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Assay Detail

CHEMBL894220

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Binding
Inhibition of HIV integrase activity by HIV strand transfer assay
ChEMBL ↗
60
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Human immunodeficiency virus type 1 integrase (CHEMBL3471) ↗
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Discovery and synthesis of HIV integrase inhibitors: development of potent and orally bioavailable N-methyl pyrimidones.
Gardelli C, Nizi E, Muraglia E, Crescenzi B, Ferrara M, Orvieto F, Pace P, Pescatore G, Poma M, Ferreira Mdel R, Scarpelli R, Homnick CF, Ikemoto N, Alfieri A, Verdirame M, Bonelli F, Paz OG, Taliani M, Monteagudo E, Pesci S, Laufer R, Felock P, Stillmock KA, Hazuda D, Rowley M, Summa V.
J Med Chem (2007) 50 : 4953 -4975
PubMed 17824681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 7.25 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242926 — — 1 8.40
CHEMBL243151 — — 1 8.15
CHEMBL243365 — — 1 8.10
CHEMBL216874 — — 1 8.00
CHEMBL390027 — — 1 8.00
CHEMBL243150 — — 1 7.96
CHEMBL242924 — — 1 7.92
CHEMBL389829 — — 1 7.82
CHEMBL244863 — — 1 7.72
CHEMBL538587 — — 2 7.70
CHEMBL243377 — — 1 7.70
CHEMBL394847 — — 1 7.70
CHEMBL388908 — — 1 7.70
CHEMBL243265 — — 1 7.68
CHEMBL394353 — — 1 7.68
CHEMBL394610 — — 1 7.55
CHEMBL244520 — — 1 7.52
CHEMBL216683 — — 1 7.52
CHEMBL242561 — — 1 7.52
CHEMBL394786 — — 1 7.50
CHEMBL243366 — — 1 7.48
CHEMBL389566 — — 1 7.43
CHEMBL394537 — — 1 7.39
CHEMBL395819 — — 1 7.36
CHEMBL394782 — — 1 7.30
CHEMBL430194 — — 1 7.30
CHEMBL394781 — — 1 7.28
CHEMBL1161980 — — 1 7.22
CHEMBL386710 — — 1 7.22
CHEMBL244700 — — 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242926 — IC50 = 4.0 nM 8.40
CHEMBL243151 — IC50 = 7.0 nM 8.15
CHEMBL243365 — IC50 = 8.0 nM 8.10
CHEMBL216874 — IC50 = 10.0 nM 8.00
CHEMBL390027 — IC50 = 10.0 nM 8.00
CHEMBL243150 — IC50 = 11.0 nM 7.96
CHEMBL242924 — IC50 = 12.0 nM 7.92
CHEMBL389829 — IC50 = 15.0 nM 7.82
CHEMBL244863 — IC50 = 19.0 nM 7.72
CHEMBL538587 — IC50 = 20.0 nM 7.70
CHEMBL388908 — IC50 = 20.0 nM 7.70
CHEMBL394847 — IC50 = 20.0 nM 7.70
CHEMBL243377 — IC50 = 20.0 nM 7.70
CHEMBL394353 — IC50 = 21.0 nM 7.68
CHEMBL243265 — IC50 = 21.0 nM 7.68
CHEMBL538587 — IC50 = 25.0 nM 7.60
CHEMBL394610 — IC50 = 28.0 nM 7.55
CHEMBL216683 — IC50 = 30.0 nM 7.52
CHEMBL244520 — IC50 = 30.0 nM 7.52
CHEMBL242561 — IC50 = 30.0 nM 7.52
CHEMBL394786 — IC50 = 32.0 nM 7.50
CHEMBL243366 — IC50 = 33.0 nM 7.48
CHEMBL389566 — IC50 = 37.0 nM 7.43
CHEMBL394537 — IC50 = 41.0 nM 7.39
CHEMBL395819 — IC50 = 44.0 nM 7.36
CHEMBL430194 — IC50 = 50.0 nM 7.30
CHEMBL394782 — IC50 = 50.0 nM 7.30
CHEMBL394781 — IC50 = 52.0 nM 7.28
CHEMBL1161980 — IC50 = 60.0 nM 7.22
CHEMBL386710 — IC50 = 60.0 nM 7.22
CHEMBL244651 — IC50 = 62.0 nM 7.21
CHEMBL244964 — IC50 = 62.0 nM 7.21
CHEMBL389142 — IC50 = 62.0 nM 7.21
CHEMBL244700 — IC50 = 61.0 nM 7.21
CHEMBL243655 — IC50 = 62.0 nM 7.21
CHEMBL428570 — IC50 = 66.0 nM 7.18
CHEMBL244904 — IC50 = 70.0 nM 7.16
CHEMBL428215 — IC50 = 71.0 nM 7.15
CHEMBL244236 — IC50 = 86.0 nM 7.07
CHEMBL437708 — IC50 = 85.0 nM 7.07
CHEMBL244754 — IC50 = 100.0 nM 7.00
CHEMBL242137 — IC50 = 100.0 nM 7.00
CHEMBL244963 — IC50 = 100.0 nM 7.00
CHEMBL226764 — IC50 = 120.0 nM 6.92
CHEMBL242609 — IC50 = 130.0 nM 6.89
CHEMBL389332 — IC50 = 130.0 nM 6.89
CHEMBL397268 — IC50 = 140.0 nM 6.85
CHEMBL244235 — IC50 = 140.0 nM 6.85
CHEMBL389141 — IC50 = 175.0 nM 6.76
CHEMBL389331 — IC50 = 180.0 nM 6.75