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Assay Detail

CHEMBL827685

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Functional
Effective concentration of against HIV Wild Type (IIIB) strain
17
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Discovery and selection of TMC114, a next generation HIV-1 protease inhibitor.
Surleraux DL, Tahri A, Verschueren WG, Pille GM, de Kock HA, Jonckers TH, Peeters A, De Meyer S, Azijn H, Pauwels R, de Bethune MP, King NM, Prabu-Jeyabalan M, Schiffer CA, Wigerinck PB.
J Med Chem (2005) 48 : 1813 -1822
PubMed 15771427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.16 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469086 1 9.23
CHEMBL178593 1 9.21
CHEMBL360661 1 8.82
CHEMBL366784 1 8.71
CHEMBL175861 1 8.61
CHEMBL176379 1 8.56
CHEMBL1323 DARUNAVIR 4.0 2 8.39
CHEMBL176275 1 8.36
CHEMBL366830 1 8.28
CHEMBL359662 1 8.28
CHEMBL177418 1 8.20
CHEMBL176823 1 8.15
CHEMBL175231 1 7.97
CHEMBL116 AMPRENAVIR 4.0 1 7.43
CHEMBL179266 1 6.62
CHEMBL262307 1 6.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469086 EC50 = 0.5888 nM 9.23
CHEMBL178593 EC50 = 0.6166 nM 9.21
CHEMBL360661 EC50 = 1.514 nM 8.82
CHEMBL366784 EC50 = 1.95 nM 8.71
CHEMBL175861 EC50 = 2.455 nM 8.61
CHEMBL176379 EC50 = 2.754 nM 8.56
CHEMBL1323 DARUNAVIR EC50 = 4.074 nM 8.39
CHEMBL176275 EC50 = 4.365 nM 8.36
CHEMBL366830 EC50 = 5.248 nM 8.28
CHEMBL359662 EC50 = 5.248 nM 8.28
CHEMBL177418 EC50 = 6.31 nM 8.20
CHEMBL176823 EC50 = 7.079 nM 8.15
CHEMBL175231 EC50 = 10.72 nM 7.97
CHEMBL116 AMPRENAVIR EC50 = 37.15 nM 7.43
CHEMBL1323 DARUNAVIR EC50 = 43.65 nM 7.36
CHEMBL179266 EC50 = 239.88 nM 6.62
CHEMBL262307 EC50 = 309.03 nM 6.51