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Assay Detail

CHEMBL1019872

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Functional
Antiproliferative activity against human A2780 cells after 72 hrs by luciferase based assay
ChEMBL ↗
45
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A2780
Confidence 1 — Organism
Curated By Autocuration

Target

A2780 (CHEMBL614004) ↗
Type CELL-LINE
Organism Homo sapiens

Publication

First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.
Menichincheri M, Bargiotti A, Berthelsen J, Bertrand JA, Bossi R, Ciavolella A, Cirla A, Cristiani C, Croci V, D'Alessio R, Fasolini M, Fiorentini F, Forte B, Isacchi A, Martina K, Molinari A, Montagnoli A, Orsini P, Orzi F, Pesenti E, Pezzetta D, Pillan A, Poggesi I, Roletto F, Scolaro A, Tatò M, Tibolla M, Valsasina B, Varasi M, Volpi D, Santocanale C, Vanotti E.
J Med Chem (2009) 52 : 293 -307
PubMed 19115845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.08 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459285 — — 1 6.70
CHEMBL459283 — — 1 6.70
CHEMBL449372 — — 1 6.70
CHEMBL497995 — — 3 6.70
CHEMBL498200 — — 3 6.52
CHEMBL495757 — — 1 6.52
CHEMBL496961 — — 1 6.52
CHEMBL445340 — — 3 6.40
CHEMBL526092 — — 3 6.40
CHEMBL498207 — — 1 6.40
CHEMBL524266 — — 1 6.30
CHEMBL513429 — — 1 6.30
CHEMBL509776 — — 1 6.30
CHEMBL447369 — — 1 6.22
CHEMBL443669 — — 1 6.22
CHEMBL459284 — — 1 6.16
CHEMBL496772 — — 1 6.10
CHEMBL444154 — — 1 6.05
CHEMBL451570 — — 1 6.00
CHEMBL225519 — — 1 5.96
CHEMBL451213 — — 1 5.96
CHEMBL495947 — — 1 5.96
CHEMBL523902 — — 1 5.96
CHEMBL496773 — — 1 5.92
CHEMBL525775 — — 1 5.89
CHEMBL522717 — — 1 5.89
CHEMBL495953 — — 1 5.80
CHEMBL402272 — — 1 5.77
CHEMBL495556 — — 1 5.75
CHEMBL522398 — — 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459283 — IC50 = 200.0 nM 6.70
CHEMBL459285 — IC50 = 200.0 nM 6.70
CHEMBL449372 — IC50 = 200.0 nM 6.70
CHEMBL497995 — IC50 = 200.0 nM 6.70
CHEMBL498200 — IC50 = 300.0 nM 6.52
CHEMBL495757 — IC50 = 300.0 nM 6.52
CHEMBL497995 — IC50 = 300.0 nM 6.52
CHEMBL496961 — IC50 = 300.0 nM 6.52
CHEMBL526092 — IC50 = 400.0 nM 6.40
CHEMBL445340 — IC50 = 400.0 nM 6.40
CHEMBL498207 — IC50 = 400.0 nM 6.40
CHEMBL526092 — IC50 = 400.0 nM 6.40
CHEMBL526092 — IC50 = 400.0 nM 6.40
CHEMBL513429 — IC50 = 500.0 nM 6.30
CHEMBL524266 — IC50 = 500.0 nM 6.30
CHEMBL498200 — IC50 = 500.0 nM 6.30
CHEMBL509776 — IC50 = 500.0 nM 6.30
CHEMBL447369 — IC50 = 600.0 nM 6.22
CHEMBL443669 — IC50 = 600.0 nM 6.22
CHEMBL445340 — IC50 = 600.0 nM 6.22
CHEMBL459284 — IC50 = 700.0 nM 6.16
CHEMBL496772 — IC50 = 800.0 nM 6.10
CHEMBL444154 — IC50 = 900.0 nM 6.05
CHEMBL445340 — IC50 = 1000.0 nM 6.00
CHEMBL498200 — IC50 = 1000.0 nM 6.00
CHEMBL451570 — IC50 = 1000.0 nM 6.00
CHEMBL225519 — IC50 = 1100.0 nM 5.96
CHEMBL451213 — IC50 = 1100.0 nM 5.96
CHEMBL495947 — IC50 = 1100.0 nM 5.96
CHEMBL523902 — IC50 = 1100.0 nM 5.96
CHEMBL496773 — IC50 = 1200.0 nM 5.92
CHEMBL525775 — IC50 = 1300.0 nM 5.89
CHEMBL522717 — IC50 = 1300.0 nM 5.89
CHEMBL497995 — IC50 = 1300.0 nM 5.89
CHEMBL495953 — IC50 = 1600.0 nM 5.80
CHEMBL402272 — IC50 = 1700.0 nM 5.77
CHEMBL495556 — IC50 = 1800.0 nM 5.75
CHEMBL522398 — IC50 = 2000.0 nM 5.70
CHEMBL449148 — IC50 = 2400.0 nM 5.62
CHEMBL522890 — IC50 = 3000.0 nM 5.52
CHEMBL522578 — IC50 = 3000.0 nM 5.52
CHEMBL495750 — IC50 = 3900.0 nM 5.41
CHEMBL512744 — IC50 = 4000.0 nM 5.40
CHEMBL495539 — IC50 = 4800.0 nM 5.32
CHEMBL496560 — IC50 = 6000.0 nM 5.22