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Assay Detail

CHEMBL2329241

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

Binding
Inhibition of human recombinant carbonic anhydrase 2 by dansylamide (DNSA) competition assay
13
Total Activities
13
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 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A multivalent approach towards linked dual-pharmacology prostaglandin F receptor agonist/carbonic anhydrase-II inhibitors for the treatment of glaucoma.
Long DD, Frieman B, Hegde SS, Hill CM, Jiang L, Kintz S, Marquess DG, Purkey H, Shaw JP, Steinfeld T, Wilson MS, Wrench K.
Bioorg Med Chem Lett (2013) 23 : 939 -943
PubMed 23317571 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 8.21 9.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL220491 BRINZOLAMIDE 4.0 1 9.90
CHEMBL218490 DORZOLAMIDE 4.0 1 9.70
CHEMBL2325977 1 9.20
CHEMBL2325981 1 8.90
CHEMBL2325976 1 8.30
CHEMBL2326219 1 8.10
CHEMBL2326218 1 8.10
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.10
CHEMBL2325978 1 7.40
CHEMBL2325975 1 7.40
CHEMBL2326217 1 7.30
CHEMBL2325980 1 7.30
CHEMBL2325979 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL220491 BRINZOLAMIDE Ki = 0.1259 nM 9.90
CHEMBL218490 DORZOLAMIDE Ki = 0.1995 nM 9.70
CHEMBL2325977 Ki = 0.631 nM 9.20
CHEMBL2325981 Ki = 1.259 nM 8.90
CHEMBL2325976 Ki = 5.012 nM 8.30
CHEMBL2326219 Ki = 7.943 nM 8.10
CHEMBL2326218 Ki = 7.943 nM 8.10
CHEMBL20 ACETAZOLAMIDE Ki = 7.943 nM 8.10
CHEMBL2325978 Ki = 39.81 nM 7.40
CHEMBL2325975 Ki = 39.81 nM 7.40
CHEMBL2326217 Ki = 50.12 nM 7.30
CHEMBL2325980 Ki = 50.12 nM 7.30
CHEMBL2325979 Ki = 100.0 nM 7.00