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Assay Detail

CHEMBL834062

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 227L+106A
15
Total Activities
15
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 15 7.94 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL175691 RILPIVIRINE 4.0 1 9.00
CHEMBL367969 1 8.50
CHEMBL424781 1 8.40
CHEMBL177437 1 8.40
CHEMBL177643 1 8.40
CHEMBL2096760 1 8.30
CHEMBL443047 1 8.30
CHEMBL177703 1 8.10
CHEMBL70442 1 7.90
CHEMBL223228 EFAVIRENZ 4.0 1 7.60
CHEMBL175913 1 7.60
CHEMBL368555 1 7.50
CHEMBL360489 1 7.30
CHEMBL369875 1 6.90
CHEMBL369518 1 6.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL175691 RILPIVIRINE EC50 = 1.0 nM 9.00
CHEMBL367969 EC50 = 3.16 nM 8.50
CHEMBL424781 EC50 = 4.0 nM 8.40
CHEMBL177437 EC50 = 4.0 nM 8.40
CHEMBL177643 EC50 = 4.0 nM 8.40
CHEMBL2096760 EC50 = 5.0 nM 8.30
CHEMBL443047 EC50 = 5.0 nM 8.30
CHEMBL177703 EC50 = 7.95 nM 8.10
CHEMBL70442 EC50 = 12.6 nM 7.90
CHEMBL223228 EFAVIRENZ EC50 = 25.1 nM 7.60
CHEMBL175913 EC50 = 25.1 nM 7.60
CHEMBL368555 EC50 = 31.6 nM 7.50
CHEMBL360489 EC50 = 50.0 nM 7.30
CHEMBL369875 EC50 = 125.0 nM 6.90
CHEMBL369518 EC50 = 125.0 nM 6.90