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Assay Detail

CHEMBL5676672

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

Binding
Activation of PKC in human U1 cells infected with latent HIV-1 assessed as reversal of HIV-1 latency by measuring increase in p24 antigen level incubated for 48 hrs by chemiluminescent enzyme immunoassay
7
Total Activities
6
Compounds Tested
2
Activity Types
2
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type U1
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein kinase C (PKC) (CHEMBL2093867)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Benzolactam-related compounds promote apoptosis of HIV-infected human cells via protein kinase C-induced HIV latency reversal.
Matsuda K, Kobayakawa T, Tsuchiya K, Hattori SI, Nomura W, Gatanaga H, Yoshimura K, Oka S, Endo Y, Tamamura H, Mitsuya H, Maeda K.
J Biol Chem (2019) 294 : 116 -129
PubMed 30413535 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.08 7.47
Activity 1 - -

Assay Parameters

Parameter Type Value Units Text
EFO_ID EFO_ID - EFO:0000764
EFO_TERM EFO_TERM - hiv infection

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL34971 2 7.47
CHEMBL170518 PROSTRATIN 1 6.55
CHEMBL27266 INDOLACTUM 1 6.44
CHEMBL5678793 1 5.63
CHEMBL5678789 1 5.40
CHEMBL35696 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL34971 EC50 = 34.0 nM 7.47
CHEMBL170518 PROSTRATIN EC50 = 280.0 nM 6.55
CHEMBL27266 INDOLACTUM EC50 = 360.0 nM 6.44
CHEMBL5678793 EC50 = 2330.0 nM 5.63
CHEMBL5678789 EC50 = 4000.0 nM 5.40
CHEMBL35696 EC50 = 9890.0 nM 5.00
CHEMBL34971 Activity - -