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Assay Detail

CHEMBL827063

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Binding
Inhibitory constant against human Carbonic anhydrase I
44
Total Activities
44
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Carbonic anhydrase inhibitors: novel sulfonamides incorporating 1,3,5-triazine moieties as inhibitors of the cytosolic and tumour-associated carbonic anhydrase isozymes I, II and IX.
Garaj V, Puccetti L, Fasolis G, Winum JY, Montero JL, Scozzafava A, Vullo D, Innocenti A, Supuran CT.
Bioorg Med Chem Lett (2005) 15 : 3102 -3108
PubMed 15905091 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 44 6.59 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18 ETHOXZOLAMIDE 4.0 1 7.60
CHEMBL77517 INDISULAM 2.0 1 7.51
CHEMBL190024 1 7.51
CHEMBL189526 1 7.48
CHEMBL191045 1 7.46
CHEMBL190733 1 7.41
CHEMBL19 METHAZOLAMIDE 4.0 1 7.30
CHEMBL190023 1 7.20
CHEMBL189523 1 7.12
CHEMBL192834 1 7.12
CHEMBL363874 1 7.06
CHEMBL190550 1 7.03
CHEMBL364754 1 7.02
CHEMBL191380 1 6.98
CHEMBL190721 1 6.98
CHEMBL364919 1 6.95
CHEMBL371403 1 6.95
CHEMBL193178 1 6.89
CHEMBL191576 1 6.89
CHEMBL440026 1 6.81
CHEMBL190907 1 6.75
CHEMBL190538 1 6.75
CHEMBL189681 1 6.70
CHEMBL366223 1 6.63
CHEMBL189527 1 6.62
CHEMBL191884 1 6.61
CHEMBL20 ACETAZOLAMIDE 4.0 1 6.60
CHEMBL193513 1 6.43
CHEMBL434909 1 6.37
CHEMBL192950 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18 ETHOXZOLAMIDE Ki = 25.0 nM 7.60
CHEMBL77517 INDISULAM Ki = 31.0 nM 7.51
CHEMBL190024 Ki = 31.0 nM 7.51
CHEMBL189526 Ki = 33.0 nM 7.48
CHEMBL191045 Ki = 35.0 nM 7.46
CHEMBL190733 Ki = 39.0 nM 7.41
CHEMBL19 METHAZOLAMIDE Ki = 50.0 nM 7.30
CHEMBL190023 Ki = 63.0 nM 7.20
CHEMBL189523 Ki = 76.0 nM 7.12
CHEMBL192834 Ki = 75.0 nM 7.12
CHEMBL363874 Ki = 87.0 nM 7.06
CHEMBL190550 Ki = 93.0 nM 7.03
CHEMBL364754 Ki = 95.0 nM 7.02
CHEMBL191380 Ki = 105.0 nM 6.98
CHEMBL190721 Ki = 104.0 nM 6.98
CHEMBL364919 Ki = 112.0 nM 6.95
CHEMBL371403 Ki = 113.0 nM 6.95
CHEMBL193178 Ki = 130.0 nM 6.89
CHEMBL191576 Ki = 128.0 nM 6.89
CHEMBL440026 Ki = 156.0 nM 6.81
CHEMBL190907 Ki = 180.0 nM 6.75
CHEMBL190538 Ki = 176.0 nM 6.75
CHEMBL189681 Ki = 198.0 nM 6.70
CHEMBL366223 Ki = 235.0 nM 6.63
CHEMBL189527 Ki = 241.0 nM 6.62
CHEMBL191884 Ki = 247.0 nM 6.61
CHEMBL20 ACETAZOLAMIDE Ki = 250.0 nM 6.60
CHEMBL193513 Ki = 368.0 nM 6.43
CHEMBL434909 Ki = 425.0 nM 6.37
CHEMBL192950 Ki = 540.0 nM 6.27
CHEMBL190464 Ki = 549.0 nM 6.26
CHEMBL190278 Ki = 558.0 nM 6.25
CHEMBL190531 Ki = 561.0 nM 6.25
CHEMBL371632 Ki = 622.0 nM 6.21
CHEMBL190056 Ki = 613.0 nM 6.21
CHEMBL366276 Ki = 631.0 nM 6.20
CHEMBL372442 Ki = 875.0 nM 6.06
CHEMBL17 DICHLORPHENAMIDE Ki = 1200.0 nM 5.92
CHEMBL190329 Ki = 1560.0 nM 5.81
CHEMBL426625 Ki = 1635.0 nM 5.79
CHEMBL365380 Ki = 3500.0 nM 5.46
CHEMBL192670 Ki = 4200.0 nM 5.38
CHEMBL193008 Ki = 8500.0 nM 5.07
CHEMBL218490 DORZOLAMIDE Ki = 50000.0 nM 4.30