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Assay Detail

CHEMBL658041

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Binding
Inhibition constant evaluated for the inhibition of human CA II (Carbonic anhydrase II)
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Carbonic anhydrase inhibitors. Design of selective, membrane-impermeant inhibitors targeting the human tumor-associated isozyme IX.
Casey JR, Morgan PE, Vullo D, Scozzafava A, Mastrolorenzo A, Supuran CT.
J Med Chem (2004) 47 : 2337 -2347
PubMed 15084132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 8.64 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL77402 1 9.70
CHEMBL75812 1 9.68
CHEMBL264618 1 9.59
CHEMBL76206 1 9.52
CHEMBL75595 1 9.41
CHEMBL307401 1 8.94
CHEMBL307402 1 8.92
CHEMBL77986 1 8.91
CHEMBL420572 1 8.86
CHEMBL307259 1 8.81
CHEMBL309069 1 8.79
CHEMBL268439 1 8.69
CHEMBL73929 1 8.50
CHEMBL76078 1 8.46
CHEMBL263457 1 8.43
CHEMBL308820 1 8.41
CHEMBL78240 1 8.39
CHEMBL309890 1 8.34
CHEMBL307838 1 8.32
CHEMBL407460 1 8.31
CHEMBL77483 1 8.30
CHEMBL309578 1 8.22
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

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL77402 Ki = 0.2 nM 9.70
CHEMBL75812 Ki = 0.21 nM 9.68
CHEMBL264618 Ki = 0.26 nM 9.59
CHEMBL76206 Ki = 0.3 nM 9.52
CHEMBL75595 Ki = 0.39 nM 9.41
CHEMBL307401 Ki = 1.14 nM 8.94
CHEMBL307402 Ki = 1.21 nM 8.92
CHEMBL77986 Ki = 1.24 nM 8.91
CHEMBL420572 Ki = 1.37 nM 8.86
CHEMBL307259 Ki = 1.54 nM 8.81
CHEMBL309069 Ki = 1.61 nM 8.79
CHEMBL268439 Ki = 2.04 nM 8.69
CHEMBL73929 Ki = 3.13 nM 8.50
CHEMBL76078 Ki = 3.45 nM 8.46
CHEMBL263457 Ki = 3.74 nM 8.43
CHEMBL308820 Ki = 3.9 nM 8.41
CHEMBL78240 Ki = 4.11 nM 8.39
CHEMBL309890 Ki = 4.62 nM 8.34
CHEMBL307838 Ki = 4.78 nM 8.32
CHEMBL407460 Ki = 4.93 nM 8.31
CHEMBL77483 Ki = 4.95 nM 8.30
CHEMBL309578 Ki = 5.96 nM 8.22
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