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Assay Detail

CHEMBL4428282

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Binding
Inhibition of re-constituted HIV1 reverse transcriptase RNase H domain fragment
ChEMBL ↗
65
Total Activities
65
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 reverse transcriptase (CHEMBL247) ↗
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

3-Hydroxypyrimidine-2,4-diones as Selective Active Site Inhibitors of HIV Reverse Transcriptase-Associated RNase H: Design, Synthesis, and Biochemical Evaluations.
Tang J, Liu F, Nagy E, Miller L, Kirby KA, Wilson DJ, Wu B, Sarafianos SG, Parniak MA, Wang Z.
J Med Chem (2016) 59 : 2648 -2659
PubMed 26927866 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 5.82 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4451895 — — 1 7.00
CHEMBL4531566 — — 1 6.82
CHEMBL4281296 — — 1 6.82
CHEMBL4280869 — — 1 6.70
CHEMBL4549947 — — 1 6.40
CHEMBL4440667 — — 1 6.05
CHEMBL4445796 — — 1 6.05
CHEMBL4586421 — — 1 6.05
CHEMBL4563882 — — 1 6.05
CHEMBL4438951 — — 1 6.00
CHEMBL4438393 — — 1 6.00
CHEMBL4473298 — — 1 6.00
CHEMBL4463922 — — 1 6.00
CHEMBL4472917 — — 1 5.96
CHEMBL4514889 — — 1 5.96
CHEMBL4578639 — — 1 5.92
CHEMBL4530415 — — 1 5.85
CHEMBL4471489 — — 1 5.77
CHEMBL4437367 — — 1 5.77
CHEMBL4466948 — — 1 5.77
CHEMBL4529253 — — 1 5.75
CHEMBL4443953 — — 1 5.75
CHEMBL4445181 — — 1 5.72
CHEMBL4566144 — — 1 5.68
CHEMBL4450408 — — 1 5.66
CHEMBL4441277 — — 1 5.44
CHEMBL4440786 — — 1 5.41
CHEMBL4535894 — — 1 5.36
CHEMBL4531433 — — 1 5.33
CHEMBL4589112 — — 1 5.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4451895 — IC50 = 100.0 nM 7.00
CHEMBL4531566 — IC50 = 150.0 nM 6.82
CHEMBL4281296 — IC50 = 150.0 nM 6.82
CHEMBL4280869 — IC50 = 200.0 nM 6.70
CHEMBL4549947 — IC50 = 400.0 nM 6.40
CHEMBL4440667 — IC50 = 900.0 nM 6.05
CHEMBL4445796 — IC50 = 900.0 nM 6.05
CHEMBL4586421 — IC50 = 900.0 nM 6.05
CHEMBL4563882 — IC50 = 900.0 nM 6.05
CHEMBL4438951 — IC50 = 1000.0 nM 6.00
CHEMBL4438393 — IC50 = 1000.0 nM 6.00
CHEMBL4473298 — IC50 = 1000.0 nM 6.00
CHEMBL4463922 — IC50 = 1000.0 nM 6.00
CHEMBL4514889 — IC50 = 1100.0 nM 5.96
CHEMBL4472917 — IC50 = 1100.0 nM 5.96
CHEMBL4578639 — IC50 = 1200.0 nM 5.92
CHEMBL4530415 — IC50 = 1400.0 nM 5.85
CHEMBL4471489 — IC50 = 1700.0 nM 5.77
CHEMBL4437367 — IC50 = 1700.0 nM 5.77
CHEMBL4466948 — IC50 = 1700.0 nM 5.77
CHEMBL4529253 — IC50 = 1800.0 nM 5.75
CHEMBL4443953 — IC50 = 1800.0 nM 5.75
CHEMBL4445181 — IC50 = 1900.0 nM 5.72
CHEMBL4566144 — IC50 = 2100.0 nM 5.68
CHEMBL4450408 — IC50 = 2200.0 nM 5.66
CHEMBL4441277 — IC50 = 3600.0 nM 5.44
CHEMBL4440786 — IC50 = 3900.0 nM 5.41
CHEMBL4535894 — IC50 = 4400.0 nM 5.36
CHEMBL4531433 — IC50 = 4700.0 nM 5.33
CHEMBL4589112 — IC50 = 5100.0 nM 5.29
CHEMBL4584257 — IC50 = 5100.0 nM 5.29
CHEMBL4465689 — IC50 = 6200.0 nM 5.21
CHEMBL4545702 — IC50 = 6400.0 nM 5.19
CHEMBL4456393 — IC50 = 12000.0 nM 4.92
CHEMBL4450288 — IC50 = 13000.0 nM 4.89
CHEMBL4581611 — IC50 - — -
CHEMBL4553870 — IC50 - — -
CHEMBL4291913 — IC50 - — -
CHEMBL4455962 — IC50 - — -
CHEMBL4454510 — IC50 - — -
CHEMBL4475877 — IC50 - — -
CHEMBL4474029 — IC50 - — -
CHEMBL4466368 — IC50 - — -
CHEMBL4461191 — IC50 - — -
CHEMBL4550191 — IC50 - — -
CHEMBL4453169 — IC50 - — -
CHEMBL4534109 — IC50 - — -
CHEMBL4549918 — IC50 - — -
CHEMBL4532735 — IC50 - — -
CHEMBL4563474 — IC50 - — -