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Assay Detail

CHEMBL4379868

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

ADMET
Inhibition of recombinant human carbonic anhydrase 2 incubated for 1 hr prior to testing measured for 10 to 100 secs by phenol red-based stopped-flow CO2 hydration assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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 Sweet Combination": Developing Saccharin and Acesulfame K Structures for Selectively Targeting the Tumor-Associated Carbonic Anhydrases IX and XII.
Bua S, Lomelino C, Murray AB, Osman SM, ALOthman ZA, Bozdag M, Abdel-Aziz HA, Eldehna WM, McKenna R, Nocentini A, Supuran CT.
J Med Chem (2020) 63 : 321 -333
PubMed 31794211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.06 7.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.90
CHEMBL4453203 1 6.85
CHEMBL4437873 1 6.84
CHEMBL3976024 1 6.82
CHEMBL4474233 1 6.32
CHEMBL4542190 1 6.28
CHEMBL4571323 1 6.27
CHEMBL4550437 1 6.16
CHEMBL4587101 1 6.12
CHEMBL4521083 1 6.07
CHEMBL4553482 1 6.06
CHEMBL1615281 SLC-0111 1.0 1 6.02
CHEMBL4449637 1 5.97
CHEMBL4586255 1 5.94
CHEMBL4531304 1 5.72
CHEMBL4435951 1 5.66
CHEMBL4539322 1 5.63
CHEMBL4469385 1 5.63
CHEMBL4440314 1 5.61
CHEMBL4536306 1 5.53
CHEMBL4444406 1 5.52
CHEMBL310671 SACCHARIN 3.0 1 5.22
CHEMBL4442867 1 5.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20 ACETAZOLAMIDE Ki = 12.5 nM 7.90
CHEMBL4453203 Ki = 140.1 nM 6.85
CHEMBL4437873 Ki = 143.8 nM 6.84
CHEMBL3976024 Ki = 150.3 nM 6.82
CHEMBL4474233 Ki = 483.6 nM 6.32
CHEMBL4542190 Ki = 526.9 nM 6.28
CHEMBL4571323 Ki = 533.6 nM 6.27
CHEMBL4550437 Ki = 685.5 nM 6.16
CHEMBL4587101 Ki = 763.5 nM 6.12
CHEMBL4521083 Ki = 853.1 nM 6.07
CHEMBL4553482 Ki = 871.7 nM 6.06
CHEMBL1615281 SLC-0111 Ki = 960.0 nM 6.02
CHEMBL4449637 Ki = 1060.0 nM 5.97
CHEMBL4586255 Ki = 1141.0 nM 5.94
CHEMBL4531304 Ki = 1922.0 nM 5.72
CHEMBL4435951 Ki = 2192.0 nM 5.66
CHEMBL4539322 Ki = 2362.0 nM 5.63
CHEMBL4469385 Ki = 2337.0 nM 5.63
CHEMBL4440314 Ki = 2445.0 nM 5.61
CHEMBL4536306 Ki = 2936.0 nM 5.53
CHEMBL4444406 Ki = 3024.0 nM 5.52
CHEMBL310671 SACCHARIN Ki = 5950.0 nM 5.22
CHEMBL4442867 Ki = 6775.0 nM 5.17