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Assay Detail

CHEMBL4316151

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

Binding
Inhibition of recombinant human carbonic anhydrase-12 incubated for 15 mins by stopped flow CO2 hydrase assay
32
Total Activities
32
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 12 (CHEMBL3242)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological and molecular dynamics investigations with a series of triazolopyrimidine/triazole-based benzenesulfonamides as novel carbonic anhydrase inhibitors.
Said MA, Eldehna WM, Nocentini A, Bonardi A, Fahim SH, Bua S, Soliman DH, Abdel-Aziz HA, Gratteri P, Abou-Seri SM, Supuran CT.
Eur J Med Chem (2020) 185 : 111843 -111843
PubMed 31718943 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 32 7.65 8.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4587956 1 8.36
CHEMBL1615281 SLC-0111 1.0 1 8.35
CHEMBL20 ACETAZOLAMIDE 4.0 1 8.24
CHEMBL4559106 1 8.11
CHEMBL4585562 1 8.09
CHEMBL4555991 1 8.09
CHEMBL4529889 1 8.01
CHEMBL4578451 1 8.00
CHEMBL4458130 1 7.99
CHEMBL4446087 1 7.79
CHEMBL4470233 1 7.75
CHEMBL4461308 1 7.75
CHEMBL4455591 1 7.70
CHEMBL4452122 1 7.66
CHEMBL4441461 1 7.62
CHEMBL4520887 1 7.62
CHEMBL4552517 1 7.62
CHEMBL4561594 1 7.58
CHEMBL4579505 1 7.58
CHEMBL4538248 1 7.53
CHEMBL4535291 1 7.53
CHEMBL4441389 1 7.51
CHEMBL4462487 1 7.46
CHEMBL4586998 1 7.42
CHEMBL4553410 1 7.34
CHEMBL4538508 1 7.32
CHEMBL4459278 1 7.30
CHEMBL4526879 1 7.23
CHEMBL4555212 1 7.19
CHEMBL4458902 1 7.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4587956 Ki = 4.4 nM 8.36
CHEMBL1615281 SLC-0111 Ki = 4.5 nM 8.35
CHEMBL20 ACETAZOLAMIDE Ki = 5.7 nM 8.24
CHEMBL4559106 Ki = 7.8 nM 8.11
CHEMBL4585562 Ki = 8.1 nM 8.09
CHEMBL4555991 Ki = 8.2 nM 8.09
CHEMBL4529889 Ki = 9.8 nM 8.01
CHEMBL4578451 Ki = 9.9 nM 8.00
CHEMBL4458130 Ki = 10.2 nM 7.99
CHEMBL4446087 Ki = 16.2 nM 7.79
CHEMBL4470233 Ki = 17.6 nM 7.75
CHEMBL4461308 Ki = 17.6 nM 7.75
CHEMBL4455591 Ki = 19.9 nM 7.70
CHEMBL4452122 Ki = 21.9 nM 7.66
CHEMBL4520887 Ki = 23.8 nM 7.62
CHEMBL4552517 Ki = 23.8 nM 7.62
CHEMBL4441461 Ki = 24.1 nM 7.62
CHEMBL4561594 Ki = 26.0 nM 7.58
CHEMBL4579505 Ki = 26.2 nM 7.58
CHEMBL4538248 Ki = 29.5 nM 7.53
CHEMBL4535291 Ki = 29.4 nM 7.53
CHEMBL4441389 Ki = 31.0 nM 7.51
CHEMBL4462487 Ki = 34.4 nM 7.46
CHEMBL4586998 Ki = 38.3 nM 7.42
CHEMBL4553410 Ki = 45.3 nM 7.34
CHEMBL4538508 Ki = 48.2 nM 7.32
CHEMBL4459278 Ki = 49.7 nM 7.30
CHEMBL4526879 Ki = 59.3 nM 7.23
CHEMBL4555212 Ki = 64.3 nM 7.19
CHEMBL4458902 Ki = 73.6 nM 7.13
CHEMBL4458904 Ki = 103.9 nM 6.98
CHEMBL4455961 Ki = 105.0 nM 6.98