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Assay Detail

CHEMBL993111

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

Binding
Inhibition of human recombinant PARP1
58
Total Activities
58
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors.
Zhang WT, Ruan JL, Wu PF, Jiang FC, Zhang LN, Fang W, Chen XL, Wang Y, Cao BS, Chen GY, Zhu YJ, Gu J, Chen JG.
J Med Chem (2009) 52 : 718 -725
PubMed 19125579 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 58 7.03 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481511 1 8.52
CHEMBL370838 1 8.42
CHEMBL370217 1 8.39
CHEMBL196444 1 8.30
CHEMBL196450 1 8.17
CHEMBL195402 1 7.92
CHEMBL251030 1 7.89
CHEMBL401843 1 7.80
CHEMBL195913 1 7.72
CHEMBL371425 1 7.70
CHEMBL399725 1 7.68
CHEMBL251028 1 7.64
CHEMBL433356 1 7.60
CHEMBL480039 1 7.60
CHEMBL479471 1 7.58
CHEMBL479861 1 7.57
CHEMBL371205 1 7.48
CHEMBL371244 1 7.44
CHEMBL510733 1 7.35
CHEMBL480234 1 7.34
CHEMBL381208 1 7.30
CHEMBL196507 1 7.26
CHEMBL372450 1 7.25
CHEMBL480613 1 7.20
CHEMBL425201 1 7.19
CHEMBL519443 1 7.15
CHEMBL443077 1 7.06
CHEMBL519778 1 7.06
CHEMBL381652 1 7.05
CHEMBL425560 1 7.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481511 IC50 = 3.0 nM 8.52
CHEMBL370838 IC50 = 3.8 nM 8.42
CHEMBL370217 IC50 = 4.1 nM 8.39
CHEMBL196444 IC50 = 5.0 nM 8.30
CHEMBL196450 IC50 = 6.8 nM 8.17
CHEMBL195402 IC50 = 12.0 nM 7.92
CHEMBL251030 IC50 = 13.0 nM 7.89
CHEMBL401843 IC50 = 16.0 nM 7.80
CHEMBL195913 IC50 = 19.0 nM 7.72
CHEMBL371425 IC50 = 20.0 nM 7.70
CHEMBL399725 IC50 = 21.0 nM 7.68
CHEMBL251028 IC50 = 23.0 nM 7.64
CHEMBL433356 IC50 = 25.0 nM 7.60
CHEMBL480039 IC50 = 25.0 nM 7.60
CHEMBL479471 IC50 = 26.0 nM 7.58
CHEMBL479861 IC50 = 27.0 nM 7.57
CHEMBL371205 IC50 = 33.0 nM 7.48
CHEMBL371244 IC50 = 36.0 nM 7.44
CHEMBL510733 IC50 = 45.0 nM 7.35
CHEMBL480234 IC50 = 46.0 nM 7.34
CHEMBL381208 IC50 = 50.0 nM 7.30
CHEMBL196507 IC50 = 55.0 nM 7.26
CHEMBL372450 IC50 = 56.0 nM 7.25
CHEMBL480613 IC50 = 63.0 nM 7.20
CHEMBL425201 IC50 = 64.0 nM 7.19
CHEMBL519443 IC50 = 71.0 nM 7.15
CHEMBL519778 IC50 = 88.0 nM 7.06
CHEMBL443077 IC50 = 87.0 nM 7.06
CHEMBL381652 IC50 = 90.0 nM 7.05
CHEMBL425560 IC50 = 90.0 nM 7.05
CHEMBL481403 IC50 = 97.0 nM 7.01
CHEMBL473036 IC50 = 100.0 nM 7.00
CHEMBL481603 IC50 = 101.0 nM 7.00
CHEMBL372303 PJ34 IC50 = 110.0 nM 6.96
CHEMBL480227 IC50 = 109.0 nM 6.96
CHEMBL481204 IC50 = 111.0 nM 6.96
CHEMBL320031 IC50 = 116.0 nM 6.94
CHEMBL521428 IC50 = 118.0 nM 6.93
CHEMBL194482 IC50 = 119.0 nM 6.92
CHEMBL196559 IC50 = 120.0 nM 6.92
CHEMBL294060 IC50 = 141.0 nM 6.85
CHEMBL520924 IC50 = 161.0 nM 6.79
CHEMBL106154 IC50 = 180.0 nM 6.75
CHEMBL322268 IC50 = 200.0 nM 6.70
CHEMBL452100 IC50 = 224.0 nM 6.65
CHEMBL452158 IC50 = 240.0 nM 6.62
CHEMBL480452 IC50 = 240.0 nM 6.62
CHEMBL480614 IC50 = 249.0 nM 6.60
CHEMBL480615 IC50 = 274.0 nM 6.56
CHEMBL480108 IC50 = 299.0 nM 6.52