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Assay Detail

CHEMBL4428279

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Binding
Inhibition of RNase H activity of full length recombinant HIV1 reverse transcriptase assessed as reduction in nonspecific internal cleavage using HTS1 substrate
ChEMBL ↗
66
Total Activities
66
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 66 5.93 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4280869 — — 1 6.82
CHEMBL4550191 — — 1 6.75
CHEMBL4474029 — — 1 6.72
CHEMBL4531566 — — 1 6.70
CHEMBL4451895 — — 1 6.70
CHEMBL4291913 — — 1 6.66
CHEMBL4461191 — — 1 6.66
CHEMBL4466368 — — 1 6.62
CHEMBL4281296 — — 1 6.60
CHEMBL4475877 — — 1 6.51
CHEMBL4453169 — — 1 6.42
CHEMBL4549947 — — 1 6.40
CHEMBL4529253 — — 1 6.40
CHEMBL4455962 — — 1 6.33
CHEMBL4563882 — — 1 6.30
CHEMBL4472917 — — 1 6.30
CHEMBL4454510 — — 1 6.29
CHEMBL4471489 — — 1 6.22
CHEMBL4530415 — — 1 6.22
CHEMBL4438951 — — 1 6.16
CHEMBL4288759 — — 1 6.16
CHEMBL4471917 — — 1 6.12
CHEMBL4586421 — — 1 6.12
CHEMBL4466948 — — 1 6.10
CHEMBL4437367 — — 1 6.10
CHEMBL4581611 — — 1 6.07
CHEMBL4472002 — — 1 6.05
CHEMBL4553834 — — 1 6.05
CHEMBL4514889 — — 1 6.00
CHEMBL4441277 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4280869 — IC50 = 150.0 nM 6.82
CHEMBL4550191 — IC50 = 180.0 nM 6.75
CHEMBL4474029 — IC50 = 190.0 nM 6.72
CHEMBL4531566 — IC50 = 200.0 nM 6.70
CHEMBL4451895 — IC50 = 200.0 nM 6.70
CHEMBL4291913 — IC50 = 220.0 nM 6.66
CHEMBL4461191 — IC50 = 220.0 nM 6.66
CHEMBL4466368 — IC50 = 240.0 nM 6.62
CHEMBL4281296 — IC50 = 250.0 nM 6.60
CHEMBL4475877 — IC50 = 310.0 nM 6.51
CHEMBL4453169 — IC50 = 380.0 nM 6.42
CHEMBL4549947 — IC50 = 400.0 nM 6.40
CHEMBL4529253 — IC50 = 400.0 nM 6.40
CHEMBL4455962 — IC50 = 470.0 nM 6.33
CHEMBL4472917 — IC50 = 500.0 nM 6.30
CHEMBL4563882 — IC50 = 500.0 nM 6.30
CHEMBL4454510 — IC50 = 510.0 nM 6.29
CHEMBL4471489 — IC50 = 600.0 nM 6.22
CHEMBL4530415 — IC50 = 600.0 nM 6.22
CHEMBL4438951 — IC50 = 700.0 nM 6.16
CHEMBL4288759 — IC50 = 700.0 nM 6.16
CHEMBL4471917 — IC50 = 750.0 nM 6.12
CHEMBL4586421 — IC50 = 750.0 nM 6.12
CHEMBL4466948 — IC50 = 800.0 nM 6.10
CHEMBL4437367 — IC50 = 800.0 nM 6.10
CHEMBL4581611 — IC50 = 850.0 nM 6.07
CHEMBL4553834 — IC50 = 900.0 nM 6.05
CHEMBL4472002 — IC50 = 900.0 nM 6.05
CHEMBL4514889 — IC50 = 1000.0 nM 6.00
CHEMBL4441277 — IC50 = 1000.0 nM 6.00
CHEMBL4440786 — IC50 = 1000.0 nM 6.00
CHEMBL4438393 — IC50 = 1100.0 nM 5.96
CHEMBL4473298 — IC50 = 1100.0 nM 5.96
CHEMBL4476701 — IC50 = 1200.0 nM 5.92
CHEMBL4463922 — IC50 = 1200.0 nM 5.92
CHEMBL4440667 — IC50 = 1200.0 nM 5.92
CHEMBL4445796 — IC50 = 1400.0 nM 5.85
CHEMBL4540166 — IC50 = 1500.0 nM 5.82
CHEMBL4443953 — IC50 = 1600.0 nM 5.80
CHEMBL4437185 — IC50 = 1600.0 nM 5.80
CHEMBL4531433 — IC50 = 1600.0 nM 5.80
CHEMBL4581637 — IC50 = 1700.0 nM 5.77
CHEMBL4566144 — IC50 = 1900.0 nM 5.72
CHEMBL4449792 — IC50 = 1900.0 nM 5.72
CHEMBL4578639 — IC50 = 1900.0 nM 5.72
CHEMBL4589112 — IC50 = 2000.0 nM 5.70
CHEMBL4563474 — IC50 = 2200.0 nM 5.66
CHEMBL4545702 — IC50 = 2300.0 nM 5.64
CHEMBL4534109 — IC50 = 2400.0 nM 5.62
CHEMBL4454421 — IC50 = 2500.0 nM 5.60