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Assay Detail

CHEMBL1815535

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Binding
Inhibition of human recombinant carbonic anhydrase 14 preincubated for 15 mins by CO2 hydration method
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Carbonic anhydrase 14 (CHEMBL3510)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Sulfonamides incorporating 1,3,5-triazine moieties selectively and potently inhibit carbonic anhydrase transmembrane isoforms IX, XII and XIV over cytosolic isoforms I and II: Solution and X-ray crystallographic studies.
Carta F, Garaj V, Maresca A, Wagner J, Avvaru BS, Robbins AH, Scozzafava A, McKenna R, Supuran CT.
Bioorg Med Chem (2011) 19 : 3105 -3119
PubMed 21515057 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 7.82 9.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1813208 1 9.04
CHEMBL18 ETHOXZOLAMIDE 4.0 1 8.60
CHEMBL1738787 1 8.42
CHEMBL78755 1 8.39
CHEMBL1738792 1 8.19
CHEMBL1813207 1 8.15
CHEMBL1813206 1 8.14
CHEMBL1813210 1 8.13
CHEMBL1813219 1 8.12
CHEMBL1813218 1 8.06
CHEMBL1813214 1 8.05
CHEMBL1813213 1 8.04
CHEMBL191045 1 8.03
CHEMBL1813209 1 8.00
CHEMBL189526 1 7.98
CHEMBL187274 1 7.81
CHEMBL1813215 1 7.77
CHEMBL190024 1 7.75
CHEMBL190733 1 7.63
CHEMBL187901 1 7.62
CHEMBL1813211 1 7.56
CHEMBL366069 1 7.46
CHEMBL20 ACETAZOLAMIDE 4.0 1 7.39
CHEMBL1813216 1 7.14
CHEMBL1813217 1 7.11
CHEMBL17 DICHLORPHENAMIDE 4.0 1 6.46
CHEMBL1813212 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1813208 Ki = 0.92 nM 9.04
CHEMBL18 ETHOXZOLAMIDE Ki = 2.5 nM 8.60
CHEMBL1738787 Ki = 3.8 nM 8.42
CHEMBL78755 Ki = 4.1 nM 8.39
CHEMBL1738792 Ki = 6.5 nM 8.19
CHEMBL1813207 Ki = 7.0 nM 8.15
CHEMBL1813206 Ki = 7.2 nM 8.14
CHEMBL1813210 Ki = 7.4 nM 8.13
CHEMBL1813219 Ki = 7.6 nM 8.12
CHEMBL1813218 Ki = 8.8 nM 8.06
CHEMBL1813214 Ki = 8.9 nM 8.05
CHEMBL1813213 Ki = 9.1 nM 8.04
CHEMBL191045 Ki = 9.3 nM 8.03
CHEMBL1813209 Ki = 10.1 nM 8.00
CHEMBL189526 Ki = 10.4 nM 7.98
CHEMBL187274 Ki = 15.4 nM 7.81
CHEMBL1813215 Ki = 16.9 nM 7.77
CHEMBL190024 Ki = 17.9 nM 7.75
CHEMBL190733 Ki = 23.5 nM 7.63
CHEMBL187901 Ki = 24.1 nM 7.62
CHEMBL1813211 Ki = 27.7 nM 7.56
CHEMBL366069 Ki = 34.3 nM 7.46
CHEMBL20 ACETAZOLAMIDE Ki = 41.0 nM 7.39
CHEMBL1813216 Ki = 72.0 nM 7.14
CHEMBL1813217 Ki = 77.0 nM 7.11
CHEMBL17 DICHLORPHENAMIDE Ki = 345.0 nM 6.46
CHEMBL1813212 Ki = 583.0 nM 6.23