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Assay Detail

CHEMBL4428280

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Binding
Inhibition of RNase H activity of full length recombinant HIV1 reverse transcriptase assessed as reduction in DNA 3'-end cleavage using HTS2 substrate
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 5.59 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4280869 — — 1 6.60
CHEMBL4281296 — — 1 6.52
CHEMBL4531566 — — 1 6.52
CHEMBL4451895 — — 1 6.52
CHEMBL4474029 — — 1 6.50
CHEMBL4461191 — — 1 6.37
CHEMBL4291913 — — 1 6.35
CHEMBL4453169 — — 1 6.35
CHEMBL4550191 — — 1 6.35
CHEMBL4466368 — — 1 6.31
CHEMBL4475877 — — 1 6.27
CHEMBL4455962 — — 1 6.18
CHEMBL4454510 — — 1 6.16
CHEMBL4549947 — — 1 6.16
CHEMBL4514889 — — 1 5.68
CHEMBL4463922 — — 1 5.68
CHEMBL4563882 — — 1 5.66
CHEMBL4438951 — — 1 5.64
CHEMBL4472917 — — 1 5.58
CHEMBL4438393 — — 1 5.58
CHEMBL4530415 — — 1 5.55
CHEMBL4473298 — — 1 5.50
CHEMBL4471489 — — 1 5.46
CHEMBL4437367 — — 1 5.46
CHEMBL4581611 — — 1 5.46
CHEMBL4466948 — — 1 5.46
CHEMBL4440667 — — 1 5.43
CHEMBL4471917 — — 1 5.42
CHEMBL4529253 — — 1 5.40
CHEMBL4445796 — — 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4280869 — IC50 = 250.0 nM 6.60
CHEMBL4281296 — IC50 = 300.0 nM 6.52
CHEMBL4531566 — IC50 = 300.0 nM 6.52
CHEMBL4451895 — IC50 = 300.0 nM 6.52
CHEMBL4474029 — IC50 = 320.0 nM 6.50
CHEMBL4461191 — IC50 = 430.0 nM 6.37
CHEMBL4291913 — IC50 = 450.0 nM 6.35
CHEMBL4453169 — IC50 = 450.0 nM 6.35
CHEMBL4550191 — IC50 = 450.0 nM 6.35
CHEMBL4466368 — IC50 = 490.0 nM 6.31
CHEMBL4475877 — IC50 = 540.0 nM 6.27
CHEMBL4455962 — IC50 = 660.0 nM 6.18
CHEMBL4454510 — IC50 = 700.0 nM 6.16
CHEMBL4549947 — IC50 = 700.0 nM 6.16
CHEMBL4463922 — IC50 = 2100.0 nM 5.68
CHEMBL4514889 — IC50 = 2100.0 nM 5.68
CHEMBL4563882 — IC50 = 2200.0 nM 5.66
CHEMBL4438951 — IC50 = 2300.0 nM 5.64
CHEMBL4472917 — IC50 = 2600.0 nM 5.58
CHEMBL4438393 — IC50 = 2600.0 nM 5.58
CHEMBL4530415 — IC50 = 2800.0 nM 5.55
CHEMBL4473298 — IC50 = 3200.0 nM 5.50
CHEMBL4466948 — IC50 = 3500.0 nM 5.46
CHEMBL4581611 — IC50 = 3500.0 nM 5.46
CHEMBL4471489 — IC50 = 3500.0 nM 5.46
CHEMBL4437367 — IC50 = 3500.0 nM 5.46
CHEMBL4440667 — IC50 = 3700.0 nM 5.43
CHEMBL4471917 — IC50 = 3800.0 nM 5.42
CHEMBL4529253 — IC50 = 4000.0 nM 5.40
CHEMBL4445796 — IC50 = 4100.0 nM 5.39
CHEMBL4540166 — IC50 = 4300.0 nM 5.37
CHEMBL4437185 — IC50 = 4400.0 nM 5.36
CHEMBL4566144 — IC50 = 5300.0 nM 5.28
CHEMBL4445181 — IC50 = 6500.0 nM 5.19
CHEMBL4586421 — IC50 = 6600.0 nM 5.18
CHEMBL4553834 — IC50 = 6700.0 nM 5.17
CHEMBL4476701 — IC50 = 6900.0 nM 5.16
CHEMBL4578639 — IC50 = 6900.0 nM 5.16
CHEMBL4581637 — IC50 = 7200.0 nM 5.14
CHEMBL4443953 — IC50 = 7200.0 nM 5.14
CHEMBL4450408 — IC50 = 8900.0 nM 5.05
CHEMBL4443222 — IC50 = 9300.0 nM 5.03
CHEMBL4531433 — IC50 = 11000.0 nM 4.96
CHEMBL4454421 — IC50 = 11000.0 nM 4.96
CHEMBL4472002 — IC50 = 12000.0 nM 4.92
CHEMBL4449792 — IC50 = 13000.0 nM 4.89
CHEMBL4563474 — IC50 = 15000.0 nM 4.82
CHEMBL4589112 — IC50 = 16000.0 nM 4.80
CHEMBL4441277 — IC50 = 17000.0 nM 4.77
CHEMBL4465689 — IC50 - — -