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Compound Detail

CHEMBL550202

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Cc1nc(C)c(C(=O)N2CCCCC2(C)c2nc(C(=O)NCc3ccc(F)cc3)c(O)c(=O)[nH]2)s1

Basic Information

ChEMBL ID CHEMBL550202
Phase Preclinical
Structure Type MOL
InChI Key ICPPCODEZYGZTO-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

499.6
MW (Da)
3.16
ALogP
7
HBA
3
HBD
128.3
PSA (Ų)
0.49
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H26FN5O4S
MW 499.57
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 7.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus type 1 integrase
CHEMBL3471
IC50 7.7 7.7 20.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.13 - Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19616948 10.1016/j.bmcl.2009.06.091 No relevant target 3
19616948 10.1016/j.bmcl.2009.06.091 Human immunodeficiency virus type 1 integrase 1
19616948 10.1016/j.bmcl.2009.06.091 Human immunodeficiency virus 1 1
19616948 10.1016/j.bmcl.2009.06.091 Plasma 1
19616948 10.1016/j.bmcl.2009.06.091 ADMET 1

Data from ChEMBL 36 via Core Engine