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Assay Detail

CHEMBL4428281

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Binding
Inhibition of RNase H activity of full length recombinant HIV1 reverse transcriptase assessed as reduction in RNA 5'-end directed cleavage using HTS3 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 5.49 6.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4474029 — — 1 6.60
CHEMBL4280869 — — 1 6.60
CHEMBL4281296 — — 1 6.52
CHEMBL4531566 — — 1 6.52
CHEMBL4291913 — — 1 6.43
CHEMBL4550191 — — 1 6.43
CHEMBL4451895 — — 1 6.40
CHEMBL4461191 — — 1 6.40
CHEMBL4453169 — — 1 6.36
CHEMBL4466368 — — 1 6.34
CHEMBL4454510 — — 1 6.33
CHEMBL4549947 — — 1 6.30
CHEMBL4455962 — — 1 6.22
CHEMBL4475877 — — 1 5.62
CHEMBL4471917 — — 1 5.57
CHEMBL4563882 — — 1 5.52
CHEMBL4472917 — — 1 5.51
CHEMBL4440667 — — 1 5.48
CHEMBL4581611 — — 1 5.47
CHEMBL4438951 — — 1 5.47
CHEMBL4438393 — — 1 5.43
CHEMBL4437185 — — 1 5.42
CHEMBL4463922 — — 1 5.42
CHEMBL4476701 — — 1 5.41
CHEMBL4445796 — — 1 5.41
CHEMBL4530415 — — 1 5.40
CHEMBL4473298 — — 1 5.39
CHEMBL4514889 — — 1 5.38
CHEMBL4471489 — — 1 5.37
CHEMBL4472002 — — 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4474029 — IC50 = 250.0 nM 6.60
CHEMBL4280869 — IC50 = 250.0 nM 6.60
CHEMBL4531566 — IC50 = 300.0 nM 6.52
CHEMBL4281296 — IC50 = 300.0 nM 6.52
CHEMBL4291913 — IC50 = 370.0 nM 6.43
CHEMBL4550191 — IC50 = 370.0 nM 6.43
CHEMBL4451895 — IC50 = 400.0 nM 6.40
CHEMBL4461191 — IC50 = 400.0 nM 6.40
CHEMBL4453169 — IC50 = 440.0 nM 6.36
CHEMBL4466368 — IC50 = 460.0 nM 6.34
CHEMBL4454510 — IC50 = 470.0 nM 6.33
CHEMBL4549947 — IC50 = 500.0 nM 6.30
CHEMBL4455962 — IC50 = 600.0 nM 6.22
CHEMBL4475877 — IC50 = 2400.0 nM 5.62
CHEMBL4471917 — IC50 = 2700.0 nM 5.57
CHEMBL4563882 — IC50 = 3000.0 nM 5.52
CHEMBL4472917 — IC50 = 3100.0 nM 5.51
CHEMBL4440667 — IC50 = 3300.0 nM 5.48
CHEMBL4581611 — IC50 = 3400.0 nM 5.47
CHEMBL4438951 — IC50 = 3400.0 nM 5.47
CHEMBL4438393 — IC50 = 3700.0 nM 5.43
CHEMBL4437185 — IC50 = 3800.0 nM 5.42
CHEMBL4463922 — IC50 = 3800.0 nM 5.42
CHEMBL4476701 — IC50 = 3900.0 nM 5.41
CHEMBL4445796 — IC50 = 3900.0 nM 5.41
CHEMBL4530415 — IC50 = 4000.0 nM 5.40
CHEMBL4473298 — IC50 = 4100.0 nM 5.39
CHEMBL4514889 — IC50 = 4200.0 nM 5.38
CHEMBL4471489 — IC50 = 4300.0 nM 5.37
CHEMBL4472002 — IC50 = 4300.0 nM 5.37
CHEMBL4578639 — IC50 = 4500.0 nM 5.35
CHEMBL4553834 — IC50 = 4600.0 nM 5.34
CHEMBL4454421 — IC50 = 4700.0 nM 5.33
CHEMBL4529253 — IC50 = 4700.0 nM 5.33
CHEMBL4586421 — IC50 = 5000.0 nM 5.30
CHEMBL4437367 — IC50 = 5100.0 nM 5.29
CHEMBL4466948 — IC50 = 5100.0 nM 5.29
CHEMBL4540166 — IC50 = 5300.0 nM 5.28
CHEMBL4566144 — IC50 = 6000.0 nM 5.22
CHEMBL4581637 — IC50 = 6200.0 nM 5.21
CHEMBL4445181 — IC50 = 6600.0 nM 5.18
CHEMBL4450408 — IC50 = 6600.0 nM 5.18
CHEMBL4443222 — IC50 = 8900.0 nM 5.05
CHEMBL4443953 — IC50 = 9200.0 nM 5.04
CHEMBL4441277 — IC50 = 9400.0 nM 5.03
CHEMBL4549918 — IC50 = 10000.0 nM 5.00
CHEMBL4449792 — IC50 = 11000.0 nM 4.96
CHEMBL4563474 — IC50 = 11000.0 nM 4.96
CHEMBL4534109 — IC50 = 11000.0 nM 4.96
CHEMBL4531433 — IC50 = 12000.0 nM 4.92