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Assay Detail

CHEMBL702850

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Functional
Plasma equilibrium dissociation constant was determined
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Tissue Plasma
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
Hoffman JM, Smith AM, Rooney CS, Fisher TE, Wai JS, Thomas CM, Bamberger DL, Barnes JL, Williams TM, Jones JH.
J Med Chem (1993) 36 : 953 -966
PubMed 7683054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 5.21 6.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99235 1 6.12
CHEMBL329720 1 5.92
CHEMBL177016 1 5.61
CHEMBL171920 1 5.38
CHEMBL367052 1 5.09
CHEMBL176972 1 4.75
CHEMBL177271 1 4.74
CHEMBL83622 1 4.67
CHEMBL176362 1 4.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99235 Kd = 760.0 nM 6.12
CHEMBL329720 Kd = 1210.0 nM 5.92
CHEMBL177016 Kd = 2450.0 nM 5.61
CHEMBL171920 Kd = 4160.0 nM 5.38
CHEMBL367052 Kd = 8160.0 nM 5.09
CHEMBL176972 Kd = 17600.0 nM 4.75
CHEMBL177271 Kd = 18200.0 nM 4.74
CHEMBL83622 Kd = 21600.0 nM 4.67
CHEMBL176362 Kd = 24000.0 nM 4.62