j Rattus norvegicus 3
24900538 10.1021/ml300074j Canis familiaris 3
- 10.6019/CHEMBL3301361 ADMET 3
24900538 10.1021/ml300074j NIH3T3 2
24900538 10.1021/ml300074j Unchecked 1
24900538 10.1021/ml300074j Hepatocyte 1
24900538 10.1021/ml300074j No relevant target 1
24900538 10.1021/ml300074j Plasma 1
24900538 10.1021/ml300074j Voltage-gated inwardly rectifying potassium channel KCNH2 1
24900538 10.1021/ml300074j Mus musculus 1
- 10.6019/CHEMBL3301361 No relevant target 1

Data from ChEMBL 36 via Core Engine