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Assay Detail

CHEMBL679972

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Binding
Inhibitory activity against ErmC methylase
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bacillus subtilis
Confidence 9 — Direct single protein target
Curated By Expert

Target

rRNA adenine N-6-methyltransferase (CHEMBL4251)
Type SINGLE PROTEIN
Organism Bacillus subtilis

Publication

Novel inhibitors of Erm methyltransferases from NMR and parallel synthesis.
Hajduk PJ, Dinges J, Schkeryantz JM, Janowick D, Kaminski M, Tufano M, Augeri DJ, Petros A, Nienaber V, Zhong P, Hammond R, Coen M, Beutel B, Katz L, Fesik SW.
J Med Chem (1999) 42 : 3852 -3859
PubMed 10508434 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 4.48 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127777 1 5.00
CHEMBL125085 1 4.90
CHEMBL340522 1 4.70
CHEMBL125249 1 4.43
CHEMBL124572 1 4.12
CHEMBL333812 1 4.12
CHEMBL331440 1 4.12
CHEMBL124519 1 -
CHEMBL330769 1 -
CHEMBL127767 1 -
CHEMBL123502 1 -
CHEMBL126375 1 -
CHEMBL124981 1 -
CHEMBL333773 1 -
CHEMBL126068 1 -
CHEMBL127729 1 -
CHEMBL124520 1 -
CHEMBL331635 1 -
CHEMBL125250 1 -
CHEMBL332852 1 -
CHEMBL338033 1 -
CHEMBL419433 1 -
CHEMBL126964 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127777 Ki = 10000.0 nM 5.00
CHEMBL125085 Ki = 12500.0 nM 4.90
CHEMBL340522 Ki = 20000.0 nM 4.70
CHEMBL125249 Ki = 37000.0 nM 4.43
CHEMBL124572 Ki = 75000.0 nM 4.12
CHEMBL333812 Ki = 75000.0 nM 4.12
CHEMBL331440 Ki = 75000.0 nM 4.12
CHEMBL124519 Ki > 100000.0 nM -
CHEMBL330769 Ki > 100000.0 nM -
CHEMBL127767 Ki > 100000.0 nM -
CHEMBL123502 Ki > 100000.0 nM -
CHEMBL126375 Ki > 100000.0 nM -
CHEMBL124981 Ki > 100000.0 nM -
CHEMBL333773 Ki > 100000.0 nM -
CHEMBL126068 Ki > 100000.0 nM -
CHEMBL127729 Ki > 100000.0 nM -
CHEMBL124520 Ki > 100000.0 nM -
CHEMBL331635 Ki > 100000.0 nM -
CHEMBL125250 Ki > 100000.0 nM -
CHEMBL332852 Ki > 100000.0 nM -
CHEMBL338033 Ki > 100000.0 nM -
CHEMBL419433 Ki > 100000.0 nM -
CHEMBL126964 Ki > 50000.0 nM -