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Assay Detail

CHEMBL766844

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

Binding
In vitro inhibitory activity against protein kinase A
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism unidentified
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

cAMP-dependent protein kinase (PKA) (CHEMBL2094138)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.
Dow RL, Chou TT, Bechle BM, Goddard C, Larson ER.
J Med Chem (1994) 37 : 2224 -2231
PubMed 7518523 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 4.97 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71144 1 6.30
CHEMBL6246 ELLAGIC ACID 2.0 1 6.22
CHEMBL304361 1 6.00
CHEMBL69174 1 5.82
CHEMBL72338 1 5.64
CHEMBL304362 1 5.50
CHEMBL302981 1 5.40
CHEMBL308175 1 5.38
CHEMBL304808 1 5.18
CHEMBL71002 1 5.16
CHEMBL305234 1 5.08
CHEMBL422771 1 5.00
CHEMBL70346 1 4.77
CHEMBL69237 1 4.70
CHEMBL73937 1 4.64
CHEMBL305223 1 4.40
CHEMBL73721 1 4.40
CHEMBL69240 1 4.33
CHEMBL308112 1 4.30
CHEMBL72035 1 4.30
CHEMBL302472 1 4.29
CHEMBL70659 1 4.24
CHEMBL421872 1 4.11
CHEMBL302483 1 4.04
CHEMBL70750 1 -
CHEMBL71205 1 -
CHEMBL70413 1 -
CHEMBL305966 1 -
CHEMBL266154 1 -
CHEMBL304983 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71144 IC50 = 500.0 nM 6.30
CHEMBL6246 ELLAGIC ACID IC50 = 600.0 nM 6.22
CHEMBL304361 IC50 = 1000.0 nM 6.00
CHEMBL69174 IC50 = 1500.0 nM 5.82
CHEMBL72338 IC50 = 2300.0 nM 5.64
CHEMBL304362 IC50 = 3200.0 nM 5.50
CHEMBL302981 IC50 = 4000.0 nM 5.40
CHEMBL308175 IC50 = 4200.0 nM 5.38
CHEMBL304808 IC50 = 6600.0 nM 5.18
CHEMBL71002 IC50 = 7000.0 nM 5.16
CHEMBL305234 IC50 = 8400.0 nM 5.08
CHEMBL422771 IC50 = 10000.0 nM 5.00
CHEMBL70346 IC50 = 17000.0 nM 4.77
CHEMBL69237 IC50 = 20000.0 nM 4.70
CHEMBL73937 IC50 = 23000.0 nM 4.64
CHEMBL305223 IC50 = 40000.0 nM 4.40
CHEMBL73721 IC50 = 40000.0 nM 4.40
CHEMBL69240 IC50 = 47000.0 nM 4.33
CHEMBL308112 IC50 = 50000.0 nM 4.30
CHEMBL72035 IC50 = 50000.0 nM 4.30
CHEMBL302472 IC50 = 51000.0 nM 4.29
CHEMBL70659 IC50 = 58000.0 nM 4.24
CHEMBL421872 IC50 = 78000.0 nM 4.11
CHEMBL302483 IC50 = 92000.0 nM 4.04
CHEMBL302325 IC50 = 168000.0 nM -
CHEMBL71210 IC50 = 390000.0 nM -
CHEMBL72682 IC50 > 2000000.0 nM -
CHEMBL305794 IC50 = 250000.0 nM -
CHEMBL70360 IC50 > 600000.0 nM -
CHEMBL307112 IC50 = 415000.0 nM -
CHEMBL306785 IC50 > 800000.0 nM -
CHEMBL308311 IC50 = 223000.0 nM -
CHEMBL71206 IC50 = 410000.0 nM -
CHEMBL70942 IC50 = 284000.0 nM -
CHEMBL308438 IC50 = 210000.0 nM -
CHEMBL306019 IC50 = 275000.0 nM -
CHEMBL70594 IC50 = 240000.0 nM -
CHEMBL305621 IC50 = 317000.0 nM -
CHEMBL302824 IC50 = 634000.0 nM -
CHEMBL304983 IC50 = 435000.0 nM -
CHEMBL266154 IC50 = 108000.0 nM -
CHEMBL305966 IC50 = 374000.0 nM -
CHEMBL70413 IC50 = 541000.0 nM -
CHEMBL71205 IC50 = 309000.0 nM -
CHEMBL70750 IC50 = 115000.0 nM -