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Assay Detail

CHEMBL833135

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Effective concentration against human immunodeficiency virus type 1 mutated at 100I+103N
12
Total Activities
12
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

Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1.
Guillemont J, Pasquier E, Palandjian P, Vernier D, Gaurrand S, Lewi PJ, Heeres J, de Jonge MR, Koymans LM, Daeyaert FF, Vinkers MH, Arnold E, Das K, Pauwels R, Andries K, de Béthune MP, Bettens E, Hertogs K, Wigerinck P, Timmerman P, Janssen PA.
J Med Chem (2005) 48 : 2072 -2079
PubMed 15771449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 7.21 8.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL443047 1 8.60
CHEMBL175691 RILPIVIRINE 4.0 1 8.10
CHEMBL367969 1 7.90
CHEMBL424781 1 7.50
CHEMBL177643 1 7.50
CHEMBL177703 1 7.50
CHEMBL360489 1 6.60
CHEMBL368555 1 6.30
CHEMBL177437 1 6.10
CHEMBL70442 1 6.00
CHEMBL223228 EFAVIRENZ 4.0 1 -
CHEMBL2096760 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL443047 EC50 = 2.51 nM 8.60
CHEMBL175691 RILPIVIRINE EC50 = 7.95 nM 8.10
CHEMBL367969 EC50 = 12.5 nM 7.90
CHEMBL424781 EC50 = 31.6 nM 7.50
CHEMBL177643 EC50 = 31.6 nM 7.50
CHEMBL177703 EC50 = 31.6 nM 7.50
CHEMBL360489 EC50 = 251.0 nM 6.60
CHEMBL368555 EC50 = 500.0 nM 6.30
CHEMBL177437 EC50 = 794.0 nM 6.10
CHEMBL70442 EC50 = 1000.0 nM 6.00
CHEMBL223228 EFAVIRENZ EC50 > 10.0 nM -
CHEMBL2096760 EC50 > 10000.0 nM -