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Assay Detail

CHEMBL1111552

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Binding
Inhibition of PARP1
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of tricyclic derivatives containing a non-aromatic amide as inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1).
Park CH, Chun K, Joe BY, Park JS, Kim YC, Choi JS, Ryu DK, Koh SH, Cho GW, Kim SH, Kim MH.
Bioorg Med Chem Lett (2010) 20 : 2250 -2253
PubMed 20189385 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.27 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1089713 1 7.89
CHEMBL1092777 1 7.60
CHEMBL1093295 1 7.55
CHEMBL1092144 1 7.54
CHEMBL1090020 1 7.42
CHEMBL1092776 1 7.41
CHEMBL1092145 1 7.40
CHEMBL190434 1 7.40
CHEMBL1094039 1 7.38
CHEMBL1091454 1 7.35
CHEMBL1090019 1 7.28
CHEMBL1092778 1 7.25
CHEMBL1092143 1 7.15
CHEMBL1093610 1 7.10
CHEMBL1091710 1 7.00
CHEMBL1089332 1 6.76
CHEMBL1090018 1 6.16
CHEMBL1089020 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1089713 IC50 = 13.0 nM 7.89
CHEMBL1092777 IC50 = 25.0 nM 7.60
CHEMBL1093295 IC50 = 28.0 nM 7.55
CHEMBL1092144 IC50 = 29.0 nM 7.54
CHEMBL1090020 IC50 = 38.0 nM 7.42
CHEMBL1092776 IC50 = 39.0 nM 7.41
CHEMBL1092145 IC50 = 40.0 nM 7.40
CHEMBL190434 IC50 = 40.0 nM 7.40
CHEMBL1094039 IC50 = 42.0 nM 7.38
CHEMBL1091454 IC50 = 45.0 nM 7.35
CHEMBL1090019 IC50 = 53.0 nM 7.28
CHEMBL1092778 IC50 = 56.0 nM 7.25
CHEMBL1092143 IC50 = 71.0 nM 7.15
CHEMBL1093610 IC50 = 80.0 nM 7.10
CHEMBL1091710 IC50 = 99.0 nM 7.00
CHEMBL1089332 IC50 = 173.0 nM 6.76
CHEMBL1090018 IC50 = 695.0 nM 6.16
CHEMBL1089020 IC50 > 10000.0 nM -