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Assay Detail

CHEMBL2384053

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

Binding
Inhibition of recombinant human CA2 cytosolic isoform preincubated for 15 mins 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 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Xanthates and trithiocarbonates strongly inhibit carbonic anhydrases and show antiglaucoma effects in vivo.
Carta F, Akdemir A, Scozzafava A, Masini E, Supuran CT.
J Med Chem (2013) 56 : 4691 -4700
PubMed 23647428 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.25 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2380750 1 8.27
CHEMBL2380753 1 8.19
CHEMBL404954 1 8.18
CHEMBL2380746 1 8.09
CHEMBL2380747 1 8.02
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL2380751 1 7.88
CHEMBL2380752 1 7.67
CHEMBL2380749 1 7.35
CHEMBL2380748 1 7.23
CHEMBL2380745 1 7.22
CHEMBL2380755 1 7.13
CHEMBL2380754 1 7.12
CHEMBL2380744 1 6.53
CHEMBL2380740 1 6.53
CHEMBL2380738 1 6.52
CHEMBL2380739 1 6.51
CHEMBL2380742 1 6.47
CHEMBL2380737 1 6.46
CHEMBL2380743 1 6.44
CHEMBL2380741 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2380750 Ki = 5.4 nM 8.27
CHEMBL2380753 Ki = 6.4 nM 8.19
CHEMBL404954 Ki = 6.6 nM 8.18
CHEMBL2380746 Ki = 8.1 nM 8.09
CHEMBL2380747 Ki = 9.5 nM 8.02
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL2380751 Ki = 13.1 nM 7.88
CHEMBL2380752 Ki = 21.5 nM 7.67
CHEMBL2380749 Ki = 45.1 nM 7.35
CHEMBL2380748 Ki = 59.0 nM 7.23
CHEMBL2380745 Ki = 60.4 nM 7.22
CHEMBL2380755 Ki = 73.6 nM 7.13
CHEMBL2380754 Ki = 75.7 nM 7.12
CHEMBL2380744 Ki = 293.0 nM 6.53
CHEMBL2380740 Ki = 298.0 nM 6.53
CHEMBL2380738 Ki = 305.0 nM 6.52
CHEMBL2380739 Ki = 307.0 nM 6.51
CHEMBL2380742 Ki = 337.0 nM 6.47
CHEMBL2380737 Ki = 346.0 nM 6.46
CHEMBL2380743 Ki = 366.0 nM 6.44
CHEMBL2380741 Ki = 361.0 nM 6.44