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Assay Detail

CHEMBL907134

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

Binding
Inhibition of human cloned CA2 by CO2 hydration method
36
Total Activities
36
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

A novel class of carbonic anhydrase inhibitors: glycoconjugate benzene sulfonamides prepared by "click-tailing".
Wilkinson BL, Bornaghi LF, Houston TA, Innocenti A, Supuran CT, Poulsen SA.
J Med Chem (2006) 49 : 6539 -6548
PubMed 17064072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 36 7.51 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL216319 1 8.24
CHEMBL216208 1 8.17
CHEMBL425274 1 8.15
CHEMBL216214 1 8.15
CHEMBL217288 1 8.14
CHEMBL217303 1 8.14
CHEMBL216312 1 8.14
CHEMBL217359 1 8.14
CHEMBL386416 1 8.13
CHEMBL215105 1 8.12
CHEMBL216563 1 8.12
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.10
CHEMBL385152 1 8.09
CHEMBL214926 1 8.09
CHEMBL216245 1 8.07
CHEMBL220491 BRINZOLAMIDE 4.0 1 8.05
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.92
CHEMBL19 METHAZOLAMIDE 4.0 1 7.85
CHEMBL77517 INDISULAM 2.0 1 7.82
CHEMBL17 DICHLORPHENAMIDE 4.0 1 7.42
CHEMBL217304 1 7.36
CHEMBL217569 1 7.35
CHEMBL216210 1 7.35
CHEMBL386542 1 7.33
CHEMBL217454 1 7.30
CHEMBL410510 1 7.05
CHEMBL383897 1 6.92
CHEMBL217166 1 6.89
CHEMBL215182 1 6.66
CHEMBL217232 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL216319 Ki = 5.8 nM 8.24
CHEMBL216208 Ki = 6.8 nM 8.17
CHEMBL216214 Ki = 7.0 nM 8.15
CHEMBL425274 Ki = 7.0 nM 8.15
CHEMBL217288 Ki = 7.3 nM 8.14
CHEMBL217303 Ki = 7.3 nM 8.14
CHEMBL216312 Ki = 7.2 nM 8.14
CHEMBL217359 Ki = 7.3 nM 8.14
CHEMBL386416 Ki = 7.4 nM 8.13
CHEMBL216563 Ki = 7.6 nM 8.12
CHEMBL215105 Ki = 7.5 nM 8.12
CHEMBL18 ETHOXZOLAMIDE Ki = 8.0 nM 8.10
CHEMBL385152 Ki = 8.2 nM 8.09
CHEMBL214926 Ki = 8.1 nM 8.09
CHEMBL216245 Ki = 8.6 nM 8.07
CHEMBL220491 BRINZOLAMIDE Ki = 9.0 nM 8.05
CHEMBL20 ACETAZOLAMIDE Ki = 12.0 nM 7.92
CHEMBL19 METHAZOLAMIDE Ki = 14.0 nM 7.85
CHEMBL77517 INDISULAM Ki = 15.0 nM 7.82
CHEMBL17 DICHLORPHENAMIDE Ki = 38.0 nM 7.42
CHEMBL217304 Ki = 44.0 nM 7.36
CHEMBL217569 Ki = 45.0 nM 7.35
CHEMBL216210 Ki = 45.0 nM 7.35
CHEMBL386542 Ki = 47.0 nM 7.33
CHEMBL217454 Ki = 50.0 nM 7.30
CHEMBL410510 Ki = 90.0 nM 7.05
CHEMBL383897 Ki = 119.0 nM 6.92
CHEMBL217166 Ki = 128.0 nM 6.89
CHEMBL215182 Ki = 218.0 nM 6.66
CHEMBL217232 Ki = 265.0 nM 6.58
CHEMBL384644 Ki = 267.0 nM 6.57
CHEMBL386318 Ki = 279.0 nM 6.55
CHEMBL217683 Ki = 378.0 nM 6.42
CHEMBL387076 Ki = 384.0 nM 6.42
CHEMBL215156 Ki = 423.0 nM 6.37
CHEMBL386266 Ki = 470.0 nM 6.33