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Assay Detail

CHEMBL1763333

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

Binding
Inhibition of c-Jun
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Transcription factor Jun (CHEMBL4977)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and SAR of novel quinazolines as potent and brain-penetrant c-jun N-terminal kinase (JNK) inhibitors.
He Y, Kamenecka TM, Shin Y, Song X, Jiang R, Noel R, Duckett D, Chen W, Ling YY, Cameron MD, Lin L, Khan S, Koenig M, LoGrasso PV.
Bioorg Med Chem Lett (2011) 21 : 1719 -1723
PubMed 21316221 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 31 6.57 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1761563 1 7.70
CHEMBL1761583 1 7.40
CHEMBL1761582 1 7.40
CHEMBL1761561 1 7.40
CHEMBL1761584 1 7.30
CHEMBL1761577 1 7.00
CHEMBL1761555 1 6.92
CHEMBL1761581 1 6.89
CHEMBL1761579 1 6.80
CHEMBL1761569 1 6.70
CHEMBL1761565 1 6.60
CHEMBL1761562 1 6.54
CHEMBL1761554 1 6.51
CHEMBL1761564 1 6.48
CHEMBL1761568 1 6.30
CHEMBL1761578 1 6.21
CHEMBL1761572 1 6.20
CHEMBL1761575 1 6.03
CHEMBL1761567 1 5.85
CHEMBL1761576 1 5.52
CHEMBL1761566 1 5.52
CHEMBL1761570 1 5.29
CHEMBL1761574 1 -
CHEMBL1761573 1 -
CHEMBL1761571 1 -
CHEMBL1761558 1 -
CHEMBL1761580 1 -
CHEMBL1761559 1 -
CHEMBL1761557 1 -
CHEMBL1761556 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1761563 IC50 = 20.0 nM 7.70
CHEMBL1761583 IC50 = 40.0 nM 7.40
CHEMBL1761582 IC50 = 40.0 nM 7.40
CHEMBL1761561 IC50 = 40.0 nM 7.40
CHEMBL1761584 IC50 = 50.0 nM 7.30
CHEMBL1761577 IC50 = 100.0 nM 7.00
CHEMBL1761555 IC50 = 120.0 nM 6.92
CHEMBL1761581 IC50 = 130.0 nM 6.89
CHEMBL1761579 IC50 = 160.0 nM 6.80
CHEMBL1761569 IC50 = 200.0 nM 6.70
CHEMBL1761565 IC50 = 250.0 nM 6.60
CHEMBL1761562 IC50 = 290.0 nM 6.54
CHEMBL1761554 IC50 = 310.0 nM 6.51
CHEMBL1761564 IC50 = 330.0 nM 6.48
CHEMBL1761568 IC50 = 500.0 nM 6.30
CHEMBL1761578 IC50 = 620.0 nM 6.21
CHEMBL1761572 IC50 = 630.0 nM 6.20
CHEMBL1761575 IC50 = 930.0 nM 6.03
CHEMBL1761567 IC50 = 1400.0 nM 5.85
CHEMBL1761576 IC50 = 3000.0 nM 5.52
CHEMBL1761566 IC50 = 3000.0 nM 5.52
CHEMBL1761570 IC50 = 5100.0 nM 5.29
CHEMBL1761574 IC50 - -
CHEMBL1761573 IC50 - -
CHEMBL1761571 IC50 - -
CHEMBL1761558 IC50 - -
CHEMBL1761580 IC50 - -
CHEMBL1761559 IC50 - -
CHEMBL1761557 IC50 - -
CHEMBL1761556 IC50 - -
CHEMBL1761560 IC50 - -