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Assay Detail

CHEMBL909955

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Binding
Binding affinity to human caspase 3
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Caspase-3 (CHEMBL2334)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-pyrrolidinylsulfonyl isatins as a potential tool for the molecular imaging of caspases in apoptosis.
Kopka K, Faust A, Keul P, Wagner S, Breyholz HJ, Höltke C, Schober O, Schäfers M, Levkau B.
J Med Chem (2006) 49 : 6704 -6715
PubMed 17154501 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.23 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL213759 1 9.70
CHEMBL216071 1 9.10
CHEMBL216819 1 8.92
CHEMBL384023 1 8.92
CHEMBL387041 1 8.72
CHEMBL200927 1 8.40
CHEMBL200677 1 8.32
CHEMBL217457 1 8.23
CHEMBL216447 1 8.10
CHEMBL62993 1 8.08
CHEMBL386510 1 8.07
CHEMBL217777 1 8.05
CHEMBL217821 1 8.01
CHEMBL217822 (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(4-(tributylstannyl)benzyl)isatin 1 7.90
CHEMBL385930 1 7.90
CHEMBL215480 1 7.75
CHEMBL217220 1 7.63
CHEMBL60190 1 7.38
CHEMBL293034 1 7.25
CHEMBL386464 (S)-5-[1-(2-phenoxymethylpyrrolidinyl)sulfonyl]-1-(4-(tributylstannyl)benzyl)isatin 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL213759 Ki = 0.2 nM 9.70
CHEMBL216071 Ki = 0.8 nM 9.10
CHEMBL216819 Ki = 1.2 nM 8.92
CHEMBL384023 Ki = 1.2 nM 8.92
CHEMBL387041 Ki = 1.9 nM 8.72
CHEMBL200927 Ki = 4.0 nM 8.40
CHEMBL200677 Ki = 4.8 nM 8.32
CHEMBL217457 Ki = 5.9 nM 8.23
CHEMBL216447 Ki = 8.0 nM 8.10
CHEMBL62993 Ki = 8.3 nM 8.08
CHEMBL386510 Ki = 8.6 nM 8.07
CHEMBL217777 Ki = 9.0 nM 8.05
CHEMBL217821 Ki = 9.8 nM 8.01
CHEMBL217822 (S)-5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]-1-(4-(tributylstannyl)benzyl)isatin Ki = 12.6 nM 7.90
CHEMBL385930 Ki = 12.6 nM 7.90
CHEMBL215480 Ki = 17.9 nM 7.75
CHEMBL217220 Ki = 23.5 nM 7.63
CHEMBL60190 Ki = 41.8 nM 7.38
CHEMBL293034 Ki = 56.1 nM 7.25
CHEMBL386464 (S)-5-[1-(2-phenoxymethylpyrrolidinyl)sulfonyl]-1-(4-(tributylstannyl)benzyl)isatin Ki > 5000.0 nM -