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Assay Detail

CHEMBL3119218

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

Binding
Inhibition of demethylase activity of PCA-1 (unknown origin) using 3-methyl cytosine oligo DNA as substrate after 1 hr by RT-PCR analysis
49
Total Activities
49
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

Publication

Design and synthesis of prostate cancer antigen-1 (PCA-1/ALKBH3) inhibitors as anti-prostate cancer drugs.
Nakao S, Mabuchi M, Shimizu T, Itoh Y, Takeuchi Y, Ueda M, Mizuno H, Shigi N, Ohshio I, Jinguji K, Ueda Y, Yamamoto M, Furukawa T, Aoki S, Tsujikawa K, Tanaka A.
Bioorg Med Chem Lett (2014) 24 : 1071 -1074
PubMed 24461353 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 5.80 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3145429 1 6.32
CHEMBL3145446 1 6.31
CHEMBL3145436 1 6.27
CHEMBL3145440 1 6.26
CHEMBL3145451 1 6.24
CHEMBL3145441 1 6.22
CHEMBL3145447 1 6.21
CHEMBL3145442 1 6.20
CHEMBL3145448 1 6.19
CHEMBL3145419 1 6.17
CHEMBL3145452 1 6.17
CHEMBL3145443 1 6.14
CHEMBL3145410 1 6.14
CHEMBL3145430 1 6.12
CHEMBL3145412 1 6.12
CHEMBL3145413 1 6.11
CHEMBL3145449 1 6.09
CHEMBL3145411 1 6.04
CHEMBL3145408 1 5.82
CHEMBL3145246 1 5.77
CHEMBL3114990 1 5.70
CHEMBL3145409 1 5.68
CHEMBL3145427 1 5.58
CHEMBL3145439 1 5.51
CHEMBL3145435 1 5.48
CHEMBL3145417 1 5.44
CHEMBL3145414 1 5.43
CHEMBL3145421 1 5.40
CHEMBL3145444 1 5.39
CHEMBL3145431 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3145429 IC50 = 480.0 nM 6.32
CHEMBL3145446 IC50 = 490.0 nM 6.31
CHEMBL3145436 IC50 = 540.0 nM 6.27
CHEMBL3145440 IC50 = 550.0 nM 6.26
CHEMBL3145451 IC50 = 570.0 nM 6.24
CHEMBL3145441 IC50 = 600.0 nM 6.22
CHEMBL3145447 IC50 = 610.0 nM 6.21
CHEMBL3145442 IC50 = 630.0 nM 6.20
CHEMBL3145448 IC50 = 640.0 nM 6.19
CHEMBL3145419 IC50 = 670.0 nM 6.17
CHEMBL3145452 IC50 = 680.0 nM 6.17
CHEMBL3145443 IC50 = 720.0 nM 6.14
CHEMBL3145410 IC50 = 720.0 nM 6.14
CHEMBL3145430 IC50 = 750.0 nM 6.12
CHEMBL3145412 IC50 = 750.0 nM 6.12
CHEMBL3145413 IC50 = 780.0 nM 6.11
CHEMBL3145449 IC50 = 810.0 nM 6.09
CHEMBL3145411 IC50 = 910.0 nM 6.04
CHEMBL3145408 IC50 = 1500.0 nM 5.82
CHEMBL3145246 IC50 = 1700.0 nM 5.77
CHEMBL3114990 IC50 = 2000.0 nM 5.70
CHEMBL3145409 IC50 = 2100.0 nM 5.68
CHEMBL3145427 IC50 = 2600.0 nM 5.58
CHEMBL3145439 IC50 = 3100.0 nM 5.51
CHEMBL3145435 IC50 = 3300.0 nM 5.48
CHEMBL3145417 IC50 = 3600.0 nM 5.44
CHEMBL3145414 IC50 = 3700.0 nM 5.43
CHEMBL3145421 IC50 = 4000.0 nM 5.40
CHEMBL3145444 IC50 = 4100.0 nM 5.39
CHEMBL3145431 IC50 = 4300.0 nM 5.37
CHEMBL3145445 IC50 = 4500.0 nM 5.35
CHEMBL3145415 IC50 = 5300.0 nM 5.28
CHEMBL3114991 IC50 = 5800.0 nM 5.24
CHEMBL3145450 IC50 = 5900.0 nM 5.23
CHEMBL3145067 IC50 = 7200.0 nM 5.14
CHEMBL3145432 IC50 = 15000.0 nM 4.82
CHEMBL3145416 IC50 > 10000.0 nM -
CHEMBL3145422 IC50 > 10000.0 nM -
CHEMBL3145423 IC50 > 10000.0 nM -
CHEMBL3145424 IC50 > 10000.0 nM -
CHEMBL3145425 IC50 > 10000.0 nM -
CHEMBL3145426 IC50 > 10000.0 nM -
CHEMBL3145428 IC50 > 10000.0 nM -
CHEMBL3145433 IC50 > 10000.0 nM -
CHEMBL3145434 IC50 > 10000.0 nM -
CHEMBL3145418 IC50 > 10000.0 nM -
CHEMBL3145437 IC50 > 10000.0 nM -
CHEMBL3145420 IC50 > 10000.0 nM -
CHEMBL3145438 IC50 > 10000.0 nM -