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Assay Detail

CHEMBL2340804

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Binding
Inhibition of human carbonic anhydrase 1 preincubated for 15 mins by CO2 hydration stopped-flow assay
31
Total Activities
31
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 1 (CHEMBL261)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Mono-/dihydroxybenzoic acid esters and phenol pyridinium derivatives as inhibitors of the mammalian carbonic anhydrase isoforms I, II, VII, IX, XII and XIV.
Carta F, Vullo D, Maresca A, Scozzafava A, Supuran CT.
Bioorg Med Chem (2013) 21 : 1564 -1569
PubMed 22668600 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 5.86 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2074640 ETHYL P-COUMARATE 1 6.50
CHEMBL2333960 1 6.41
CHEMBL2333963 1 6.41
CHEMBL2333961 1 6.30
CHEMBL1940391 ISOPROPYL 3-(4-HYDROXYPHENYL)ACRYLATE 1 6.27
CHEMBL466810 1 6.20
CHEMBL486216 1 6.19
CHEMBL2333586 1 6.17
CHEMBL2333587 1 6.17
CHEMBL448695 1 6.16
CHEMBL486027 METHYL PROTOCATECHUATE 1 6.15
CHEMBL2333584 1 6.15
CHEMBL2333588 1 6.14
CHEMBL146816 METHYL P-HYDROXYCINNAMATE 1 6.11
CHEMBL486218 METHYL 3,5-DIHYDROXYBENZOATE 1 6.11
CHEMBL1978880 METHYL 2,5-DIHYDROXYBENZOATE 1 6.09
CHEMBL2333589 1 6.08
CHEMBL486026 METHYL 2,4-DIHYDROXYBENZOATE 1 6.08
CHEMBL2333590 1 6.04
CHEMBL2333585 1 6.01
CHEMBL325372 METHYLPARABEN -1.0 1 5.58
CHEMBL1461 GENTISIC ACID 1 5.38
CHEMBL2333956 1 5.32
CHEMBL269755 3-AMINOPHENOL 1 5.31
CHEMBL2333958 1 5.29
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID 1 5.28
CHEMBL454808 1 5.24
CHEMBL2333959 1 5.20
CHEMBL2333962 ISOPROPYL 4-HYDROXYBENZOATE 1 5.14
CHEMBL2333957 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2074640 ETHYL P-COUMARATE Ki = 320.0 nM 6.50
CHEMBL2333960 Ki = 390.0 nM 6.41
CHEMBL2333963 Ki = 390.0 nM 6.41
CHEMBL2333961 Ki = 500.0 nM 6.30
CHEMBL1940391 ISOPROPYL 3-(4-HYDROXYPHENYL)ACRYLATE Ki = 540.0 nM 6.27
CHEMBL466810 Ki = 630.0 nM 6.20
CHEMBL486216 Ki = 650.0 nM 6.19
CHEMBL2333586 Ki = 680.0 nM 6.17
CHEMBL2333587 Ki = 670.0 nM 6.17
CHEMBL448695 Ki = 690.0 nM 6.16
CHEMBL486027 METHYL PROTOCATECHUATE Ki = 710.0 nM 6.15
CHEMBL2333584 Ki = 710.0 nM 6.15
CHEMBL2333588 Ki = 720.0 nM 6.14
CHEMBL146816 METHYL P-HYDROXYCINNAMATE Ki = 780.0 nM 6.11
CHEMBL486218 METHYL 3,5-DIHYDROXYBENZOATE Ki = 770.0 nM 6.11
CHEMBL1978880 METHYL 2,5-DIHYDROXYBENZOATE Ki = 820.0 nM 6.09
CHEMBL2333589 Ki = 830.0 nM 6.08
CHEMBL486026 METHYL 2,4-DIHYDROXYBENZOATE Ki = 830.0 nM 6.08
CHEMBL2333590 Ki = 920.0 nM 6.04
CHEMBL2333585 Ki = 970.0 nM 6.01
CHEMBL325372 METHYLPARABEN Ki = 2600.0 nM 5.58
CHEMBL1461 GENTISIC ACID Ki = 4200.0 nM 5.38
CHEMBL2333956 Ki = 4800.0 nM 5.32
CHEMBL269755 3-AMINOPHENOL Ki = 4900.0 nM 5.31
CHEMBL2333958 Ki = 5100.0 nM 5.29
CHEMBL328910 2,4-DIHYDROXYBENZOIC ACID Ki = 5200.0 nM 5.28
CHEMBL454808 Ki = 5700.0 nM 5.24
CHEMBL2333959 Ki = 6300.0 nM 5.20
CHEMBL2333962 ISOPROPYL 4-HYDROXYBENZOATE Ki = 7300.0 nM 5.14
CHEMBL2333957 Ki = 7400.0 nM 5.13
CHEMBL15841 ETHYLPARABEN Ki = 7900.0 nM 5.10