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Assay Detail

CHEMBL862669

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

Binding
Inhibitory activity against human recombinant cytosolic CA2
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Carbonic anhydrase 2 (CHEMBL205)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors. The mitochondrial isozyme VB as a new target for sulfonamide and sulfamate inhibitors.
Nishimori I, Vullo D, Innocenti A, Scozzafava A, Mastrolorenzo A, Supuran CT.
J Med Chem (2005) 48 : 7860 -7866
PubMed 16302824 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 7.38 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL268439 1 8.70
CHEMBL220491 BRINZOLAMIDE 4.0 1 8.52
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL73962 BENZOLAMIDE 1 8.05
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL220492 TOPIRAMATE 4.0 1 8.00
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL360356 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL6753 1 7.72
CHEMBL6685 1 7.52
CHEMBL6633 1 7.48
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL26 SULPIRIDE 3.0 1 7.40
CHEMBL6724 1 7.40
CHEMBL266026 1 7.34
CHEMBL7146 1 7.30
CHEMBL265674 1 7.22
CHEMBL6853 1 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE 1 7.20
CHEMBL268177 1 7.16
CHEMBL266240 1 7.12
CHEMBL6919 1 7.10
CHEMBL7092 1 6.96
CHEMBL6784 1 6.90
CHEMBL176495 1 6.90
CHEMBL414 CARZENIDE 2.0 1 6.88
CHEMBL7087 1 6.80
CHEMBL419 MAFENIDE 4.0 1 6.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL268439 Ki = 2.0 nM 8.70
CHEMBL220491 BRINZOLAMIDE Ki = 3.0 nM 8.52
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL73962 BENZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL220492 TOPIRAMATE Ki = 10.0 nM 8.00
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL360356 Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL6753 Ki = 19.0 nM 7.72
CHEMBL6685 Ki = 30.0 nM 7.52
CHEMBL6633 Ki = 33.0 nM 7.48
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL6724 Ki = 40.0 nM 7.40
CHEMBL26 SULPIRIDE Ki = 40.0 nM 7.40
CHEMBL266026 Ki = 46.0 nM 7.34
CHEMBL7146 Ki = 50.0 nM 7.30
CHEMBL265674 Ki = 60.0 nM 7.22
CHEMBL6853 Ki = 60.0 nM 7.22
CHEMBL418 2,4-DISULFAMYLTRIFLUOROMETHYLANILINE Ki = 63.0 nM 7.20
CHEMBL268177 Ki = 70.0 nM 7.16
CHEMBL266240 Ki = 75.0 nM 7.12
CHEMBL6919 Ki = 80.0 nM 7.10
CHEMBL7092 Ki = 110.0 nM 6.96
CHEMBL6784 Ki = 125.0 nM 6.90
CHEMBL176495 Ki = 125.0 nM 6.90
CHEMBL414 CARZENIDE Ki = 133.0 nM 6.88
CHEMBL7087 Ki = 160.0 nM 6.80
CHEMBL419 MAFENIDE Ki = 170.0 nM 6.77
CHEMBL21 SULFANILAMIDE Ki = 240.0 nM 6.62
CHEMBL6705 Ki = 295.0 nM 6.53
CHEMBL7204 Ki = 300.0 nM 6.52
CHEMBL574 P-TOLUENESULFONAMIDE Ki = 320.0 nM 6.50