Reaction Details Report a problem with these data
Target
Monocarboxylate transporter 1
Ligand
BDBM21985
Substrate
BDBM22022
Meas. Tech.
SPA Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
4.8±n/a nM
Citation
 Guile, SD; Bantick, JR; Cheshire, DR; Cooper, ME; Davis, AM; Donald, DK; Evans, R; Eyssade, C; Ferguson, DD; Hill, S; Hutchinson, R; Ingall, AH; Kingston, LP; Martin, I; Martin, BP; Mohammed, RT; Murray, C; Perry, MW; Reynolds, RH; Thorne, PV; Wilkinson, DJ; Withnall, J Potent blockers of the monocarboxylate transporter MCT1: novel immunomodulatory compounds. Bioorg Med Chem Lett 16:2260-5 (2006) [PubMed]  Article 
Target
Name:
Monocarboxylate transporter 1
Synonyms:
MCT 1 | MCT1 | MOT1_HUMAN | Monocarboxylate transporter 1 | SLC16A1 | Solute carrier family 16 member 1
Type:
PROTEIN
Mol. Mass.:
53956.64
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1451367
Residue:
500
Sequence:
MPPAVGGPVGYTPPDGGWGWAVVIGAFISIGFSYAFPKSITVFFKEIEGIFHATTSEVSWISSIMLAVMYGGGPISSILVNKYGSRIVMIVGGCLSGCGLIAASFCNTVQQLYVCIGVIGGLGLAFNLNPALTMIGKYFYKRRPLANGLAMAGSPVFLCTLAPLNQVFFGIFGWRGSFLILGGLLLNCCVAGALMRPIGPKPTKAGKDKSKASLEKAGKSGVKKDLHDANTDLIGRHPKQEKRSVFQTINQFLDLTLFTHRGFLLYLSGNVIMFFGLFAPLVFLSSYGKSQHYSSEKSAFLLSILAFVDMVARPSMGLVANTKPIRPRIQYFFAASVVANGVCHMLAPLSTTYVGFCVYAGFFGFAFGWLSSVLFETLMDLVGPQRFSSAVGLVTIVECCPVLLGPPLLGRLNDMYGDYKYTYWACGVVLIISGIYLFIGMGINYRLLAKEQKANEQKKESKEEETSIDVAGKPNEVTKAAESPDQKDTDGGPKEEESPV
  
Inhibitor
Name:
BDBM21985
Synonyms:
5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-3-methyl-1-(2-methylpropyl)-6-(quinolin-4-ylmethyl)-1H,2H,3H,4H-thieno[2,3-d]pyrimidine-2,4-dione | 5-{[(3R)-3-hydroxypyrrolidin-1-yl]carbonyl}-3-methyl-1-(2-methylpropyl)-6-(quinolin-4-ylmethyl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione | BMCL162260 Compound 30 | Thienopyrimidine-2,4-dione, 1
Type:
Small organic molecule
Emp. Form.:
C26H28N4O4S
Mol. Mass.:
492.59
SMILES:
CC(C)Cn1c2sc(Cc3ccnc4ccccc34)c(C(=O)N3CC[C@@H](O)C3)c2c(=O)n(C)c1=O |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM22022
Synonyms:
6-benzyl-7-[(3-hydroxypropyl)sulfanyl]-2-methyl-4-(2-methylpropyl)-1H,2H,6H-pyrrolo[3,4-d]pyridazin-1-one | 6-benzyl-7-[(3-hydroxypropyl)sulfanyl]-2-methyl-4-(2-methylpropyl)-2,6-dihydro-1H-pyrrolo[3,4-d]pyridazin-1-one | [125I]-pyrrolo[3,4-d]pyridazin-1-one
Type:
radiolabeled ligand
Emp. Form.:
C21H27N3O2S
Mol. Mass.:
385.523
SMILES:
CC(C)Cc1nn(C)c(=O)c2c(SCCCO)n(Cc3ccccc3)cc12
Structure:
Search PDB for entries with ligand similarity: