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Assay Detail

CHEMBL3993916

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

Binding
Inhibition of human recombinant carbonic anhydrase 4 incubated for 15 mins prior to testing by stopped-flow CO2 hydration assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 4 (CHEMBL3729)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel indolin-2-one-based sulfonamides as carbonic anhydrase inhibitors: Synthesis, in vitro biological evaluation against carbonic anhydrases isoforms I, II, IV and VII and molecular docking studies.
Eldehna WM, Al-Ansary GH, Bua S, Nocentini A, Gratteri P, Altoukhy A, Ghabbour H, Ahmed HY, Supuran CT.
Eur J Med Chem (2017) 127 : 521 -530
PubMed 28109946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.05 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067135 1 8.40
CHEMBL4069845 1 7.79
CHEMBL4078069 1 7.58
CHEMBL4095939 1 7.51
CHEMBL4096684 1 7.48
CHEMBL4085590 1 7.44
CHEMBL4088398 1 7.44
CHEMBL4103521 1 7.43
CHEMBL4060777 1 7.39
CHEMBL4096121 1 7.37
CHEMBL4088987 1 7.35
CHEMBL4077244 1 7.34
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.13
CHEMBL4085952 1 7.10
CHEMBL4099138 1 6.57
CHEMBL4066127 1 6.57
CHEMBL4081098 1 6.48
CHEMBL7087 1 6.46
CHEMBL4080175 1 5.84
CHEMBL4104409 1 5.75
CHEMBL4069467 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067135 Ki = 4.0 nM 8.40
CHEMBL4069845 Ki = 16.3 nM 7.79
CHEMBL4078069 Ki = 26.6 nM 7.58
CHEMBL4095939 Ki = 31.2 nM 7.51
CHEMBL4096684 Ki = 33.1 nM 7.48
CHEMBL4085590 Ki = 36.3 nM 7.44
CHEMBL4088398 Ki = 36.6 nM 7.44
CHEMBL4103521 Ki = 36.7 nM 7.43
CHEMBL4060777 Ki = 40.7 nM 7.39
CHEMBL4096121 Ki = 42.8 nM 7.37
CHEMBL4088987 Ki = 44.7 nM 7.35
CHEMBL4077244 Ki = 46.1 nM 7.34
CHEMBL20 ACETAZOLAMIDE Ki = 74.0 nM 7.13
CHEMBL4085952 Ki = 79.4 nM 7.10
CHEMBL4099138 Ki = 270.2 nM 6.57
CHEMBL4066127 Ki = 272.3 nM 6.57
CHEMBL4081098 Ki = 329.3 nM 6.48
CHEMBL7087 Ki = 348.8 nM 6.46
CHEMBL4080175 Ki = 1433.5 nM 5.84
CHEMBL4104409 Ki = 1799.5 nM 5.75
CHEMBL4069467 Ki = 2069.5 nM 5.68