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Assay Detail

CHEMBL4684411

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

Binding
Inhibition of recombinant human carbonic anhydrase 9 preincubated with enzyme for 15 mins by phenol red dye based stopped flow CO2 hydrase assay
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 Autocuration

Target

Carbonic anhydrase 9 (CHEMBL3594)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfonamide-based ring-fused analogues for CAN508 as novel carbonic anhydrase inhibitors endowed with antitumor activity: Design, synthesis, and in vitro biological evaluation.
Said MA,Eldehna WM,Nocentini A,Fahim SH,Bonardi A,Elgazar AA,Kryštof V,Soliman DH,Abdel-Aziz HA,Gratteri P,Abou-Seri SM,Supuran CT
Eur J Med Chem (2020) 189 : 112019 -112019
PubMed 31972394 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.53 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4790806 1 8.22
CHEMBL4786073 1 8.06
CHEMBL4784840 1 8.03
CHEMBL4747175 1 7.78
CHEMBL1775075 1 7.66
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.60
CHEMBL4785207 1 7.55
CHEMBL4751980 1 7.53
CHEMBL4760748 1 7.50
CHEMBL4741017 1 7.50
CHEMBL4741899 1 7.47
CHEMBL4783101 1 7.42
CHEMBL4762561 1 7.40
CHEMBL4747714 1 7.35
CHEMBL4747600 1 7.35
CHEMBL4758858 1 7.34
CHEMBL4798487 1 7.25
CHEMBL4780776 1 7.19
CHEMBL4782119 1 7.18
CHEMBL4790351 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4790806 Ki = 6.0 nM 8.22
CHEMBL4786073 Ki = 8.8 nM 8.06
CHEMBL4784840 Ki = 9.4 nM 8.03
CHEMBL4747175 Ki = 16.6 nM 7.78
CHEMBL1775075 Ki = 22.0 nM 7.66
CHEMBL20 ACETAZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL4785207 Ki = 28.4 nM 7.55
CHEMBL4751980 Ki = 29.3 nM 7.53
CHEMBL4760748 Ki = 31.8 nM 7.50
CHEMBL4741017 Ki = 31.3 nM 7.50
CHEMBL4741899 Ki = 33.5 nM 7.47
CHEMBL4783101 Ki = 38.1 nM 7.42
CHEMBL4762561 Ki = 40.1 nM 7.40
CHEMBL4747714 Ki = 44.3 nM 7.35
CHEMBL4747600 Ki = 44.9 nM 7.35
CHEMBL4758858 Ki = 45.7 nM 7.34
CHEMBL4798487 Ki = 56.3 nM 7.25
CHEMBL4780776 Ki = 65.0 nM 7.19
CHEMBL4782119 Ki = 65.7 nM 7.18
CHEMBL4790351 Ki = 67.6 nM 7.17