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Assay Detail

CHEMBL5366419

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Functional
Antiproliferative activity against human Olaparib-resistant CAPAN-1 cells assessed as cell proliferation inhibition incubated for 7 days by SRB assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type Olaparib-resistant CAPAN-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

YCH1899, a Highly Effective Phthalazin-1(2<i>H</i>)-one Derivative That Overcomes Resistance to Prior PARP Inhibitors.
Sun Y, Yang H, Yuan J, Wang L, Song S, Chen R, Bao X, Jia L, Yang T, Zhang X, He Q, Gan Y, Miao Z, He J, Yang C.
J Med Chem (2023) 66 : 12284 -12303
PubMed 37605459 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 33 6.58 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5402698 1 9.05
CHEMBL5428376 1 8.08
CHEMBL5408163 1 7.90
CHEMBL5425913 1 7.69
CHEMBL5437176 1 7.66
CHEMBL5438131 1 7.37
CHEMBL5437055 1 7.28
CHEMBL5425393 1 7.25
CHEMBL5436743 1 7.15
CHEMBL5395197 1 7.13
CHEMBL5412306 1 7.11
CHEMBL5436154 1 6.87
CHEMBL5417924 1 6.86
CHEMBL5416682 1 6.75
CHEMBL5421957 1 6.46
CHEMBL5423216 1 6.44
CHEMBL5433982 1 6.37
CHEMBL5425729 1 6.22
CHEMBL5401127 1 6.21
CHEMBL3137320 TALAZOPARIB 4.0 1 6.16
CHEMBL5427638 1 6.12
CHEMBL5425070 1 6.09
CHEMBL5435418 1 5.99
CHEMBL5397203 1 5.96
CHEMBL5432616 1 5.84
CHEMBL5429957 1 5.29
CHEMBL5419303 1 5.21
CHEMBL5410501 1 5.19
CHEMBL5436989 1 5.14
CHEMBL521686 OLAPARIB 4.0 1 4.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5402698 IC50 = 0.89 nM 9.05
CHEMBL5428376 IC50 = 8.28 nM 8.08
CHEMBL5408163 IC50 = 12.58 nM 7.90
CHEMBL5425913 IC50 = 20.33 nM 7.69
CHEMBL5437176 IC50 = 22.14 nM 7.66
CHEMBL5438131 IC50 = 42.25 nM 7.37
CHEMBL5437055 IC50 = 52.26 nM 7.28
CHEMBL5425393 IC50 = 56.4 nM 7.25
CHEMBL5436743 IC50 = 71.12 nM 7.15
CHEMBL5395197 IC50 = 73.63 nM 7.13
CHEMBL5412306 IC50 = 78.15 nM 7.11
CHEMBL5436154 IC50 = 135.03 nM 6.87
CHEMBL5417924 IC50 = 137.1 nM 6.86
CHEMBL5416682 IC50 = 178.48 nM 6.75
CHEMBL5421957 IC50 = 348.47 nM 6.46
CHEMBL5423216 IC50 = 363.12 nM 6.44
CHEMBL5433982 IC50 = 422.95 nM 6.37
CHEMBL5425729 IC50 = 604.54 nM 6.22
CHEMBL5401127 IC50 = 617.99 nM 6.21
CHEMBL3137320 TALAZOPARIB IC50 = 686.09 nM 6.16
CHEMBL5427638 IC50 = 766.42 nM 6.12
CHEMBL5425070 IC50 = 811.72 nM 6.09
CHEMBL5435418 IC50 = 1025.99 nM 5.99
CHEMBL5397203 IC50 = 1108.99 nM 5.96
CHEMBL5432616 IC50 = 1431.64 nM 5.84
CHEMBL5429957 IC50 = 5141.44 nM 5.29
CHEMBL5419303 IC50 = 6148.25 nM 5.21
CHEMBL5410501 IC50 = 6486.4 nM 5.19
CHEMBL5436989 IC50 = 7164.59 nM 5.14
CHEMBL521686 OLAPARIB IC50 = 21410.95 nM 4.67
CHEMBL5422190 IC50 > 10000.0 nM -
CHEMBL5404605 IC50 - -
CHEMBL5427132 IC50 - -