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Assay Detail

CHEMBL2329016

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Binding
Inhibition of Escherichia coli thymidylate synthase A
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Thymidylate synthase (CHEMBL2555)
Type SINGLE PROTEIN
Organism Escherichia coli K-12

Publication

Ligand-based discovery of N-(1,3-dioxo-1H,3H-benzo[de]isochromen-5-yl)-carboxamide and sulfonamide derivatives as thymidylate synthase A inhibitors.
Ferrari S, Ingrami M, Soragni F, Wade RC, Costi MP.
Bioorg Med Chem Lett (2013) 23 : 663 -668
PubMed 23273520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 45 5.34 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2323403 1 6.52
CHEMBL2323397 1 6.05
CHEMBL2323395 1 5.96
CHEMBL2323390 1 5.92
CHEMBL2323393 1 5.92
CHEMBL2323392 1 5.89
CHEMBL2323362 1 5.72
CHEMBL2323389 1 5.68
CHEMBL2323391 1 5.66
CHEMBL2323396 1 5.54
CHEMBL2323383 1 5.40
CHEMBL2323388 1 5.38
CHEMBL2323382 1 5.36
CHEMBL2323394 1 5.34
CHEMBL2323385 1 5.28
CHEMBL2323402 1 5.21
CHEMBL2323386 1 5.19
CHEMBL2323381 1 5.19
CHEMBL2323384 1 5.17
CHEMBL2323377 1 5.17
CHEMBL2323387 1 5.15
CHEMBL2323378 1 5.14
CHEMBL2323398 1 5.13
CHEMBL2323400 1 4.97
CHEMBL2323379 1 4.77
CHEMBL2323380 1 4.67
CHEMBL2323371 1 4.57
CHEMBL2323399 1 4.49
CHEMBL2323401 1 4.35
CHEMBL2323364 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2323403 Ki = 300.0 nM 6.52
CHEMBL2323397 Ki = 900.0 nM 6.05
CHEMBL2323395 Ki = 1100.0 nM 5.96
CHEMBL2323390 Ki = 1200.0 nM 5.92
CHEMBL2323393 Ki = 1200.0 nM 5.92
CHEMBL2323392 Ki = 1300.0 nM 5.89
CHEMBL2323362 Ki = 1900.0 nM 5.72
CHEMBL2323389 Ki = 2100.0 nM 5.68
CHEMBL2323391 Ki = 2200.0 nM 5.66
CHEMBL2323396 Ki = 2900.0 nM 5.54
CHEMBL2323383 Ki = 4000.0 nM 5.40
CHEMBL2323388 Ki = 4200.0 nM 5.38
CHEMBL2323382 Ki = 4400.0 nM 5.36
CHEMBL2323394 Ki = 4600.0 nM 5.34
CHEMBL2323385 Ki = 5300.0 nM 5.28
CHEMBL2323402 Ki = 6100.0 nM 5.21
CHEMBL2323386 Ki = 6500.0 nM 5.19
CHEMBL2323381 Ki = 6400.0 nM 5.19
CHEMBL2323384 Ki = 6700.0 nM 5.17
CHEMBL2323377 Ki = 6800.0 nM 5.17
CHEMBL2323387 Ki = 7100.0 nM 5.15
CHEMBL2323378 Ki = 7300.0 nM 5.14
CHEMBL2323398 Ki = 7400.0 nM 5.13
CHEMBL2323400 Ki = 10600.0 nM 4.97
CHEMBL2323379 Ki = 17000.0 nM 4.77
CHEMBL2323380 Ki = 21600.0 nM 4.67
CHEMBL2323371 Ki = 26800.0 nM 4.57
CHEMBL2323399 Ki = 32300.0 nM 4.49
CHEMBL2323401 Ki = 44700.0 nM 4.35
CHEMBL2323370 Ki = 105000.0 nM -
CHEMBL2323376 Ki > 196000.0 nM -
CHEMBL2323375 Ki > 152000.0 nM -
CHEMBL2323374 Ki > 588000.0 nM -
CHEMBL2323373 Ki > 451000.0 nM -
CHEMBL2323372 Ki > 784000.0 nM -
CHEMBL316059 1,8-NAPHTHALIC ANHYDRIDE Ki > 294000.0 nM -
CHEMBL2323369 Ki > 294000.0 nM -
CHEMBL2323368 Ki > 588000.0 nM -
CHEMBL1479195 Ki > 304000.0 nM -
CHEMBL2323367 Ki > 294000.0 nM -
CHEMBL2314369 Ki > 294000.0 nM -
CHEMBL2323366 Ki > 294000.0 nM -
CHEMBL2323365 Ki > 103000.0 nM -
CHEMBL2323363 Ki > 265000.0 nM -
CHEMBL2323364 Ki > 196000.0 nM -