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Assay Detail

CHEMBL941003

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

Binding
Inhibition of human PARP1
33
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Poly [ADP-ribose] polymerase 1 (CHEMBL3105)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Rational design of conformationally restricted quinazolinone inhibitors of poly(ADP-ribose)polymerase.
Hattori K, Kido Y, Yamamoto H, Ishida J, Iwashita A, Mihara K.
Bioorg Med Chem Lett (2007) 17 : 5577 -5581
PubMed 17804225 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 7.20 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401843 1 8.10
CHEMBL248648 1 8.06
CHEMBL251028 1 8.05
CHEMBL250851 1 7.92
CHEMBL251030 1 7.89
CHEMBL248827 1 7.82
CHEMBL399725 1 7.80
CHEMBL251027 1 7.80
CHEMBL250488 1 7.80
CHEMBL250013 1 7.80
CHEMBL248826 1 7.75
CHEMBL400344 1 7.60
CHEMBL400343 1 7.60
CHEMBL399637 1 7.60
CHEMBL251029 1 7.58
CHEMBL250849 1 7.52
CHEMBL248649 1 7.46
CHEMBL249026 1 7.44
CHEMBL249813 1 7.34
CHEMBL250850 1 7.34
CHEMBL250490 1 7.33
CHEMBL250489 1 6.99
CHEMBL249220 1 6.88
CHEMBL250210 1 6.80
CHEMBL250672 1 6.59
CHEMBL248834 1 6.54
CHEMBL399635 1 6.52
CHEMBL246185 2 6.36
CHEMBL400581 1 6.30
CHEMBL250211 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401843 IC50 = 8.0 nM 8.10
CHEMBL248648 IC50 = 8.7 nM 8.06
CHEMBL251028 IC50 = 8.9 nM 8.05
CHEMBL250851 IC50 = 12.0 nM 7.92
CHEMBL251030 IC50 = 13.0 nM 7.89
CHEMBL248827 IC50 = 15.0 nM 7.82
CHEMBL399725 IC50 = 16.0 nM 7.80
CHEMBL251027 IC50 = 16.0 nM 7.80
CHEMBL250488 IC50 = 16.0 nM 7.80
CHEMBL250013 IC50 = 16.0 nM 7.80
CHEMBL248826 IC50 = 18.0 nM 7.75
CHEMBL400344 IC50 = 25.0 nM 7.60
CHEMBL400343 IC50 = 25.0 nM 7.60
CHEMBL399637 IC50 = 25.0 nM 7.60
CHEMBL251029 IC50 = 26.0 nM 7.58
CHEMBL250849 IC50 = 30.0 nM 7.52
CHEMBL248649 IC50 = 35.0 nM 7.46
CHEMBL249026 IC50 = 36.0 nM 7.44
CHEMBL249813 IC50 = 46.0 nM 7.34
CHEMBL250850 IC50 = 46.0 nM 7.34
CHEMBL250490 IC50 = 47.0 nM 7.33
CHEMBL250489 IC50 = 103.0 nM 6.99
CHEMBL249220 IC50 = 131.0 nM 6.88
CHEMBL250210 IC50 = 160.0 nM 6.80
CHEMBL250672 IC50 = 257.0 nM 6.59
CHEMBL248834 IC50 = 286.0 nM 6.54
CHEMBL399635 IC50 = 300.0 nM 6.52
CHEMBL246185 IC50 = 435.0 nM 6.36
CHEMBL400581 IC50 = 504.0 nM 6.30
CHEMBL246185 IC50 = 555.0 nM 6.26
CHEMBL250211 IC50 = 1600.0 nM 5.80
CHEMBL400299 IC50 = 1800.0 nM 5.75
CHEMBL250023 IC50 = 8400.0 nM 5.08