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Assay Detail

CHEMBL840150

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

Binding
Inhibitory potency against human cloned Carbonic anhydrase II expressed in Escherichia coli strain BL21
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 Expert

Target

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

Publication

Carbonic anhydrase inhibitors. Novel sulfanilamide/acetazolamide derivatives obtained by the tail approach and their interaction with the cytosolic isozymes I and II, and the tumor-associated isozyme IX.
Turkmen H, Durgun M, Yilmaztekin S, Emul M, Innocenti A, Vullo D, Scozzafava A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 367 -372
PubMed 15603956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.54 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL182634 1 9.05
CHEMBL179897 1 8.80
CHEMBL183705 1 8.74
CHEMBL360097 1 8.72
CHEMBL183442 1 8.42
CHEMBL17 DICHLORPHENAMIDE 4.0 1 8.10
CHEMBL218490 DORZOLAMIDE 4.0 1 8.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.42
CHEMBL265674 1 7.22
CHEMBL183450 1 7.11
CHEMBL183775 1 7.09
CHEMBL180943 1 7.06
CHEMBL360041 1 6.98
CHEMBL183763 1 6.78
CHEMBL182476 1 6.76
CHEMBL182637 1 6.63
CHEMBL182523 1 6.59
CHEMBL182185 1 6.58
CHEMBL21 SULFANILAMIDE 4.0 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL182634 Ki = 0.9 nM 9.05
CHEMBL179897 Ki = 1.6 nM 8.80
CHEMBL183705 Ki = 1.8 nM 8.74
CHEMBL360097 Ki = 1.9 nM 8.72
CHEMBL183442 Ki = 3.8 nM 8.42
CHEMBL17 DICHLORPHENAMIDE Ki = 8.0 nM 8.10
CHEMBL218490 DORZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL18 ETHOXZOLAMIDE Ki = 38.0 nM 7.42
CHEMBL265674 Ki = 60.0 nM 7.22
CHEMBL183450 Ki = 77.0 nM 7.11
CHEMBL183775 Ki = 82.0 nM 7.09
CHEMBL180943 Ki = 87.0 nM 7.06
CHEMBL360041 Ki = 104.0 nM 6.98
CHEMBL183763 Ki = 165.0 nM 6.78
CHEMBL182476 Ki = 173.0 nM 6.76
CHEMBL182637 Ki = 234.0 nM 6.63
CHEMBL182523 Ki = 258.0 nM 6.59
CHEMBL182185 Ki = 265.0 nM 6.58
CHEMBL21 SULFANILAMIDE Ki = 300.0 nM 6.52